Chemicals

Showing 11251–11400 of 41137 results

  • Bestatin is an aminopeptidase inhibitor originally isolated from S. olivoreticuli.{33261} It inhibits aminopeptidase B (IC50 = 0.05 µg/ml), aminopeptidase N (IC50 = 16.9 µM), leucine aminopeptidase (IC50 = 0.01 µg/ml), and the aminopeptidase activity of leukotriene A4 (LTA4) hydrolase (Kapp = 172 nM).{33261,48771,91} It is selective for these aminopeptidases over aminopeptidase A, trypsin, chymotrypsin, elastase, papain, pepsin, and thermolysin.{33261} Bestatin inhibits the production of LTB4 (Item No. 20110) in erythrocytes when used at a concentration of 70 µM.{91} It increases the expression of Akt, inhibits proliferation, migration, and invasion, and induces autophagy and apoptosis in 5637 bladder cancer cells.{48772} Bestatin (5 and 15 mg/kg) decreases serum levels of LTB4 and reduces tumor growth in a patient-derived xenograft (PDX) mouse model of colorectal cancer.{48773}  

     

    Brand:
    Cayman
    SKU:70520 - 100 mg

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  • Bestatin is an aminopeptidase inhibitor originally isolated from S. olivoreticuli.{33261} It inhibits aminopeptidase B (IC50 = 0.05 µg/ml), aminopeptidase N (IC50 = 16.9 µM), leucine aminopeptidase (IC50 = 0.01 µg/ml), and the aminopeptidase activity of leukotriene A4 (LTA4) hydrolase (Kapp = 172 nM).{33261,48771,91} It is selective for these aminopeptidases over aminopeptidase A, trypsin, chymotrypsin, elastase, papain, pepsin, and thermolysin.{33261} Bestatin inhibits the production of LTB4 (Item No. 20110) in erythrocytes when used at a concentration of 70 µM.{91} It increases the expression of Akt, inhibits proliferation, migration, and invasion, and induces autophagy and apoptosis in 5637 bladder cancer cells.{48772} Bestatin (5 and 15 mg/kg) decreases serum levels of LTB4 and reduces tumor growth in a patient-derived xenograft (PDX) mouse model of colorectal cancer.{48773}  

     

    Brand:
    Cayman
    SKU:70520 - 5 mg

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  • Bestatin is an aminopeptidase inhibitor originally isolated from S. olivoreticuli.{33261} It inhibits aminopeptidase B (IC50 = 0.05 µg/ml), aminopeptidase N (IC50 = 16.9 µM), leucine aminopeptidase (IC50 = 0.01 µg/ml), and the aminopeptidase activity of leukotriene A4 (LTA4) hydrolase (Kapp = 172 nM).{33261,48771,91} It is selective for these aminopeptidases over aminopeptidase A, trypsin, chymotrypsin, elastase, papain, pepsin, and thermolysin.{33261} Bestatin inhibits the production of LTB4 (Item No. 20110) in erythrocytes when used at a concentration of 70 µM.{91} It increases the expression of Akt, inhibits proliferation, migration, and invasion, and induces autophagy and apoptosis in 5637 bladder cancer cells.{48772} Bestatin (5 and 15 mg/kg) decreases serum levels of LTB4 and reduces tumor growth in a patient-derived xenograft (PDX) mouse model of colorectal cancer.{48773}  

     

    Brand:
    Cayman
    SKU:70520 - 50 mg

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  • Betahistine is a histamine H3 receptor antagonist and histamine H1 receptor agonist.{45328} In vivo, betahistine dilates pre-capillary arterioles and increases blood flow to the stria vascularis in guinea pigs.{45329,45330} Betahistine (8 mg/kg) reduces weight gain and increased feeding behavior induced by olanzapine (Item No. 11937) in female rats.{45331} Formulations containing betahistine have been used in the treatment of balance disorders and vertigo symptoms associated with Meniere’s disease.  

     

    Brand:
    Cayman
    SKU:27602 - 1 g

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  • Betahistine is a histamine H3 receptor antagonist and histamine H1 receptor agonist.{45328} In vivo, betahistine dilates pre-capillary arterioles and increases blood flow to the stria vascularis in guinea pigs.{45329,45330} Betahistine (8 mg/kg) reduces weight gain and increased feeding behavior induced by olanzapine (Item No. 11937) in female rats.{45331} Formulations containing betahistine have been used in the treatment of balance disorders and vertigo symptoms associated with Meniere’s disease.  

     

    Brand:
    Cayman
    SKU:27602 - 10 g

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  • Betahistine is a histamine H3 receptor antagonist and histamine H1 receptor agonist.{45328} In vivo, betahistine dilates pre-capillary arterioles and increases blood flow to the stria vascularis in guinea pigs.{45329,45330} Betahistine (8 mg/kg) reduces weight gain and increased feeding behavior induced by olanzapine (Item No. 11937) in female rats.{45331} Formulations containing betahistine have been used in the treatment of balance disorders and vertigo symptoms associated with Meniere’s disease.  

     

    Brand:
    Cayman
    SKU:27602 - 5 g

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  • Betaine is a quaternary ammonium compound with diverse biological activities.{47329,47330,47331} It has been found in spinach and can be acquired through the diet or formed via oxidation of betaine aldehyde (Item No. 17270) during choline metabolism in the liver and kidney.{47329,47332} Betaine has roles in osmoregulation and serves as a methyl donor in the conversion of homocysteine to methionine.{47329} Betaine (1.5% w/v in drinking water) reduces serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activity, increases serum HDL levels, decreases serum LDL levels, and reduces hepatic steatosis and inflammation in a mouse model of non-alcoholic fatty liver disease (NAFLD) induced by a methionine- and choline-deficient diet.{47330} It also reduces plasma levels of total homocysteine (tHcy), S-adenosylmethionine (AdoMet), S-adenosylhomocysteine (AdoHcy; Item No. 13603), and cystathionine, and attenuates hypercoagulation in a mouse model of homocystinuria.{47331} Formulations containing betaine have been used in the treatment of homocystinuria.  

     

    Brand:
    Cayman
    SKU:26814 - 100 g

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  • Betaine is a quaternary ammonium compound with diverse biological activities.{47329,47330,47331} It has been found in spinach and can be acquired through the diet or formed via oxidation of betaine aldehyde (Item No. 17270) during choline metabolism in the liver and kidney.{47329,47332} Betaine has roles in osmoregulation and serves as a methyl donor in the conversion of homocysteine to methionine.{47329} Betaine (1.5% w/v in drinking water) reduces serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activity, increases serum HDL levels, decreases serum LDL levels, and reduces hepatic steatosis and inflammation in a mouse model of non-alcoholic fatty liver disease (NAFLD) induced by a methionine- and choline-deficient diet.{47330} It also reduces plasma levels of total homocysteine (tHcy), S-adenosylmethionine (AdoMet), S-adenosylhomocysteine (AdoHcy; Item No. 13603), and cystathionine, and attenuates hypercoagulation in a mouse model of homocystinuria.{47331} Formulations containing betaine have been used in the treatment of homocystinuria.  

     

    Brand:
    Cayman
    SKU:26814 - 250 g

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  • Betaine is a quaternary ammonium compound with diverse biological activities.{47329,47330,47331} It has been found in spinach and can be acquired through the diet or formed via oxidation of betaine aldehyde (Item No. 17270) during choline metabolism in the liver and kidney.{47329,47332} Betaine has roles in osmoregulation and serves as a methyl donor in the conversion of homocysteine to methionine.{47329} Betaine (1.5% w/v in drinking water) reduces serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activity, increases serum HDL levels, decreases serum LDL levels, and reduces hepatic steatosis and inflammation in a mouse model of non-alcoholic fatty liver disease (NAFLD) induced by a methionine- and choline-deficient diet.{47330} It also reduces plasma levels of total homocysteine (tHcy), S-adenosylmethionine (AdoMet), S-adenosylhomocysteine (AdoHcy; Item No. 13603), and cystathionine, and attenuates hypercoagulation in a mouse model of homocystinuria.{47331} Formulations containing betaine have been used in the treatment of homocystinuria.  

     

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    Cayman
    SKU:26814 - 500 g

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  • Betaine aldehyde is the physiological intermediate in the oxidation of choline to betaine. This step is involved in glycine, serine, and threonine metabolism.  

     

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    SKU:-

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  • Betaine aldehyde is the physiological intermediate in the oxidation of choline to betaine. This step is involved in glycine, serine, and threonine metabolism.  

     

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  • Betaine aldehyde is the physiological intermediate in the oxidation of choline to betaine. This step is involved in glycine, serine, and threonine metabolism.  

     

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  • Betaine aldehyde is the physiological intermediate in the oxidation of choline to betaine. This step is involved in glycine, serine, and threonine metabolism.  

     

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  • Betamethasone is a synthetic corticosteroid. Like other corticosteroids, betamethasone has anti-inflammatory actions.{32497} Betamethasone also accelerates fetal lung maturation and has been used to decrease neonatal mortality and morbidity in infants born before 34 weeks of gestation.{32498}  

     

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    Cayman
    SKU:20363 -

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  • Betamethasone is a synthetic corticosteroid. Like other corticosteroids, betamethasone has anti-inflammatory actions.{32497} Betamethasone also accelerates fetal lung maturation and has been used to decrease neonatal mortality and morbidity in infants born before 34 weeks of gestation.{32498}  

     

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    Cayman
    SKU:20363 -

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  • Betamethasone is a synthetic corticosteroid. Like other corticosteroids, betamethasone has anti-inflammatory actions.{32497} Betamethasone also accelerates fetal lung maturation and has been used to decrease neonatal mortality and morbidity in infants born before 34 weeks of gestation.{32498}  

     

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    Cayman
    SKU:20363 -

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  • Betamethasone is a synthetic corticosteroid. Like other corticosteroids, betamethasone has anti-inflammatory actions.{32497} Betamethasone also accelerates fetal lung maturation and has been used to decrease neonatal mortality and morbidity in infants born before 34 weeks of gestation.{32498}  

     

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    Cayman
    SKU:20363 -

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  • Betamethasone 17-valerate is a glucocorticoid with anti-inflammatory activity.{48033,40484} It inhibits the binding of the radiolabeled glucocorticoid dexamethasone to human epidermis and mouse skin (IC50s = 5 and 6 nM, respectively).{48033} Topical application of betamethasone 17-valerate ointment (0.12%) blocks increases in ear weight in a rat model of ear edema induced by croton oil.{40484} Formulations containing betamethasone 17-valerate have been used in the treatment of corticosteroid-responsive dermatoses of the scalp.  

     

    Brand:
    Cayman
    SKU:25640 - 100 mg

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  • Betamethasone 17-valerate is a glucocorticoid with anti-inflammatory activity.{48033,40484} It inhibits the binding of the radiolabeled glucocorticoid dexamethasone to human epidermis and mouse skin (IC50s = 5 and 6 nM, respectively).{48033} Topical application of betamethasone 17-valerate ointment (0.12%) blocks increases in ear weight in a rat model of ear edema induced by croton oil.{40484} Formulations containing betamethasone 17-valerate have been used in the treatment of corticosteroid-responsive dermatoses of the scalp.  

     

    Brand:
    Cayman
    SKU:25640 - 25 mg

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  • Betamethasone 17-valerate is a glucocorticoid with anti-inflammatory activity.{48033,40484} It inhibits the binding of the radiolabeled glucocorticoid dexamethasone to human epidermis and mouse skin (IC50s = 5 and 6 nM, respectively).{48033} Topical application of betamethasone 17-valerate ointment (0.12%) blocks increases in ear weight in a rat model of ear edema induced by croton oil.{40484} Formulations containing betamethasone 17-valerate have been used in the treatment of corticosteroid-responsive dermatoses of the scalp.  

     

    Brand:
    Cayman
    SKU:25640 - 50 mg

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  • Betamethasone 17-valerate is a glucocorticoid with anti-inflammatory activity.{48033,40484} It inhibits the binding of the radiolabeled glucocorticoid dexamethasone to human epidermis and mouse skin (IC50s = 5 and 6 nM, respectively).{48033} Topical application of betamethasone 17-valerate ointment (0.12%) blocks increases in ear weight in a rat model of ear edema induced by croton oil.{40484} Formulations containing betamethasone 17-valerate have been used in the treatment of corticosteroid-responsive dermatoses of the scalp.  

     

    Brand:
    Cayman
    SKU:25640 - 500 mg

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  • Betaxolol (hydrochloride) (Item No. 26285) is an analytical reference standard categorized as a β1-adrenergic receptor antagonist.{25151} Formulations containing β-adrenergic receptor antagonists have been used to enhance physical performance in athletes.{48104,46103} This product is intended for use in analytical forensic applications. This product is also available as a general research tool (Item No. 18625).  

     

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    Cayman
    SKU:26285 - 1 mg

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  • Betaxolol is a selective β1-adrenergic receptor antagonist (log KDs = -8.21, -7.38, and -5.97 for β1, β2, and β3, respectively).{25151} This beta-blocker has been used to reduce intraocular pressure in research models of ocular hypertension and glaucoma.{30089,30088,30087} It is also reported to act as a neuroprotective agent in animals, attenuating excitotoxicity or ischemia-induced damage to retinal ganglion cells.{30086}  

     

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    Cayman
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  • Betaxolol is a selective β1-adrenergic receptor antagonist (log KDs = -8.21, -7.38, and -5.97 for β1, β2, and β3, respectively).{25151} This beta-blocker has been used to reduce intraocular pressure in research models of ocular hypertension and glaucoma.{30089,30088,30087} It is also reported to act as a neuroprotective agent in animals, attenuating excitotoxicity or ischemia-induced damage to retinal ganglion cells.{30086}  

     

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    Cayman
    SKU:-

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  • Betaxolol (hydrochloride) (Item No. 26285) is an analytical reference standard categorized as a β1-adrenergic receptor antagonist.{25151} Formulations containing β-adrenergic receptor antagonists have been used to enhance physical performance in athletes.{48104,46103} This product is intended for use in analytical forensic applications. This product is also available as a general research tool (Item No. 18625).  

     

    Brand:
    Cayman
    SKU:26285 - 5 mg

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  • Betaxolol is a selective β1-adrenergic receptor antagonist (log KDs = -8.21, -7.38, and -5.97 for β1, β2, and β3, respectively).{25151} This beta-blocker has been used to reduce intraocular pressure in research models of ocular hypertension and glaucoma.{30089,30088,30087} It is also reported to act as a neuroprotective agent in animals, attenuating excitotoxicity or ischemia-induced damage to retinal ganglion cells.{30086}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Betaxolol is a selective β1-adrenergic receptor antagonist (log KDs = -8.21, -7.38, and -5.97 for β1, β2, and β3, respectively).{25151} This beta-blocker has been used to reduce intraocular pressure in research models of ocular hypertension and glaucoma.{30089,30088,30087} It is also reported to act as a neuroprotective agent in animals, attenuating excitotoxicity or ischemia-induced damage to retinal ganglion cells.{30086}  

     

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    Cayman
    SKU:-

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  • Bethanechol is an agonist of muscarinic acetylcholine receptors with IC50 values of 1,837, 25, 631, 317, and 393 µM for M1-5, respectively, in a radioligand binding assay using CHO cells expressing the human receptors.{40682} It inhibits M2-mediated increases in cyclic AMP induced by isoproterenol (Item No. 15592) in isolated guinea pig small intestine (IC50 = 127 µM).{18340} Bethanechol increases basal tone of isolated porcine intravesical ureter (EC50 = 4.27 µM).{27105} It also induces fluid secretion in the ileum, duodenum, and jejunum of anesthetized rats when administered at a dose of 60 µg/kg.{40787} Formulations containing bethanechol have been used to increase urination and improve smooth muscle tone in the gastrointestinal tract.  

     

    Brand:
    Cayman
    SKU:23830 - 1 g

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  • Bethanechol is an agonist of muscarinic acetylcholine receptors with IC50 values of 1,837, 25, 631, 317, and 393 µM for M1-5, respectively, in a radioligand binding assay using CHO cells expressing the human receptors.{40682} It inhibits M2-mediated increases in cyclic AMP induced by isoproterenol (Item No. 15592) in isolated guinea pig small intestine (IC50 = 127 µM).{18340} Bethanechol increases basal tone of isolated porcine intravesical ureter (EC50 = 4.27 µM).{27105} It also induces fluid secretion in the ileum, duodenum, and jejunum of anesthetized rats when administered at a dose of 60 µg/kg.{40787} Formulations containing bethanechol have been used to increase urination and improve smooth muscle tone in the gastrointestinal tract.  

     

    Brand:
    Cayman
    SKU:23830 - 10 g

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  • Bethanechol is an agonist of muscarinic acetylcholine receptors with IC50 values of 1,837, 25, 631, 317, and 393 µM for M1-5, respectively, in a radioligand binding assay using CHO cells expressing the human receptors.{40682} It inhibits M2-mediated increases in cyclic AMP induced by isoproterenol (Item No. 15592) in isolated guinea pig small intestine (IC50 = 127 µM).{18340} Bethanechol increases basal tone of isolated porcine intravesical ureter (EC50 = 4.27 µM).{27105} It also induces fluid secretion in the ileum, duodenum, and jejunum of anesthetized rats when administered at a dose of 60 µg/kg.{40787} Formulations containing bethanechol have been used to increase urination and improve smooth muscle tone in the gastrointestinal tract.  

     

    Brand:
    Cayman
    SKU:23830 - 25 g

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  • Bethanechol is an agonist of muscarinic acetylcholine receptors with IC50 values of 1,837, 25, 631, 317, and 393 µM for M1-5, respectively, in a radioligand binding assay using CHO cells expressing the human receptors.{40682} It inhibits M2-mediated increases in cyclic AMP induced by isoproterenol (Item No. 15592) in isolated guinea pig small intestine (IC50 = 127 µM).{18340} Bethanechol increases basal tone of isolated porcine intravesical ureter (EC50 = 4.27 µM).{27105} It also induces fluid secretion in the ileum, duodenum, and jejunum of anesthetized rats when administered at a dose of 60 µg/kg.{40787} Formulations containing bethanechol have been used to increase urination and improve smooth muscle tone in the gastrointestinal tract.  

     

    Brand:
    Cayman
    SKU:23830 - 5 g

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  • BETP is a positive allosteric modulator of glucagon-like peptide 1 receptor (GLP-1R; EC50 = 0.66 µM in a reporter assay).{58027} It is selective for GLP-1R over GLP-2R, as well as glucose-dependent insulinotropic polypeptide, glucagon, and the parathyroid hormone receptors. BETP induces cAMP accumulation and intracellular calcium mobilization in CHO cells expressing human GLP-1R (EC50s = 5 and 6.3 µM, respectively).{58028} It increases glucose-induced insulin secretion in pancreatic islets isolated from patients with type 2 diabetes when used at concentrations of 3 and 10 µM. BETP (10 mg/kg) increases plasma insulin levels in an intravenous glucose tolerance test in rats.  

     

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    Cayman
    SKU:31116 - 1 mg

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  • BETP is a positive allosteric modulator of glucagon-like peptide 1 receptor (GLP-1R; EC50 = 0.66 µM in a reporter assay).{58027} It is selective for GLP-1R over GLP-2R, as well as glucose-dependent insulinotropic polypeptide, glucagon, and the parathyroid hormone receptors. BETP induces cAMP accumulation and intracellular calcium mobilization in CHO cells expressing human GLP-1R (EC50s = 5 and 6.3 µM, respectively).{58028} It increases glucose-induced insulin secretion in pancreatic islets isolated from patients with type 2 diabetes when used at concentrations of 3 and 10 µM. BETP (10 mg/kg) increases plasma insulin levels in an intravenous glucose tolerance test in rats.  

     

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    Cayman
    SKU:31116 - 10 mg

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  • BETP is a positive allosteric modulator of glucagon-like peptide 1 receptor (GLP-1R; EC50 = 0.66 µM in a reporter assay).{58027} It is selective for GLP-1R over GLP-2R, as well as glucose-dependent insulinotropic polypeptide, glucagon, and the parathyroid hormone receptors. BETP induces cAMP accumulation and intracellular calcium mobilization in CHO cells expressing human GLP-1R (EC50s = 5 and 6.3 µM, respectively).{58028} It increases glucose-induced insulin secretion in pancreatic islets isolated from patients with type 2 diabetes when used at concentrations of 3 and 10 µM. BETP (10 mg/kg) increases plasma insulin levels in an intravenous glucose tolerance test in rats.  

     

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    Cayman
    SKU:31116 - 25 mg

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  • BETP is a positive allosteric modulator of glucagon-like peptide 1 receptor (GLP-1R; EC50 = 0.66 µM in a reporter assay).{58027} It is selective for GLP-1R over GLP-2R, as well as glucose-dependent insulinotropic polypeptide, glucagon, and the parathyroid hormone receptors. BETP induces cAMP accumulation and intracellular calcium mobilization in CHO cells expressing human GLP-1R (EC50s = 5 and 6.3 µM, respectively).{58028} It increases glucose-induced insulin secretion in pancreatic islets isolated from patients with type 2 diabetes when used at concentrations of 3 and 10 µM. BETP (10 mg/kg) increases plasma insulin levels in an intravenous glucose tolerance test in rats.  

     

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    Cayman
    SKU:31116 - 5 mg

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  • Betrixaban is an inhibitor of the serine protease Factor Xa (Ki = 0.117 nM; IC50 = 1.5 nM), the enzyme that activates prothrombin in the blood coagulation cascade.{36456} It is selective for Factor Xa over hERG channels (Ki = 1.8 µM; IC50 = 8.9 µM), indicating a low potential for adverse cardiac effects. In vitro, betrixaban inhibits thrombin generation when used at concentrations ranging from 5 to 25 ng/mL in a tissue factor-induced thrombin generation assay.{36457} In vivo, it inhibits thrombus mass formation by 76% in a rabbit clot accretion model when used at a dose of 3 mg/kg. Formulations containing betrixaban have been used as anticoagulants in the treatment and prevention of venous thromboembolism.{36458}  

     

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    Cayman
    SKU:21563 -

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  • Betrixaban is an inhibitor of the serine protease Factor Xa (Ki = 0.117 nM; IC50 = 1.5 nM), the enzyme that activates prothrombin in the blood coagulation cascade.{36456} It is selective for Factor Xa over hERG channels (Ki = 1.8 µM; IC50 = 8.9 µM), indicating a low potential for adverse cardiac effects. In vitro, betrixaban inhibits thrombin generation when used at concentrations ranging from 5 to 25 ng/mL in a tissue factor-induced thrombin generation assay.{36457} In vivo, it inhibits thrombus mass formation by 76% in a rabbit clot accretion model when used at a dose of 3 mg/kg. Formulations containing betrixaban have been used as anticoagulants in the treatment and prevention of venous thromboembolism.{36458}  

     

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    Cayman
    SKU:21563 -

    Out of stock

  • Betrixaban is an inhibitor of the serine protease Factor Xa (Ki = 0.117 nM; IC50 = 1.5 nM), the enzyme that activates prothrombin in the blood coagulation cascade.{36456} It is selective for Factor Xa over hERG channels (Ki = 1.8 µM; IC50 = 8.9 µM), indicating a low potential for adverse cardiac effects. In vitro, betrixaban inhibits thrombin generation when used at concentrations ranging from 5 to 25 ng/mL in a tissue factor-induced thrombin generation assay.{36457} In vivo, it inhibits thrombus mass formation by 76% in a rabbit clot accretion model when used at a dose of 3 mg/kg. Formulations containing betrixaban have been used as anticoagulants in the treatment and prevention of venous thromboembolism.{36458}  

     

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    Cayman
    SKU:21563 -

    Out of stock

  • Betrixaban is an inhibitor of the serine protease Factor Xa (Ki = 0.117 nM; IC50 = 1.5 nM), the enzyme that activates prothrombin in the blood coagulation cascade.{36456} It is selective for Factor Xa over hERG channels (Ki = 1.8 µM; IC50 = 8.9 µM), indicating a low potential for adverse cardiac effects. In vitro, betrixaban inhibits thrombin generation when used at concentrations ranging from 5 to 25 ng/mL in a tissue factor-induced thrombin generation assay.{36457} In vivo, it inhibits thrombus mass formation by 76% in a rabbit clot accretion model when used at a dose of 3 mg/kg. Formulations containing betrixaban have been used as anticoagulants in the treatment and prevention of venous thromboembolism.{36458}  

     

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    Cayman
    SKU:21563 -

    Out of stock

  • Sterol regulatory element binding protein 2 (SREBP-2) regulates cholesterol synthesis by activating the transcription of genes for HMG-CoA reductase and other enzymes of the cholesterol synthetic pathway.{13851,13853} When cellular sterol levels are high, SREBP is bound by SCAP and Insig to ER membranes as a glycosylated precursor protein. Upon cholesterol depletion, the protein is cleaved to its active form and translocated into the nucleus to stimulate transcription of genes involved in the uptake and synthesis of cholesterol.{13148} Betulin, the precursor of betulinic acid, is a pentacyclic triterpene found in the bark of birch trees. Betulin inhibits the SREBP-driven pathway of cholesterol and fatty acid biosynthesis by promoting SCAP–Insig binding which prevents the activation and release of SREBP-2 from the ER.{19894} At 15-30 mg/kg/day, betulin has been shown to decrease lipid levels and increase insulin sensitivity in mice fed a western-type diet.{19894} In an atherosclerosis disease model, 30 mg/kg/day betulin can reduce the size and improve the stability of atherosclerotic plaques in LDLR-knockout mice.{19894} At 2.5-5 μg/ml betulin, in combination with cholesterol, demonstrates anticancer effects by inducing apoptosis in Jurkat cells, A549 lung carcinoma cells, and HeLa cervical carcinoma cells.{22046}  

     

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    Cayman
    SKU:11041 - 1 g

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  • Sterol regulatory element binding protein 2 (SREBP-2) regulates cholesterol synthesis by activating the transcription of genes for HMG-CoA reductase and other enzymes of the cholesterol synthetic pathway.{13851,13853} When cellular sterol levels are high, SREBP is bound by SCAP and Insig to ER membranes as a glycosylated precursor protein. Upon cholesterol depletion, the protein is cleaved to its active form and translocated into the nucleus to stimulate transcription of genes involved in the uptake and synthesis of cholesterol.{13148} Betulin, the precursor of betulinic acid, is a pentacyclic triterpene found in the bark of birch trees. Betulin inhibits the SREBP-driven pathway of cholesterol and fatty acid biosynthesis by promoting SCAP–Insig binding which prevents the activation and release of SREBP-2 from the ER.{19894} At 15-30 mg/kg/day, betulin has been shown to decrease lipid levels and increase insulin sensitivity in mice fed a western-type diet.{19894} In an atherosclerosis disease model, 30 mg/kg/day betulin can reduce the size and improve the stability of atherosclerotic plaques in LDLR-knockout mice.{19894} At 2.5-5 μg/ml betulin, in combination with cholesterol, demonstrates anticancer effects by inducing apoptosis in Jurkat cells, A549 lung carcinoma cells, and HeLa cervical carcinoma cells.{22046}  

     

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    Cayman
    SKU:11041 - 250 mg

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  • Sterol regulatory element binding protein 2 (SREBP-2) regulates cholesterol synthesis by activating the transcription of genes for HMG-CoA reductase and other enzymes of the cholesterol synthetic pathway.{13851,13853} When cellular sterol levels are high, SREBP is bound by SCAP and Insig to ER membranes as a glycosylated precursor protein. Upon cholesterol depletion, the protein is cleaved to its active form and translocated into the nucleus to stimulate transcription of genes involved in the uptake and synthesis of cholesterol.{13148} Betulin, the precursor of betulinic acid, is a pentacyclic triterpene found in the bark of birch trees. Betulin inhibits the SREBP-driven pathway of cholesterol and fatty acid biosynthesis by promoting SCAP–Insig binding which prevents the activation and release of SREBP-2 from the ER.{19894} At 15-30 mg/kg/day, betulin has been shown to decrease lipid levels and increase insulin sensitivity in mice fed a western-type diet.{19894} In an atherosclerosis disease model, 30 mg/kg/day betulin can reduce the size and improve the stability of atherosclerotic plaques in LDLR-knockout mice.{19894} At 2.5-5 μg/ml betulin, in combination with cholesterol, demonstrates anticancer effects by inducing apoptosis in Jurkat cells, A549 lung carcinoma cells, and HeLa cervical carcinoma cells.{22046}  

     

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    Cayman
    SKU:11041 - 5 g

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  • Sterol regulatory element binding protein 2 (SREBP-2) regulates cholesterol synthesis by activating the transcription of genes for HMG-CoA reductase and other enzymes of the cholesterol synthetic pathway.{13851,13853} When cellular sterol levels are high, SREBP is bound by SCAP and Insig to ER membranes as a glycosylated precursor protein. Upon cholesterol depletion, the protein is cleaved to its active form and translocated into the nucleus to stimulate transcription of genes involved in the uptake and synthesis of cholesterol.{13148} Betulin, the precursor of betulinic acid, is a pentacyclic triterpene found in the bark of birch trees. Betulin inhibits the SREBP-driven pathway of cholesterol and fatty acid biosynthesis by promoting SCAP–Insig binding which prevents the activation and release of SREBP-2 from the ER.{19894} At 15-30 mg/kg/day, betulin has been shown to decrease lipid levels and increase insulin sensitivity in mice fed a western-type diet.{19894} In an atherosclerosis disease model, 30 mg/kg/day betulin can reduce the size and improve the stability of atherosclerotic plaques in LDLR-knockout mice.{19894} At 2.5-5 μg/ml betulin, in combination with cholesterol, demonstrates anticancer effects by inducing apoptosis in Jurkat cells, A549 lung carcinoma cells, and HeLa cervical carcinoma cells.{22046}  

     

    Brand:
    Cayman
    SKU:11041 - 500 mg

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  • Betulinic acid is a natural plant triterpenoid that is structurally related to mammalian bile acids. It is an agonist of the G protein-coupled bile acid receptor TGR5 (EC50 = 1 µM), which might be linked with its ability to alter gene expression and fatty liver development in cells and mice given ethanol.{24274,24272,24270} Betulinic acid also reduces NF-κB signaling and expression of microRNA-33 in LPS-treated macrophages, increasing levels of the ATP-binding cassette (ABC) cholesterol transporter ABCA1.{24273} It also inhibits replication of HIV-1 (IC50 = 1.4 µM) and has cytotoxic effects against cancer cells.{24270,22046}  

     

    Brand:
    Cayman
    SKU:11686 - 100 mg

    Available on backorder

  • Betulinic acid is a natural plant triterpenoid that is structurally related to mammalian bile acids. It is an agonist of the G protein-coupled bile acid receptor TGR5 (EC50 = 1 µM), which might be linked with its ability to alter gene expression and fatty liver development in cells and mice given ethanol.{24274,24272,24270} Betulinic acid also reduces NF-κB signaling and expression of microRNA-33 in LPS-treated macrophages, increasing levels of the ATP-binding cassette (ABC) cholesterol transporter ABCA1.{24273} It also inhibits replication of HIV-1 (IC50 = 1.4 µM) and has cytotoxic effects against cancer cells.{24270,22046}  

     

    Brand:
    Cayman
    SKU:11686 - 250 mg

    Available on backorder

  • Betulinic acid is a natural plant triterpenoid that is structurally related to mammalian bile acids. It is an agonist of the G protein-coupled bile acid receptor TGR5 (EC50 = 1 µM), which might be linked with its ability to alter gene expression and fatty liver development in cells and mice given ethanol.{24274,24272,24270} Betulinic acid also reduces NF-κB signaling and expression of microRNA-33 in LPS-treated macrophages, increasing levels of the ATP-binding cassette (ABC) cholesterol transporter ABCA1.{24273} It also inhibits replication of HIV-1 (IC50 = 1.4 µM) and has cytotoxic effects against cancer cells.{24270,22046}  

     

    Brand:
    Cayman
    SKU:11686 - 50 mg

    Available on backorder

  • Betulinic acid is a natural plant triterpenoid that is structurally related to mammalian bile acids. It is an agonist of the G protein-coupled bile acid receptor TGR5 (EC50 = 1 µM), which might be linked with its ability to alter gene expression and fatty liver development in cells and mice given ethanol.{24274,24272,24270} Betulinic acid also reduces NF-κB signaling and expression of microRNA-33 in LPS-treated macrophages, increasing levels of the ATP-binding cassette (ABC) cholesterol transporter ABCA1.{24273} It also inhibits replication of HIV-1 (IC50 = 1.4 µM) and has cytotoxic effects against cancer cells.{24270,22046}  

     

    Brand:
    Cayman
    SKU:11686 - 500 mg

    Available on backorder

  • Betulinic aldehyde is a triterpenoid that has been found in Z. cambodiana and has diverse biological activities.{48464,48465,48466,48467} It is active against P. falciparum (IC50 = 6.5 μg/ml) and M. tuberculosis (MIC = 25 μg/ml) in vitro, as well as laboratory and clinical isolates of methicillin-resistant and -sensitive S. aureus (MICs = 128-512 and 8-512 μg/ml, respectively).{48464,48465} Betulinic aldehyde inhibits dengue virus non-structural protein 5 (NS5) RNA-dependent RNA polymerase (IC50 = 6.1 μM) and inhibits dengue virus type 2 replication by 20 and 55% when used at concentrations of 5 and 10 μg/ml, respectively.{48466} It also inhibits growth of leukemia, melanoma, neuroblastoma, and normal fibroblast cell lines (IC50s = 1.1-4.9, 9.6-10.6, 7.5-8.8, and 18.5 μM, respectively).{48467}  

     

    Brand:
    Cayman
    SKU:27810 - 1 mg

    Available on backorder

  • Betulinic aldehyde is a triterpenoid that has been found in Z. cambodiana and has diverse biological activities.{48464,48465,48466,48467} It is active against P. falciparum (IC50 = 6.5 μg/ml) and M. tuberculosis (MIC = 25 μg/ml) in vitro, as well as laboratory and clinical isolates of methicillin-resistant and -sensitive S. aureus (MICs = 128-512 and 8-512 μg/ml, respectively).{48464,48465} Betulinic aldehyde inhibits dengue virus non-structural protein 5 (NS5) RNA-dependent RNA polymerase (IC50 = 6.1 μM) and inhibits dengue virus type 2 replication by 20 and 55% when used at concentrations of 5 and 10 μg/ml, respectively.{48466} It also inhibits growth of leukemia, melanoma, neuroblastoma, and normal fibroblast cell lines (IC50s = 1.1-4.9, 9.6-10.6, 7.5-8.8, and 18.5 μM, respectively).{48467}  

     

    Brand:
    Cayman
    SKU:27810 - 10 mg

    Available on backorder

  • Betulinic aldehyde is a triterpenoid that has been found in Z. cambodiana and has diverse biological activities.{48464,48465,48466,48467} It is active against P. falciparum (IC50 = 6.5 μg/ml) and M. tuberculosis (MIC = 25 μg/ml) in vitro, as well as laboratory and clinical isolates of methicillin-resistant and -sensitive S. aureus (MICs = 128-512 and 8-512 μg/ml, respectively).{48464,48465} Betulinic aldehyde inhibits dengue virus non-structural protein 5 (NS5) RNA-dependent RNA polymerase (IC50 = 6.1 μM) and inhibits dengue virus type 2 replication by 20 and 55% when used at concentrations of 5 and 10 μg/ml, respectively.{48466} It also inhibits growth of leukemia, melanoma, neuroblastoma, and normal fibroblast cell lines (IC50s = 1.1-4.9, 9.6-10.6, 7.5-8.8, and 18.5 μM, respectively).{48467}  

     

    Brand:
    Cayman
    SKU:27810 - 25 mg

    Available on backorder

  • Betulinic aldehyde is a triterpenoid that has been found in Z. cambodiana and has diverse biological activities.{48464,48465,48466,48467} It is active against P. falciparum (IC50 = 6.5 μg/ml) and M. tuberculosis (MIC = 25 μg/ml) in vitro, as well as laboratory and clinical isolates of methicillin-resistant and -sensitive S. aureus (MICs = 128-512 and 8-512 μg/ml, respectively).{48464,48465} Betulinic aldehyde inhibits dengue virus non-structural protein 5 (NS5) RNA-dependent RNA polymerase (IC50 = 6.1 μM) and inhibits dengue virus type 2 replication by 20 and 55% when used at concentrations of 5 and 10 μg/ml, respectively.{48466} It also inhibits growth of leukemia, melanoma, neuroblastoma, and normal fibroblast cell lines (IC50s = 1.1-4.9, 9.6-10.6, 7.5-8.8, and 18.5 μM, respectively).{48467}  

     

    Brand:
    Cayman
    SKU:27810 - 5 mg

    Available on backorder

  • Betulonic acid is a triterpenoid that has been found in B. chinensis and has diverse biological activities, including antiparasitic, antiviral, and anticancer properties.{52273,52274,52275,52276} It is active against the chloroquine-resistant P. falciparum W2 clone (IC50 = 10.01 µM), as well as L. infantum and L. donovani promastigotes when used at a concentration of 50 µM.{52275,52274} Betulonic acid inhibits replication of herpes simplex virus I (HSV-I), echovirus 6, and the H7N1 strain of influenza A (EC50s = 0.9, 73.32, and 5.7 µM, respectively).{52276} It inhibits proliferation of MGC803, Bcap-37, MCF-7, PC3, and NIH3T3 cancer cells by 68.1, 44.9, 56.1, 52.4, and 22.1%, respectively, when used at a concentration of 20 µM.{52273}  

     

    Brand:
    Cayman
    SKU:29765 - 10 mg

    Available on backorder

  • Betulonic acid is a triterpenoid that has been found in B. chinensis and has diverse biological activities, including antiparasitic, antiviral, and anticancer properties.{52273,52274,52275,52276} It is active against the chloroquine-resistant P. falciparum W2 clone (IC50 = 10.01 µM), as well as L. infantum and L. donovani promastigotes when used at a concentration of 50 µM.{52275,52274} Betulonic acid inhibits replication of herpes simplex virus I (HSV-I), echovirus 6, and the H7N1 strain of influenza A (EC50s = 0.9, 73.32, and 5.7 µM, respectively).{52276} It inhibits proliferation of MGC803, Bcap-37, MCF-7, PC3, and NIH3T3 cancer cells by 68.1, 44.9, 56.1, 52.4, and 22.1%, respectively, when used at a concentration of 20 µM.{52273}  

     

    Brand:
    Cayman
    SKU:29765 - 25 mg

    Available on backorder

  • Betulonic acid is a triterpenoid that has been found in B. chinensis and has diverse biological activities, including antiparasitic, antiviral, and anticancer properties.{52273,52274,52275,52276} It is active against the chloroquine-resistant P. falciparum W2 clone (IC50 = 10.01 µM), as well as L. infantum and L. donovani promastigotes when used at a concentration of 50 µM.{52275,52274} Betulonic acid inhibits replication of herpes simplex virus I (HSV-I), echovirus 6, and the H7N1 strain of influenza A (EC50s = 0.9, 73.32, and 5.7 µM, respectively).{52276} It inhibits proliferation of MGC803, Bcap-37, MCF-7, PC3, and NIH3T3 cancer cells by 68.1, 44.9, 56.1, 52.4, and 22.1%, respectively, when used at a concentration of 20 µM.{52273}  

     

    Brand:
    Cayman
    SKU:29765 - 5 mg

    Available on backorder

  • Betulonic acid is a triterpenoid that has been found in B. chinensis and has diverse biological activities, including antiparasitic, antiviral, and anticancer properties.{52273,52274,52275,52276} It is active against the chloroquine-resistant P. falciparum W2 clone (IC50 = 10.01 µM), as well as L. infantum and L. donovani promastigotes when used at a concentration of 50 µM.{52275,52274} Betulonic acid inhibits replication of herpes simplex virus I (HSV-I), echovirus 6, and the H7N1 strain of influenza A (EC50s = 0.9, 73.32, and 5.7 µM, respectively).{52276} It inhibits proliferation of MGC803, Bcap-37, MCF-7, PC3, and NIH3T3 cancer cells by 68.1, 44.9, 56.1, 52.4, and 22.1%, respectively, when used at a concentration of 20 µM.{52273}  

     

    Brand:
    Cayman
    SKU:29765 - 50 mg

    Available on backorder

  • Bevantolol is an antagonist of the β1-adrenergic receptor (β1-AR; Ki = 14.79 nM in rat cortical membranes).{52361} It is selective for β1- over β2-ARs (Ki = 588.84 nM), as well as α2-ARs up to 100 μM, but is an antagonist of α1-ARs (Ki = 125.89 nM). Bevantolol inhibits low voltage-activated calcium currents (LVA-ICa) in dissociated rat ventro-medial hypothalamic neurons (IC50 = 40 μM).{52362} It inhibits norepinephrine-induced contraction of isolated rabbit thoracic aorta (pA2 = 4.77), isoprenaline-induced inotropic effects in isolated guinea pig right atria (pA2 = 7.74), and isoprenaline-induced relaxation of isolated guinea pig trachea (pA2 = 6.69).{52363} Bevantolol (250 mg/kg per day) prevents immobilization stress-induced increases in systolic blood pressure in a rat model of stress-induced hypertension.{52364}  

     

    Brand:
    Cayman
    SKU:29792 - 100 mg

    Available on backorder

  • Bevantolol is an antagonist of the β1-adrenergic receptor (β1-AR; Ki = 14.79 nM in rat cortical membranes).{52361} It is selective for β1- over β2-ARs (Ki = 588.84 nM), as well as α2-ARs up to 100 μM, but is an antagonist of α1-ARs (Ki = 125.89 nM). Bevantolol inhibits low voltage-activated calcium currents (LVA-ICa) in dissociated rat ventro-medial hypothalamic neurons (IC50 = 40 μM).{52362} It inhibits norepinephrine-induced contraction of isolated rabbit thoracic aorta (pA2 = 4.77), isoprenaline-induced inotropic effects in isolated guinea pig right atria (pA2 = 7.74), and isoprenaline-induced relaxation of isolated guinea pig trachea (pA2 = 6.69).{52363} Bevantolol (250 mg/kg per day) prevents immobilization stress-induced increases in systolic blood pressure in a rat model of stress-induced hypertension.{52364}  

     

    Brand:
    Cayman
    SKU:29792 - 250 mg

    Available on backorder

  • Bevantolol is an antagonist of the β1-adrenergic receptor (β1-AR; Ki = 14.79 nM in rat cortical membranes).{52361} It is selective for β1- over β2-ARs (Ki = 588.84 nM), as well as α2-ARs up to 100 μM, but is an antagonist of α1-ARs (Ki = 125.89 nM). Bevantolol inhibits low voltage-activated calcium currents (LVA-ICa) in dissociated rat ventro-medial hypothalamic neurons (IC50 = 40 μM).{52362} It inhibits norepinephrine-induced contraction of isolated rabbit thoracic aorta (pA2 = 4.77), isoprenaline-induced inotropic effects in isolated guinea pig right atria (pA2 = 7.74), and isoprenaline-induced relaxation of isolated guinea pig trachea (pA2 = 6.69).{52363} Bevantolol (250 mg/kg per day) prevents immobilization stress-induced increases in systolic blood pressure in a rat model of stress-induced hypertension.{52364}  

     

    Brand:
    Cayman
    SKU:29792 - 500 mg

    Available on backorder

  • Bexarotene is an agonist of retinoid X receptors (RXRs; EC50s = 28, 25, and 20 nM for RXRα, RXRβ, and RXRγ, respectively, in reporter assays).{20758} It is selective for RXRs over retinoic acid receptors (RARs; EC50s = >10 µM for RARα, RARβ, and RARγ). Bexarotene (10 µM) induces apoptosis in MJ, HuT 78, and HH cutaneous T cell lymphoma (CTCL) cells, as well as inhibits lung metastasis and angiogenesis in A549 and MDA-MB-231 mouse xenograft models when administered at a dose of 100 mg/kg per day.{58126,58127} It reduces increased brain interstitial fluid levels of amyloid-β (1-40) (Aβ40) and Aβ42 in the APP/PS1 transgenic mouse model of Alzheimer’s disease.{20759} It also reduces viral load in the culture supernatant of Vero E6 cells infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2; EC90 = 9.4 µM) and inhibits SARS-CoV-2 replication in a plaque reduction assay (EC50 = 2.01 µM).{59330} Formulations containing bexarotene have been used in the treatment of CTCL.  

     

    Brand:
    Cayman
    SKU:11571 - 10 mg

    Available on backorder

  • Bexarotene is an agonist of retinoid X receptors (RXRs; EC50s = 28, 25, and 20 nM for RXRα, RXRβ, and RXRγ, respectively, in reporter assays).{20758} It is selective for RXRs over retinoic acid receptors (RARs; EC50s = >10 µM for RARα, RARβ, and RARγ). Bexarotene (10 µM) induces apoptosis in MJ, HuT 78, and HH cutaneous T cell lymphoma (CTCL) cells, as well as inhibits lung metastasis and angiogenesis in A549 and MDA-MB-231 mouse xenograft models when administered at a dose of 100 mg/kg per day.{58126,58127} It reduces increased brain interstitial fluid levels of amyloid-β (1-40) (Aβ40) and Aβ42 in the APP/PS1 transgenic mouse model of Alzheimer’s disease.{20759} It also reduces viral load in the culture supernatant of Vero E6 cells infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2; EC90 = 9.4 µM) and inhibits SARS-CoV-2 replication in a plaque reduction assay (EC50 = 2.01 µM).{59330} Formulations containing bexarotene have been used in the treatment of CTCL.  

     

    Brand:
    Cayman
    SKU:11571 - 5 mg

    Available on backorder

  • Bexarotene is an agonist of retinoid X receptors (RXRs; EC50s = 28, 25, and 20 nM for RXRα, RXRβ, and RXRγ, respectively, in reporter assays).{20758} It is selective for RXRs over retinoic acid receptors (RARs; EC50s = >10 µM for RARα, RARβ, and RARγ). Bexarotene (10 µM) induces apoptosis in MJ, HuT 78, and HH cutaneous T cell lymphoma (CTCL) cells, as well as inhibits lung metastasis and angiogenesis in A549 and MDA-MB-231 mouse xenograft models when administered at a dose of 100 mg/kg per day.{58126,58127} It reduces increased brain interstitial fluid levels of amyloid-β (1-40) (Aβ40) and Aβ42 in the APP/PS1 transgenic mouse model of Alzheimer’s disease.{20759} It also reduces viral load in the culture supernatant of Vero E6 cells infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2; EC90 = 9.4 µM) and inhibits SARS-CoV-2 replication in a plaque reduction assay (EC50 = 2.01 µM).{59330} Formulations containing bexarotene have been used in the treatment of CTCL.  

     

    Brand:
    Cayman
    SKU:11571 - 50 mg

    Available on backorder

  • Bezafibrate is a non-selective agonist of peroxisome proliferator-activated receptors (PPARs; EC50s = 50, 60, and 20 μM for human PPARα, PPARγ, and PPARδ, respectively).{10670} It reduces triglyceride levels and the size of lipid droplets in an oleic acid-induced HepaRG hepatocyte model of steatosis when used at a concentration of 25 μM.{42456} Bezafibrate (10 mg/kg per day) reduces plasma VLDL and LDL mass and triglyceride and free fatty acid levels in a high-fructose plus lard diet-induced rat model of insulin resistance.{42937}  

     

    Brand:
    Cayman
    SKU:10009145 - 1 g

    Available on backorder

  • Bezafibrate is a non-selective agonist of peroxisome proliferator-activated receptors (PPARs; EC50s = 50, 60, and 20 μM for human PPARα, PPARγ, and PPARδ, respectively).{10670} It reduces triglyceride levels and the size of lipid droplets in an oleic acid-induced HepaRG hepatocyte model of steatosis when used at a concentration of 25 μM.{42456} Bezafibrate (10 mg/kg per day) reduces plasma VLDL and LDL mass and triglyceride and free fatty acid levels in a high-fructose plus lard diet-induced rat model of insulin resistance.{42937}  

     

    Brand:
    Cayman
    SKU:10009145 - 10 g

    Available on backorder

  • Bezafibrate is a non-selective agonist of peroxisome proliferator-activated receptors (PPARs; EC50s = 50, 60, and 20 μM for human PPARα, PPARγ, and PPARδ, respectively).{10670} It reduces triglyceride levels and the size of lipid droplets in an oleic acid-induced HepaRG hepatocyte model of steatosis when used at a concentration of 25 μM.{42456} Bezafibrate (10 mg/kg per day) reduces plasma VLDL and LDL mass and triglyceride and free fatty acid levels in a high-fructose plus lard diet-induced rat model of insulin resistance.{42937}  

     

    Brand:
    Cayman
    SKU:10009145 - 5 g

    Available on backorder

  • Bezafibrate is a non-selective agonist of peroxisome proliferator-activated receptors (PPARs; EC50s = 50, 60, and 20 μM for human PPARα, PPARγ, and PPARδ, respectively).{10670} It reduces triglyceride levels and the size of lipid droplets in an oleic acid-induced HepaRG hepatocyte model of steatosis when used at a concentration of 25 μM.{42456} Bezafibrate (10 mg/kg per day) reduces plasma VLDL and LDL mass and triglyceride and free fatty acid levels in a high-fructose plus lard diet-induced rat model of insulin resistance.{42937}  

     

    Brand:
    Cayman
    SKU:10009145 - 500 mg

    Available on backorder

  • Bezafibrate-d4 is intended for use as an internal standard for the quantification of bezafibrate (Item No. 10009145) by GC- or LC-MS. Bezafibrate is a non-selective agonist of peroxisome proliferator-activated receptors (PPARs; EC50s = 50, 60, and 20 μM for human PPARα, PPARγ, and PPARδ, respectively).{10670} It reduces triglyceride levels and the size of lipid droplets in an oleic acid-induced HepaRG hepatocyte model of steatosis when used at a concentration of 25 μM.{42456} Bezafibrate (10 mg/kg per day) reduces plasma VLDL and LDL mass and triglyceride and free fatty acid levels in a high-fructose plus lard diet-induced rat model of insulin resistance.{42937}  

     

    Brand:
    Cayman
    SKU:28526 - 1 mg

    Available on backorder

  • BFH772 is an inhibitor of VEGF receptor 2 (VEGFR2; IC50 = 0.0027 μM for the human receptor).{42999} It is selective for human VEGFR2 over mouse VEGFR2 and human VEGFR1 and VEGFR3 (IC50s = 1.5, 1.7, and 1.1 μM, respectively), as well as 40-fold selective over B-RAF, RET, and Tie2. BFH772 inhibits VEGF-induced proliferation of human umbilical vein endothelial cells (HUVECs; IC50 = <0.01 nM). It inhibits VEGF-induced increases in tissue weight and Tie2 levels in an angiogenesis chamber implant model in mice when administered at doses of 1 and 3 mg/kg per day. BFH772 (3 mg/kg per day) inhibits primary tumor and metastasis growth in a B16 melanoma mouse model.  

     

    Brand:
    Cayman
    SKU:21386 -

    Out of stock

  • BFH772 is an inhibitor of VEGF receptor 2 (VEGFR2; IC50 = 0.0027 μM for the human receptor).{42999} It is selective for human VEGFR2 over mouse VEGFR2 and human VEGFR1 and VEGFR3 (IC50s = 1.5, 1.7, and 1.1 μM, respectively), as well as 40-fold selective over B-RAF, RET, and Tie2. BFH772 inhibits VEGF-induced proliferation of human umbilical vein endothelial cells (HUVECs; IC50 = <0.01 nM). It inhibits VEGF-induced increases in tissue weight and Tie2 levels in an angiogenesis chamber implant model in mice when administered at doses of 1 and 3 mg/kg per day. BFH772 (3 mg/kg per day) inhibits primary tumor and metastasis growth in a B16 melanoma mouse model.  

     

    Brand:
    Cayman
    SKU:21386 -

    Out of stock

  • BFH772 is an inhibitor of VEGF receptor 2 (VEGFR2; IC50 = 0.0027 μM for the human receptor).{42999} It is selective for human VEGFR2 over mouse VEGFR2 and human VEGFR1 and VEGFR3 (IC50s = 1.5, 1.7, and 1.1 μM, respectively), as well as 40-fold selective over B-RAF, RET, and Tie2. BFH772 inhibits VEGF-induced proliferation of human umbilical vein endothelial cells (HUVECs; IC50 = <0.01 nM). It inhibits VEGF-induced increases in tissue weight and Tie2 levels in an angiogenesis chamber implant model in mice when administered at doses of 1 and 3 mg/kg per day. BFH772 (3 mg/kg per day) inhibits primary tumor and metastasis growth in a B16 melanoma mouse model.  

     

    Brand:
    Cayman
    SKU:21386 -

    Out of stock

  • BFH772 is an inhibitor of VEGF receptor 2 (VEGFR2; IC50 = 0.0027 μM for the human receptor).{42999} It is selective for human VEGFR2 over mouse VEGFR2 and human VEGFR1 and VEGFR3 (IC50s = 1.5, 1.7, and 1.1 μM, respectively), as well as 40-fold selective over B-RAF, RET, and Tie2. BFH772 inhibits VEGF-induced proliferation of human umbilical vein endothelial cells (HUVECs; IC50 = <0.01 nM). It inhibits VEGF-induced increases in tissue weight and Tie2 levels in an angiogenesis chamber implant model in mice when administered at doses of 1 and 3 mg/kg per day. BFH772 (3 mg/kg per day) inhibits primary tumor and metastasis growth in a B16 melanoma mouse model.  

     

    Brand:
    Cayman
    SKU:21386 -

    Out of stock

  • BG45 is an HDAC class I inhibitor with selectivity for HDAC3 (IC50 = 289 nM). It inhibits HDAC1, HDAC2, and HDAC6 with greatly reduced potency (IC50s = 2, 2.2, and >20 µM, respectively).{27757} At concentrations up to 50 mg/kg, BG45 alone or in combination with bortezomib has been shown to dose-dependently inhibit tumor growth in a mouse model of multiple myeloma.{27757}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • BG45 is an HDAC class I inhibitor with selectivity for HDAC3 (IC50 = 289 nM). It inhibits HDAC1, HDAC2, and HDAC6 with greatly reduced potency (IC50s = 2, 2.2, and >20 µM, respectively).{27757} At concentrations up to 50 mg/kg, BG45 alone or in combination with bortezomib has been shown to dose-dependently inhibit tumor growth in a mouse model of multiple myeloma.{27757}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • BG45 is an HDAC class I inhibitor with selectivity for HDAC3 (IC50 = 289 nM). It inhibits HDAC1, HDAC2, and HDAC6 with greatly reduced potency (IC50s = 2, 2.2, and >20 µM, respectively).{27757} At concentrations up to 50 mg/kg, BG45 alone or in combination with bortezomib has been shown to dose-dependently inhibit tumor growth in a mouse model of multiple myeloma.{27757}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • BG45 is an HDAC class I inhibitor with selectivity for HDAC3 (IC50 = 289 nM). It inhibits HDAC1, HDAC2, and HDAC6 with greatly reduced potency (IC50s = 2, 2.2, and >20 µM, respectively).{27757} At concentrations up to 50 mg/kg, BG45 alone or in combination with bortezomib has been shown to dose-dependently inhibit tumor growth in a mouse model of multiple myeloma.{27757}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • BGC 20-1531 is a potent and selective antagonist of the prostaglandin E2 (PGE2; Item No. 14010) receptor subtype 4 (EP4) with Ki values of 11.7, >10,000, and >10,000 nM for EP4, EP2, and EP3, respectively.{17141} It is selective for EP4, exhibiting 2-induced cAMP accumulation in a dose-dependent manner in HEK293 EBNA cells that stably express human EP4 receptors. It also reverses PGE2-induced vasorelaxation (Kb = 15.85 nM) in human middle cerebral and middle meningeal arterial rings. BGC 20-1531 prevents PGE2-induced increases in carotid blood flow and decreases in carotid resistance with an ID50 value of 5 mg/kg in dogs.  

     

    Brand:
    Cayman
    SKU:19742 -

    Available on backorder

  • BGC 20-1531 is a potent and selective antagonist of the prostaglandin E2 (PGE2; Item No. 14010) receptor subtype 4 (EP4) with Ki values of 11.7, >10,000, and >10,000 nM for EP4, EP2, and EP3, respectively.{17141} It is selective for EP4, exhibiting 2-induced cAMP accumulation in a dose-dependent manner in HEK293 EBNA cells that stably express human EP4 receptors. It also reverses PGE2-induced vasorelaxation (Kb = 15.85 nM) in human middle cerebral and middle meningeal arterial rings. BGC 20-1531 prevents PGE2-induced increases in carotid blood flow and decreases in carotid resistance with an ID50 value of 5 mg/kg in dogs.  

     

    Brand:
    Cayman
    SKU:19742 -

    Available on backorder

  • BGC 20-1531 is a potent and selective antagonist of the prostaglandin E2 (PGE2; Item No. 14010) receptor subtype 4 (EP4) with Ki values of 11.7, >10,000, and >10,000 nM for EP4, EP2, and EP3, respectively.{17141} It is selective for EP4, exhibiting 2-induced cAMP accumulation in a dose-dependent manner in HEK293 EBNA cells that stably express human EP4 receptors. It also reverses PGE2-induced vasorelaxation (Kb = 15.85 nM) in human middle cerebral and middle meningeal arterial rings. BGC 20-1531 prevents PGE2-induced increases in carotid blood flow and decreases in carotid resistance with an ID50 value of 5 mg/kg in dogs.  

     

    Brand:
    Cayman
    SKU:19742 -

    Available on backorder

  • BGC 20-1531 is a potent and selective antagonist of the prostaglandin E2 (PGE2; Item No. 14010) receptor subtype 4 (EP4) with Ki values of 11.7, >10,000, and >10,000 nM for EP4, EP2, and EP3, respectively.{17141} It is selective for EP4, exhibiting 2-induced cAMP accumulation in a dose-dependent manner in HEK293 EBNA cells that stably express human EP4 receptors. It also reverses PGE2-induced vasorelaxation (Kb = 15.85 nM) in human middle cerebral and middle meningeal arterial rings. BGC 20-1531 prevents PGE2-induced increases in carotid blood flow and decreases in carotid resistance with an ID50 value of 5 mg/kg in dogs.  

     

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    Cayman
    SKU:19742 -

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  • BGJ398 is an orally available inhibitor of human FGFRs (IC50s = 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively).{31102,30600} It inhibits FGFR4 and VEGFR2 with IC50 values of 60 and 180 nM, respectively, and displays comparatively little activity towards Abl, Fyn, Kit, Lck, Lyn, and Yes (IC50s = 0.3-2.5 µM).{31102} BGJ398 has been shown to suppress proliferation of cancer cells with wild-type FGFR3 overexpression (IC50s = 5, 30, 32, and 15 nM, for RT112, RT4, SW780, and JMSU1 cells, respectively).{31102} In an RT112 bladder cancer xenograft mouse model overexpressing wild-type FGFR3, BGJ398 inhibited tumor growth after oral administration of 10-30 mg/kg.{31102}  

     

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    Cayman
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  • BGJ398 is an orally available inhibitor of human FGFRs (IC50s = 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively).{31102,30600} It inhibits FGFR4 and VEGFR2 with IC50 values of 60 and 180 nM, respectively, and displays comparatively little activity towards Abl, Fyn, Kit, Lck, Lyn, and Yes (IC50s = 0.3-2.5 µM).{31102} BGJ398 has been shown to suppress proliferation of cancer cells with wild-type FGFR3 overexpression (IC50s = 5, 30, 32, and 15 nM, for RT112, RT4, SW780, and JMSU1 cells, respectively).{31102} In an RT112 bladder cancer xenograft mouse model overexpressing wild-type FGFR3, BGJ398 inhibited tumor growth after oral administration of 10-30 mg/kg.{31102}  

     

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    Cayman
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  • BGJ398 is an orally available inhibitor of human FGFRs (IC50s = 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively).{31102,30600} It inhibits FGFR4 and VEGFR2 with IC50 values of 60 and 180 nM, respectively, and displays comparatively little activity towards Abl, Fyn, Kit, Lck, Lyn, and Yes (IC50s = 0.3-2.5 µM).{31102} BGJ398 has been shown to suppress proliferation of cancer cells with wild-type FGFR3 overexpression (IC50s = 5, 30, 32, and 15 nM, for RT112, RT4, SW780, and JMSU1 cells, respectively).{31102} In an RT112 bladder cancer xenograft mouse model overexpressing wild-type FGFR3, BGJ398 inhibited tumor growth after oral administration of 10-30 mg/kg.{31102}  

     

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    Cayman
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  • BGJ398 is an orally available inhibitor of human FGFRs (IC50s = 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively).{31102,30600} It inhibits FGFR4 and VEGFR2 with IC50 values of 60 and 180 nM, respectively, and displays comparatively little activity towards Abl, Fyn, Kit, Lck, Lyn, and Yes (IC50s = 0.3-2.5 µM).{31102} BGJ398 has been shown to suppress proliferation of cancer cells with wild-type FGFR3 overexpression (IC50s = 5, 30, 32, and 15 nM, for RT112, RT4, SW780, and JMSU1 cells, respectively).{31102} In an RT112 bladder cancer xenograft mouse model overexpressing wild-type FGFR3, BGJ398 inhibited tumor growth after oral administration of 10-30 mg/kg.{31102}  

     

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    Cayman
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  • The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis.{22577} BGP-15 is a PARP inhibitor and insulin sensitizer. In perfused heart, it blocks self-ADP-ribosylation of nuclear PARP (Ki = 57 µM) and mono-ADP-ribosylation of GRP78, resulting in decreased levels of reactive oxygen species, lipid peroxidation, and single-strand DNA breaks.{29058,29060} BGP-15 acts as a co-inducer of heat shock protein 72, augmenting expression induced by heat shock factor 1 in adipocytes and skeletal muscles and improving insulin sensitivity.{29057,29059}  

     

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    Cayman
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  • The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis.{22577} BGP-15 is a PARP inhibitor and insulin sensitizer. In perfused heart, it blocks self-ADP-ribosylation of nuclear PARP (Ki = 57 µM) and mono-ADP-ribosylation of GRP78, resulting in decreased levels of reactive oxygen species, lipid peroxidation, and single-strand DNA breaks.{29058,29060} BGP-15 acts as a co-inducer of heat shock protein 72, augmenting expression induced by heat shock factor 1 in adipocytes and skeletal muscles and improving insulin sensitivity.{29057,29059}  

     

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    Cayman
    SKU:-

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  • The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis.{22577} BGP-15 is a PARP inhibitor and insulin sensitizer. In perfused heart, it blocks self-ADP-ribosylation of nuclear PARP (Ki = 57 µM) and mono-ADP-ribosylation of GRP78, resulting in decreased levels of reactive oxygen species, lipid peroxidation, and single-strand DNA breaks.{29058,29060} BGP-15 acts as a co-inducer of heat shock protein 72, augmenting expression induced by heat shock factor 1 in adipocytes and skeletal muscles and improving insulin sensitivity.{29057,29059}  

     

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    Cayman
    SKU:-

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  • The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis.{22577} BGP-15 is a PARP inhibitor and insulin sensitizer. In perfused heart, it blocks self-ADP-ribosylation of nuclear PARP (Ki = 57 µM) and mono-ADP-ribosylation of GRP78, resulting in decreased levels of reactive oxygen species, lipid peroxidation, and single-strand DNA breaks.{29058,29060} BGP-15 acts as a co-inducer of heat shock protein 72, augmenting expression induced by heat shock factor 1 in adipocytes and skeletal muscles and improving insulin sensitivity.{29057,29059}  

     

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    Cayman
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  • The family of Bcl-2 proteins plays pivotal roles in either promoting or preventing apoptosis. Bcl-2 family members contain one or more of four characteristic Bcl-2 homology (BH) domains, which are crucial for function. For example, anti-apoptotic Bcl-2 family proteins prevent death signaling by heterodimerizing with pro-death proteins at their BH3 domains.{24784} BH3I-1 is a cell permeable inhibitor that blocks the binding of BH3 peptides to Bcl-xL, inducing apoptosis.{30354} It inhibits interactions of BH3 domain-containing proteins with Bcl-xL, Bcl-2, and Bcl-W, inducing apoptosis in Bcl-2 or Bcl-W expressing cells with Ki values of 43.4 and 124 µM, respectively.{30356,30355} BH3I-1 enhances radiation sensitivity in non-small cell lung cancer cells.{30356}  

     

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  • The family of Bcl-2 proteins plays pivotal roles in either promoting or preventing apoptosis. Bcl-2 family members contain one or more of four characteristic Bcl-2 homology (BH) domains, which are crucial for function. For example, anti-apoptotic Bcl-2 family proteins prevent death signaling by heterodimerizing with pro-death proteins at their BH3 domains.{24784} BH3I-1 is a cell permeable inhibitor that blocks the binding of BH3 peptides to Bcl-xL, inducing apoptosis.{30354} It inhibits interactions of BH3 domain-containing proteins with Bcl-xL, Bcl-2, and Bcl-W, inducing apoptosis in Bcl-2 or Bcl-W expressing cells with Ki values of 43.4 and 124 µM, respectively.{30356,30355} BH3I-1 enhances radiation sensitivity in non-small cell lung cancer cells.{30356}  

     

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    Cayman
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  • The family of Bcl-2 proteins plays pivotal roles in either promoting or preventing apoptosis. Bcl-2 family members contain one or more of four characteristic Bcl-2 homology (BH) domains, which are crucial for function. For example, anti-apoptotic Bcl-2 family proteins prevent death signaling by heterodimerizing with pro-death proteins at their BH3 domains.{24784} BH3I-1 is a cell permeable inhibitor that blocks the binding of BH3 peptides to Bcl-xL, inducing apoptosis.{30354} It inhibits interactions of BH3 domain-containing proteins with Bcl-xL, Bcl-2, and Bcl-W, inducing apoptosis in Bcl-2 or Bcl-W expressing cells with Ki values of 43.4 and 124 µM, respectively.{30356,30355} BH3I-1 enhances radiation sensitivity in non-small cell lung cancer cells.{30356}  

     

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  • The family of Bcl-2 proteins plays pivotal roles in either promoting or preventing apoptosis. Bcl-2 family members contain one or more of four characteristic Bcl-2 homology (BH) domains, which are crucial for function. For example, anti-apoptotic Bcl-2 family proteins prevent death signaling by heterodimerizing with pro-death proteins at their BH3 domains.{24784} BH3I-1 is a cell permeable inhibitor that blocks the binding of BH3 peptides to Bcl-xL, inducing apoptosis.{30354} It inhibits interactions of BH3 domain-containing proteins with Bcl-xL, Bcl-2, and Bcl-W, inducing apoptosis in Bcl-2 or Bcl-W expressing cells with Ki values of 43.4 and 124 µM, respectively.{30356,30355} BH3I-1 enhances radiation sensitivity in non-small cell lung cancer cells.{30356}  

     

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  • BHBM is an acylhydrazone with antifungal activity.{50810,53336} It is active against C. neoformans in vitro (MIC80 = 1 µg/ml).{53336} BHBM (0.25, 1, and 4 µg/ml) inhibits the synthesis of glucosylceramide, which is essential to fungal cell division, in C. neoformans but not J774 murine macrophages.{50810} In vivo, BHBM (1.2 mg/kg per day) increases survival in a mouse model of C. neoformans infection.  

     

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    Cayman
    SKU:29817 - 1 mg

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  • BHBM is an acylhydrazone with antifungal activity.{50810,53336} It is active against C. neoformans in vitro (MIC80 = 1 µg/ml).{53336} BHBM (0.25, 1, and 4 µg/ml) inhibits the synthesis of glucosylceramide, which is essential to fungal cell division, in C. neoformans but not J774 murine macrophages.{50810} In vivo, BHBM (1.2 mg/kg per day) increases survival in a mouse model of C. neoformans infection.  

     

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    Cayman
    SKU:29817 - 10 mg

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  • BHBM is an acylhydrazone with antifungal activity.{50810,53336} It is active against C. neoformans in vitro (MIC80 = 1 µg/ml).{53336} BHBM (0.25, 1, and 4 µg/ml) inhibits the synthesis of glucosylceramide, which is essential to fungal cell division, in C. neoformans but not J774 murine macrophages.{50810} In vivo, BHBM (1.2 mg/kg per day) increases survival in a mouse model of C. neoformans infection.  

     

    Brand:
    Cayman
    SKU:29817 - 25 mg

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  • BHBM is an acylhydrazone with antifungal activity.{50810,53336} It is active against C. neoformans in vitro (MIC80 = 1 µg/ml).{53336} BHBM (0.25, 1, and 4 µg/ml) inhibits the synthesis of glucosylceramide, which is essential to fungal cell division, in C. neoformans but not J774 murine macrophages.{50810} In vivo, BHBM (1.2 mg/kg per day) increases survival in a mouse model of C. neoformans infection.  

     

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    Cayman
    SKU:29817 - 5 mg

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  • BHPI is an antagonist of estrogen receptor α (ERα) that blocks 17β-estradiol-induced proliferation of drug-resistant breast, endometrial, and ovarian cancer cell lines at concentrations ranging from 10 to 1,000 nM.{28679} It is effective in vivo, driving tumor regression in mice bearing MCF-7 xenografts at a dose of 15 mg/kg daily.{28679} BHPI specifically inhibits ERα-dependent gene expression and protein synthesis by activating the unfolded protein response in cells.{28679}  

     

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    Cayman
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  • BHPI is an antagonist of estrogen receptor α (ERα) that blocks 17β-estradiol-induced proliferation of drug-resistant breast, endometrial, and ovarian cancer cell lines at concentrations ranging from 10 to 1,000 nM.{28679} It is effective in vivo, driving tumor regression in mice bearing MCF-7 xenografts at a dose of 15 mg/kg daily.{28679} BHPI specifically inhibits ERα-dependent gene expression and protein synthesis by activating the unfolded protein response in cells.{28679}  

     

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    Cayman
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  • BHPI is an antagonist of estrogen receptor α (ERα) that blocks 17β-estradiol-induced proliferation of drug-resistant breast, endometrial, and ovarian cancer cell lines at concentrations ranging from 10 to 1,000 nM.{28679} It is effective in vivo, driving tumor regression in mice bearing MCF-7 xenografts at a dose of 15 mg/kg daily.{28679} BHPI specifically inhibits ERα-dependent gene expression and protein synthesis by activating the unfolded protein response in cells.{28679}  

     

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    Cayman
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  • BHT is a synthetic antioxidant.{56221,56222} It scavenges peroxide, 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805), superoxide, and ABTS (Item No. 27317) radicals in cell-free assays, as well as inhibits lipid peroxidation of linoleic acid (Item Nos. 90150 | 90150.1 | 21909) in vitro when used at a concentration of 45 µg/ml.{56221} BHT (0.025-3.2 mM) reduces freeze-thaw-induced malondialdehyde (MDA) production and increases sperm viability in boar spermatozoa preparations.{56222} Formulations containing BHT have been used as antioxidant cosmetic and food additives.  

     

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    Cayman
    SKU:89910 - 1 g

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  • BHT is a synthetic antioxidant.{56221,56222} It scavenges peroxide, 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805), superoxide, and ABTS (Item No. 27317) radicals in cell-free assays, as well as inhibits lipid peroxidation of linoleic acid (Item Nos. 90150 | 90150.1 | 21909) in vitro when used at a concentration of 45 µg/ml.{56221} BHT (0.025-3.2 mM) reduces freeze-thaw-induced malondialdehyde (MDA) production and increases sperm viability in boar spermatozoa preparations.{56222} Formulations containing BHT have been used as antioxidant cosmetic and food additives.  

     

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    Cayman
    SKU:89910 - 500 mg

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  • Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} BI-2536 is a 2-aminopyrimidine-containing inhibitor of Plk1 (IC50 = 0.83 nM).{29246,24210} It displays 4- and 11-fold selectivity for Plk1 over Plk2 and Plk3, respectively. BI-2536 induces mitotic arrest and apoptosis in diverse human cancer cell lines and drives regression of human tumor xenografts in nude mice.{29246} It shows good blood-brain barrier permeability and causes mitotic arrest in glioblastoma-derived neural stem cells but not normal neural stem cells.{29225} BI-2536 is also an inhibitor of BRD4 (IC50 = 25 nM), suppressing BRD4-dependent c-Myc expression in MM.1S multiple myeloma cells.{29245}  

     

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    Cayman
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  • Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} BI-2536 is a 2-aminopyrimidine-containing inhibitor of Plk1 (IC50 = 0.83 nM).{29246,24210} It displays 4- and 11-fold selectivity for Plk1 over Plk2 and Plk3, respectively. BI-2536 induces mitotic arrest and apoptosis in diverse human cancer cell lines and drives regression of human tumor xenografts in nude mice.{29246} It shows good blood-brain barrier permeability and causes mitotic arrest in glioblastoma-derived neural stem cells but not normal neural stem cells.{29225} BI-2536 is also an inhibitor of BRD4 (IC50 = 25 nM), suppressing BRD4-dependent c-Myc expression in MM.1S multiple myeloma cells.{29245}  

     

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    Cayman
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  • Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} BI-2536 is a 2-aminopyrimidine-containing inhibitor of Plk1 (IC50 = 0.83 nM).{29246,24210} It displays 4- and 11-fold selectivity for Plk1 over Plk2 and Plk3, respectively. BI-2536 induces mitotic arrest and apoptosis in diverse human cancer cell lines and drives regression of human tumor xenografts in nude mice.{29246} It shows good blood-brain barrier permeability and causes mitotic arrest in glioblastoma-derived neural stem cells but not normal neural stem cells.{29225} BI-2536 is also an inhibitor of BRD4 (IC50 = 25 nM), suppressing BRD4-dependent c-Myc expression in MM.1S multiple myeloma cells.{29245}  

     

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    Cayman
    SKU:-

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  • Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} BI-2536 is a 2-aminopyrimidine-containing inhibitor of Plk1 (IC50 = 0.83 nM).{29246,24210} It displays 4- and 11-fold selectivity for Plk1 over Plk2 and Plk3, respectively. BI-2536 induces mitotic arrest and apoptosis in diverse human cancer cell lines and drives regression of human tumor xenografts in nude mice.{29246} It shows good blood-brain barrier permeability and causes mitotic arrest in glioblastoma-derived neural stem cells but not normal neural stem cells.{29225} BI-2536 is also an inhibitor of BRD4 (IC50 = 25 nM), suppressing BRD4-dependent c-Myc expression in MM.1S multiple myeloma cells.{29245}  

     

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    Cayman
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  • BI-409306 is a potent and selective phosphodiesterase 9A (PDE9A) inhibitor with IC50 values of 65 and 168 nM for the human and rat enzymes, respectively.{52498} It is selective for PDE9A over PDE2A, -3A, -4B, -5A, -6AB, -7A and -10A and 95 non-PDE targets at 10 µM but does inhibit human PDE1A and PDE1C (IC50s = 1.45 and 1.17 µM, respectively). BI-409306 (0.5 mg/kg), in combination with MK-801, an NMDA receptor antagonist that reduces cGMP levels, increases cGMP levels by 41% in mouse striatal tissue compared with MK-801 alone. BI 406306 enhances long-term potentiation (LTP) in hippocampal slices and reverses MK-801-induced working memory deficits in a T-maze task in mice when administered at doses ranging from 0.007 to 2.5 mg/kg.  

     

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    Cayman
    SKU:30375 - 1 mg

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  • BI-409306 is a potent and selective phosphodiesterase 9A (PDE9A) inhibitor with IC50 values of 65 and 168 nM for the human and rat enzymes, respectively.{52498} It is selective for PDE9A over PDE2A, -3A, -4B, -5A, -6AB, -7A and -10A and 95 non-PDE targets at 10 µM but does inhibit human PDE1A and PDE1C (IC50s = 1.45 and 1.17 µM, respectively). BI-409306 (0.5 mg/kg), in combination with MK-801, an NMDA receptor antagonist that reduces cGMP levels, increases cGMP levels by 41% in mouse striatal tissue compared with MK-801 alone. BI 406306 enhances long-term potentiation (LTP) in hippocampal slices and reverses MK-801-induced working memory deficits in a T-maze task in mice when administered at doses ranging from 0.007 to 2.5 mg/kg.  

     

    Brand:
    Cayman
    SKU:30375 - 10 mg

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  • BI-409306 is a potent and selective phosphodiesterase 9A (PDE9A) inhibitor with IC50 values of 65 and 168 nM for the human and rat enzymes, respectively.{52498} It is selective for PDE9A over PDE2A, -3A, -4B, -5A, -6AB, -7A and -10A and 95 non-PDE targets at 10 µM but does inhibit human PDE1A and PDE1C (IC50s = 1.45 and 1.17 µM, respectively). BI-409306 (0.5 mg/kg), in combination with MK-801, an NMDA receptor antagonist that reduces cGMP levels, increases cGMP levels by 41% in mouse striatal tissue compared with MK-801 alone. BI 406306 enhances long-term potentiation (LTP) in hippocampal slices and reverses MK-801-induced working memory deficits in a T-maze task in mice when administered at doses ranging from 0.007 to 2.5 mg/kg.  

     

    Brand:
    Cayman
    SKU:30375 - 25 mg

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  • BI-409306 is a potent and selective phosphodiesterase 9A (PDE9A) inhibitor with IC50 values of 65 and 168 nM for the human and rat enzymes, respectively.{52498} It is selective for PDE9A over PDE2A, -3A, -4B, -5A, -6AB, -7A and -10A and 95 non-PDE targets at 10 µM but does inhibit human PDE1A and PDE1C (IC50s = 1.45 and 1.17 µM, respectively). BI-409306 (0.5 mg/kg), in combination with MK-801, an NMDA receptor antagonist that reduces cGMP levels, increases cGMP levels by 41% in mouse striatal tissue compared with MK-801 alone. BI 406306 enhances long-term potentiation (LTP) in hippocampal slices and reverses MK-801-induced working memory deficits in a T-maze task in mice when administered at doses ranging from 0.007 to 2.5 mg/kg.  

     

    Brand:
    Cayman
    SKU:30375 - 5 mg

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  • Hepatocyte nuclear factor 4α (HNF4α) is a nuclear receptor transcription factor that controls the expression of many genes including those involved in glucose and lipid homeostasis and maintenance of epithelial differentiation. BI-6015 is a small molecule antagonist of HNF4α that has been shown to repress the expression of known HNF4α target genes.{21357} At concentrations up to 20 μM, BI-6015 has been shown to reduce endogenous insulin gene expression by as much as 50-fold in T6PNE cells.{21357} The hepatocytes from livers of mice injected with 10 and 30 mg/kg BI-6015 exhibit marked, dose-dependent fat accumulation (steatosis).{21357} Additionally, at a daily dose of 30 mg/kg, BI-6015 induces apoptosis in a human hepatocellular carcinoma mouse model.{21357}  

     

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    Cayman
    SKU:12032 - 10 mg

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  • Hepatocyte nuclear factor 4α (HNF4α) is a nuclear receptor transcription factor that controls the expression of many genes including those involved in glucose and lipid homeostasis and maintenance of epithelial differentiation. BI-6015 is a small molecule antagonist of HNF4α that has been shown to repress the expression of known HNF4α target genes.{21357} At concentrations up to 20 μM, BI-6015 has been shown to reduce endogenous insulin gene expression by as much as 50-fold in T6PNE cells.{21357} The hepatocytes from livers of mice injected with 10 and 30 mg/kg BI-6015 exhibit marked, dose-dependent fat accumulation (steatosis).{21357} Additionally, at a daily dose of 30 mg/kg, BI-6015 induces apoptosis in a human hepatocellular carcinoma mouse model.{21357}  

     

    Brand:
    Cayman
    SKU:12032 - 5 mg

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  • Hepatocyte nuclear factor 4α (HNF4α) is a nuclear receptor transcription factor that controls the expression of many genes including those involved in glucose and lipid homeostasis and maintenance of epithelial differentiation. BI-6015 is a small molecule antagonist of HNF4α that has been shown to repress the expression of known HNF4α target genes.{21357} At concentrations up to 20 μM, BI-6015 has been shown to reduce endogenous insulin gene expression by as much as 50-fold in T6PNE cells.{21357} The hepatocytes from livers of mice injected with 10 and 30 mg/kg BI-6015 exhibit marked, dose-dependent fat accumulation (steatosis).{21357} Additionally, at a daily dose of 30 mg/kg, BI-6015 induces apoptosis in a human hepatocellular carcinoma mouse model.{21357}  

     

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    Cayman
    SKU:12032 - 50 mg

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  • BI-605906 is an inhibitor of inhibitor of kappa B kinase subunit β (IKKβ; IC50 = 380 nM).{32502} It is selective for IKKβ over insulin-like growth factor 1 (IGF1; IC50 = 7.6 μM) and over 100 kinases in a panel up to 10 μM. BI-605906 partially inhibits IL-1-stimulated activation of IKKε/TBK1 in vitro. BI-605906 also inhibits TNF-α-dependent IkB degradation and expression of the proinflammatory cytokines IL-6, IL-1β, and C-X-C motif ligand 1/2 (CXCL1/2) without affecting lipogenic gene expression or glucose production in murine primary hepatocytes.{40150}  

     

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    Cayman
    SKU:-

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  • BI-605906 is an inhibitor of inhibitor of kappa B kinase subunit β (IKKβ; IC50 = 380 nM).{32502} It is selective for IKKβ over insulin-like growth factor 1 (IGF1; IC50 = 7.6 μM) and over 100 kinases in a panel up to 10 μM. BI-605906 partially inhibits IL-1-stimulated activation of IKKε/TBK1 in vitro. BI-605906 also inhibits TNF-α-dependent IkB degradation and expression of the proinflammatory cytokines IL-6, IL-1β, and C-X-C motif ligand 1/2 (CXCL1/2) without affecting lipogenic gene expression or glucose production in murine primary hepatocytes.{40150}  

     

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    Cayman
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  • BI-605906 is an inhibitor of inhibitor of kappa B kinase subunit β (IKKβ; IC50 = 380 nM).{32502} It is selective for IKKβ over insulin-like growth factor 1 (IGF1; IC50 = 7.6 μM) and over 100 kinases in a panel up to 10 μM. BI-605906 partially inhibits IL-1-stimulated activation of IKKε/TBK1 in vitro. BI-605906 also inhibits TNF-α-dependent IkB degradation and expression of the proinflammatory cytokines IL-6, IL-1β, and C-X-C motif ligand 1/2 (CXCL1/2) without affecting lipogenic gene expression or glucose production in murine primary hepatocytes.{40150}  

     

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    Cayman
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  • BI-671800 is an antagonist of the prostaglandin D2 (PGD2; Item No. 12010) receptor CRTH2/DP2 (IC50 = 42 nM in a radioligand binding assay).{17373} It binds selectively to CRTH2/DP2 over DP1, thromboxane, and prostacyclin receptors (IC50s = 25.6, 62.6, and >100 μM, respectively). BI-671800 inhibits PGD2-induced shape change in human eosinophils (IC50 = 744 nM).  

     

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    Cayman
    SKU:27638 - 1 mg

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  • BI-671800 is an antagonist of the prostaglandin D2 (PGD2; Item No. 12010) receptor CRTH2/DP2 (IC50 = 42 nM in a radioligand binding assay).{17373} It binds selectively to CRTH2/DP2 over DP1, thromboxane, and prostacyclin receptors (IC50s = 25.6, 62.6, and >100 μM, respectively). BI-671800 inhibits PGD2-induced shape change in human eosinophils (IC50 = 744 nM).  

     

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    Cayman
    SKU:27638 - 10 mg

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  • BI-671800 is an antagonist of the prostaglandin D2 (PGD2; Item No. 12010) receptor CRTH2/DP2 (IC50 = 42 nM in a radioligand binding assay).{17373} It binds selectively to CRTH2/DP2 over DP1, thromboxane, and prostacyclin receptors (IC50s = 25.6, 62.6, and >100 μM, respectively). BI-671800 inhibits PGD2-induced shape change in human eosinophils (IC50 = 744 nM).  

     

    Brand:
    Cayman
    SKU:27638 - 5 mg

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  • Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} BI-6727 is a dihydropteridinone that inhibits Plk1, Plk2, and Plk3 (IC50s = 0.87, 5, and 56 nM, respectively), inducing mitotic arrest and apoptosis.{29375} It inhibits proliferation of multiple cancer cell lines with EC50 values ranging from 11-37 nM and prevents the growth of various human carcinoma xenografts in mice.{29375} BI-6727 was found to reverse ABC-efflux transporter-mediated multidrug resistance activity through its inhibition of the transport activity of ABCB1 and ABCG2, thus promoting mitotic arrest in resistant cancer cells.{29376}  

     

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    Cayman
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  • Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} BI-6727 is a dihydropteridinone that inhibits Plk1, Plk2, and Plk3 (IC50s = 0.87, 5, and 56 nM, respectively), inducing mitotic arrest and apoptosis.{29375} It inhibits proliferation of multiple cancer cell lines with EC50 values ranging from 11-37 nM and prevents the growth of various human carcinoma xenografts in mice.{29375} BI-6727 was found to reverse ABC-efflux transporter-mediated multidrug resistance activity through its inhibition of the transport activity of ABCB1 and ABCG2, thus promoting mitotic arrest in resistant cancer cells.{29376}  

     

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    Cayman
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  • Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} BI-6727 is a dihydropteridinone that inhibits Plk1, Plk2, and Plk3 (IC50s = 0.87, 5, and 56 nM, respectively), inducing mitotic arrest and apoptosis.{29375} It inhibits proliferation of multiple cancer cell lines with EC50 values ranging from 11-37 nM and prevents the growth of various human carcinoma xenografts in mice.{29375} BI-6727 was found to reverse ABC-efflux transporter-mediated multidrug resistance activity through its inhibition of the transport activity of ABCB1 and ABCG2, thus promoting mitotic arrest in resistant cancer cells.{29376}  

     

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    Cayman
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  • Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} BI-6727 is a dihydropteridinone that inhibits Plk1, Plk2, and Plk3 (IC50s = 0.87, 5, and 56 nM, respectively), inducing mitotic arrest and apoptosis.{29375} It inhibits proliferation of multiple cancer cell lines with EC50 values ranging from 11-37 nM and prevents the growth of various human carcinoma xenografts in mice.{29375} BI-6727 was found to reverse ABC-efflux transporter-mediated multidrug resistance activity through its inhibition of the transport activity of ABCB1 and ABCG2, thus promoting mitotic arrest in resistant cancer cells.{29376}  

     

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  • BH3-interacting domain (Bid) is cleaved by caspase-8 to produce the truncated protein tBid, which facilitates cytochrome c release from mitochondria and drives apoptosis.{28610,28613} BI-6C9 is an inhibitor of tBid (Kd = 20 µM), blocking the release of both cytochrome c and second mitochondria-derived activator of caspase from mitochondria.{28607,28608} It prevents apoptosis in neurons treated with glutamate or oxygen-glucose deprivation.{28611,28609} BI-6C9 (10 µM) also inhibits the nuclear translocation of apoptosis-inducing factor AIF, preventing the death of ovarian OVCAR-3 cancer cells induced by IFN-α2a.{28612}  

     

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    Cayman
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  • BH3-interacting domain (Bid) is cleaved by caspase-8 to produce the truncated protein tBid, which facilitates cytochrome c release from mitochondria and drives apoptosis.{28610,28613} BI-6C9 is an inhibitor of tBid (Kd = 20 µM), blocking the release of both cytochrome c and second mitochondria-derived activator of caspase from mitochondria.{28607,28608} It prevents apoptosis in neurons treated with glutamate or oxygen-glucose deprivation.{28611,28609} BI-6C9 (10 µM) also inhibits the nuclear translocation of apoptosis-inducing factor AIF, preventing the death of ovarian OVCAR-3 cancer cells induced by IFN-α2a.{28612}  

     

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  • BH3-interacting domain (Bid) is cleaved by caspase-8 to produce the truncated protein tBid, which facilitates cytochrome c release from mitochondria and drives apoptosis.{28610,28613} BI-6C9 is an inhibitor of tBid (Kd = 20 µM), blocking the release of both cytochrome c and second mitochondria-derived activator of caspase from mitochondria.{28607,28608} It prevents apoptosis in neurons treated with glutamate or oxygen-glucose deprivation.{28611,28609} BI-6C9 (10 µM) also inhibits the nuclear translocation of apoptosis-inducing factor AIF, preventing the death of ovarian OVCAR-3 cancer cells induced by IFN-α2a.{28612}  

     

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    Cayman
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  • BI-7273 is a potent BRD9 bromodomain inhibitor (Kd = 15.4 nM; IC50 = 19 nM) that less effectively inhibits the functionally and structurally related BRD7 bromodomain (IC50 = 117 nM).{30788} It is without effect against the bromodomains of BRD2 and BRD4, as well as a panel of kinases. BI-7273 inhibits the growth of EOL-1 acute myeloid leukemia cells in vitro (EC50 = 1.4 µM).{30788}  

     

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    Cayman
    SKU:20311 -

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  • BI-7273 is a potent BRD9 bromodomain inhibitor (Kd = 15.4 nM; IC50 = 19 nM) that less effectively inhibits the functionally and structurally related BRD7 bromodomain (IC50 = 117 nM).{30788} It is without effect against the bromodomains of BRD2 and BRD4, as well as a panel of kinases. BI-7273 inhibits the growth of EOL-1 acute myeloid leukemia cells in vitro (EC50 = 1.4 µM).{30788}  

     

    Brand:
    Cayman
    SKU:20311 -

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  • BI-7273 is a potent BRD9 bromodomain inhibitor (Kd = 15.4 nM; IC50 = 19 nM) that less effectively inhibits the functionally and structurally related BRD7 bromodomain (IC50 = 117 nM).{30788} It is without effect against the bromodomains of BRD2 and BRD4, as well as a panel of kinases. BI-7273 inhibits the growth of EOL-1 acute myeloid leukemia cells in vitro (EC50 = 1.4 µM).{30788}  

     

    Brand:
    Cayman
    SKU:20311 -

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  • BI-7273 is a potent BRD9 bromodomain inhibitor (Kd = 15.4 nM; IC50 = 19 nM) that less effectively inhibits the functionally and structurally related BRD7 bromodomain (IC50 = 117 nM).{30788} It is without effect against the bromodomains of BRD2 and BRD4, as well as a panel of kinases. BI-7273 inhibits the growth of EOL-1 acute myeloid leukemia cells in vitro (EC50 = 1.4 µM).{30788}  

     

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    Cayman
    SKU:20311 -

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  • BI-78D3 is an inhibitor of JNK (IC50 = 280 nM in a TR-FRET assay) that is competitive for JNK1 binding with pepJIP1, a JNK-interacting protein, with an IC50 value of 500 nM.{38279} It is selective for JNK, being 100-fold less active for the structurally similar MAPK family protein p38α and inactive at mammalian target of rapamycin (mTOR) or phosphatidylinositol 3-kinase α (PI3Kα). In a cell-based kinase assay, BI-78D3 inhibits c-Jun phosphorylation induced by TNF-α (EC50 = 12.4 µM). In a mouse model of type 2 diabetes, BI-78D3 (25 mg/kg) restores insulin sensitivity, reducing blood glucose levels when administered 30 minutes prior to insulin. BI-78D3 (30 µM) reduces contractions in human prostate strips induced by phenylephrine (Item Nos. 17205 | 18619) or norepinephrine (Item No. 16673) and reduces phosphorylation of c-Jun, a JNK substrate.{38280}  

     

    Brand:
    Cayman
    SKU:21183 -

    Out of stock

  • BI-78D3 is an inhibitor of JNK (IC50 = 280 nM in a TR-FRET assay) that is competitive for JNK1 binding with pepJIP1, a JNK-interacting protein, with an IC50 value of 500 nM.{38279} It is selective for JNK, being 100-fold less active for the structurally similar MAPK family protein p38α and inactive at mammalian target of rapamycin (mTOR) or phosphatidylinositol 3-kinase α (PI3Kα). In a cell-based kinase assay, BI-78D3 inhibits c-Jun phosphorylation induced by TNF-α (EC50 = 12.4 µM). In a mouse model of type 2 diabetes, BI-78D3 (25 mg/kg) restores insulin sensitivity, reducing blood glucose levels when administered 30 minutes prior to insulin. BI-78D3 (30 µM) reduces contractions in human prostate strips induced by phenylephrine (Item Nos. 17205 | 18619) or norepinephrine (Item No. 16673) and reduces phosphorylation of c-Jun, a JNK substrate.{38280}  

     

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    Cayman
    SKU:21183 -

    Out of stock

  • BI-78D3 is an inhibitor of JNK (IC50 = 280 nM in a TR-FRET assay) that is competitive for JNK1 binding with pepJIP1, a JNK-interacting protein, with an IC50 value of 500 nM.{38279} It is selective for JNK, being 100-fold less active for the structurally similar MAPK family protein p38α and inactive at mammalian target of rapamycin (mTOR) or phosphatidylinositol 3-kinase α (PI3Kα). In a cell-based kinase assay, BI-78D3 inhibits c-Jun phosphorylation induced by TNF-α (EC50 = 12.4 µM). In a mouse model of type 2 diabetes, BI-78D3 (25 mg/kg) restores insulin sensitivity, reducing blood glucose levels when administered 30 minutes prior to insulin. BI-78D3 (30 µM) reduces contractions in human prostate strips induced by phenylephrine (Item Nos. 17205 | 18619) or norepinephrine (Item No. 16673) and reduces phosphorylation of c-Jun, a JNK substrate.{38280}  

     

    Brand:
    Cayman
    SKU:21183 -

    Out of stock

  • BI-78D3 is an inhibitor of JNK (IC50 = 280 nM in a TR-FRET assay) that is competitive for JNK1 binding with pepJIP1, a JNK-interacting protein, with an IC50 value of 500 nM.{38279} It is selective for JNK, being 100-fold less active for the structurally similar MAPK family protein p38α and inactive at mammalian target of rapamycin (mTOR) or phosphatidylinositol 3-kinase α (PI3Kα). In a cell-based kinase assay, BI-78D3 inhibits c-Jun phosphorylation induced by TNF-α (EC50 = 12.4 µM). In a mouse model of type 2 diabetes, BI-78D3 (25 mg/kg) restores insulin sensitivity, reducing blood glucose levels when administered 30 minutes prior to insulin. BI-78D3 (30 µM) reduces contractions in human prostate strips induced by phenylephrine (Item Nos. 17205 | 18619) or norepinephrine (Item No. 16673) and reduces phosphorylation of c-Jun, a JNK substrate.{38280}  

     

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    Cayman
    SKU:21183 -

    Out of stock

  • BI-847325 is a selective dual MEK/Aurora kinase inhibitor with IC50 values of 3, 25, 15, 25, and 4 nM for X. laevis Aurora B, human Aurora A and Aurora C, and human MEK1 and MEK2, respectively.{29630} It can inhibit the growth and survival of both treatment-naive and drug-resistant melanoma cell lines, decreasing the expression of MEK and Mcl-1 while increasing the expression of pro-apoptotic protein Bim.{29630} At 70 mg/kg, BI-847325 induces apoptosis in treatment-naive and drug-resistant xenografted melanoma in vivo.{29630}  

     

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  • BI-847325 is a selective dual MEK/Aurora kinase inhibitor with IC50 values of 3, 25, 15, 25, and 4 nM for X. laevis Aurora B, human Aurora A and Aurora C, and human MEK1 and MEK2, respectively.{29630} It can inhibit the growth and survival of both treatment-naive and drug-resistant melanoma cell lines, decreasing the expression of MEK and Mcl-1 while increasing the expression of pro-apoptotic protein Bim.{29630} At 70 mg/kg, BI-847325 induces apoptosis in treatment-naive and drug-resistant xenografted melanoma in vivo.{29630}  

     

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  • BI-882370 is an orally bioavailable RAF inhibitor with IC50 values of 0.8, 0.8, and 0.6 nM for B-RAFV600E, wild-type B-RAF, and C-RAF in the DFG-out inactive conformation, respectively.{42482} It is selective for RAF over a panel of kinases, including LCK, KIT, Src, LYNA, LYNB, and PDGFR (IC50s = 49, 415, 485, 750, 715, and 1,220 nM, respectively). It inhibits proliferation of human B-RAF-mutant melanoma cells when used at concentrations ranging from 1 to 10 nM. It reduces tumor growth in multiple B-RAF-mutant melanoma and colorectal carcinoma mouse xenograft models when administered at a dose of 25 mg/kg twice per day. BI-882370, alone and in combination with trametinib (Item No. 16292), induces tumor regression in an A375 melanoma mouse xenograft model with no resistance developing within three or five weeks, respectively.  

     

    Brand:
    Cayman
    SKU:24273 - 1 mg

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  • BI-882370 is an orally bioavailable RAF inhibitor with IC50 values of 0.8, 0.8, and 0.6 nM for B-RAFV600E, wild-type B-RAF, and C-RAF in the DFG-out inactive conformation, respectively.{42482} It is selective for RAF over a panel of kinases, including LCK, KIT, Src, LYNA, LYNB, and PDGFR (IC50s = 49, 415, 485, 750, 715, and 1,220 nM, respectively). It inhibits proliferation of human B-RAF-mutant melanoma cells when used at concentrations ranging from 1 to 10 nM. It reduces tumor growth in multiple B-RAF-mutant melanoma and colorectal carcinoma mouse xenograft models when administered at a dose of 25 mg/kg twice per day. BI-882370, alone and in combination with trametinib (Item No. 16292), induces tumor regression in an A375 melanoma mouse xenograft model with no resistance developing within three or five weeks, respectively.  

     

    Brand:
    Cayman
    SKU:24273 - 10 mg

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  • BI-882370 is an orally bioavailable RAF inhibitor with IC50 values of 0.8, 0.8, and 0.6 nM for B-RAFV600E, wild-type B-RAF, and C-RAF in the DFG-out inactive conformation, respectively.{42482} It is selective for RAF over a panel of kinases, including LCK, KIT, Src, LYNA, LYNB, and PDGFR (IC50s = 49, 415, 485, 750, 715, and 1,220 nM, respectively). It inhibits proliferation of human B-RAF-mutant melanoma cells when used at concentrations ranging from 1 to 10 nM. It reduces tumor growth in multiple B-RAF-mutant melanoma and colorectal carcinoma mouse xenograft models when administered at a dose of 25 mg/kg twice per day. BI-882370, alone and in combination with trametinib (Item No. 16292), induces tumor regression in an A375 melanoma mouse xenograft model with no resistance developing within three or five weeks, respectively.  

     

    Brand:
    Cayman
    SKU:24273 - 25 mg

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  • BI-882370 is an orally bioavailable RAF inhibitor with IC50 values of 0.8, 0.8, and 0.6 nM for B-RAFV600E, wild-type B-RAF, and C-RAF in the DFG-out inactive conformation, respectively.{42482} It is selective for RAF over a panel of kinases, including LCK, KIT, Src, LYNA, LYNB, and PDGFR (IC50s = 49, 415, 485, 750, 715, and 1,220 nM, respectively). It inhibits proliferation of human B-RAF-mutant melanoma cells when used at concentrations ranging from 1 to 10 nM. It reduces tumor growth in multiple B-RAF-mutant melanoma and colorectal carcinoma mouse xenograft models when administered at a dose of 25 mg/kg twice per day. BI-882370, alone and in combination with trametinib (Item No. 16292), induces tumor regression in an A375 melanoma mouse xenograft model with no resistance developing within three or five weeks, respectively.  

     

    Brand:
    Cayman
    SKU:24273 - 5 mg

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  • BI-9564 is a selective inhibitor of BRD9 and BRD7 bromodomains (Kds = 14.1 and 239 nM; IC50s = 75 nM and 3.4 µM, respectively) that demonstrates cellular activity by semi-quantitative FRAP assay with ~90% inhibition of BRD9 and BRD7 at 0.1 µM and 1 µM, respectively.{30788,31210} It does not bind to other bromodomain-containing BET family members (IC50s >100 µM as assessed by AlphaScreen), kinases, or G protein-coupled receptors and shows off-target selectivity only to the CECR2 bromodomain in in vitro ITC assays (Kd = 258 nM), but not in cell-based assays at concentrations up to 1 µM.{30788} BI-9564 has been shown to inhibit the growth of EOL-1 AML cells both in vitro (EC50 = 800 nM) and in a disseminated mouse model of AML (180 mg/kg/day).{30788} See the Structural Genomics Consortium (SGC) website for more information.  

     

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  • BI-9564 is a selective inhibitor of BRD9 and BRD7 bromodomains (Kds = 14.1 and 239 nM; IC50s = 75 nM and 3.4 µM, respectively) that demonstrates cellular activity by semi-quantitative FRAP assay with ~90% inhibition of BRD9 and BRD7 at 0.1 µM and 1 µM, respectively.{30788,31210} It does not bind to other bromodomain-containing BET family members (IC50s >100 µM as assessed by AlphaScreen), kinases, or G protein-coupled receptors and shows off-target selectivity only to the CECR2 bromodomain in in vitro ITC assays (Kd = 258 nM), but not in cell-based assays at concentrations up to 1 µM.{30788} BI-9564 has been shown to inhibit the growth of EOL-1 AML cells both in vitro (EC50 = 800 nM) and in a disseminated mouse model of AML (180 mg/kg/day).{30788} See the Structural Genomics Consortium (SGC) website for more information.  

     

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    Cayman
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  • BI-9564 is a selective inhibitor of BRD9 and BRD7 bromodomains (Kds = 14.1 and 239 nM; IC50s = 75 nM and 3.4 µM, respectively) that demonstrates cellular activity by semi-quantitative FRAP assay with ~90% inhibition of BRD9 and BRD7 at 0.1 µM and 1 µM, respectively.{30788,31210} It does not bind to other bromodomain-containing BET family members (IC50s >100 µM as assessed by AlphaScreen), kinases, or G protein-coupled receptors and shows off-target selectivity only to the CECR2 bromodomain in in vitro ITC assays (Kd = 258 nM), but not in cell-based assays at concentrations up to 1 µM.{30788} BI-9564 has been shown to inhibit the growth of EOL-1 AML cells both in vitro (EC50 = 800 nM) and in a disseminated mouse model of AML (180 mg/kg/day).{30788} See the Structural Genomics Consortium (SGC) website for more information.  

     

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  • BI-9627 is an inhibitor of sodium-hydrogen exchanger isoform 1 (NHE1), with IC50 values of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively.{48743} It is greater than 30-fold selective for NHE1 over NHE2 and is inactive at NHE3 up to 16 μM in a pHi assay. BI-9627 inhibits phenylephrine-induced hypertrophy in neonatal rat cardiomyocytes.{48744} It increases recovery of left ventricular developed pressure and inhibits increases in left ventricular end-diastolic pressure (LVEDP) in a Langendorff isolated perfused rat heart model of ischemia-reperfusion injury when used at a concentration of 100 nM.{48743} BI-9627 (45 and 150 ppm in the diet) also attenuates decreases in left ventricular end-systolic pressure and increases in LVEDP in coronary artery-ligated rats.{48744}  

     

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    Cayman
    SKU:27640 - 1 mg

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  • BI-9627 is an inhibitor of sodium-hydrogen exchanger isoform 1 (NHE1), with IC50 values of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively.{48743} It is greater than 30-fold selective for NHE1 over NHE2 and is inactive at NHE3 up to 16 μM in a pHi assay. BI-9627 inhibits phenylephrine-induced hypertrophy in neonatal rat cardiomyocytes.{48744} It increases recovery of left ventricular developed pressure and inhibits increases in left ventricular end-diastolic pressure (LVEDP) in a Langendorff isolated perfused rat heart model of ischemia-reperfusion injury when used at a concentration of 100 nM.{48743} BI-9627 (45 and 150 ppm in the diet) also attenuates decreases in left ventricular end-systolic pressure and increases in LVEDP in coronary artery-ligated rats.{48744}  

     

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    Cayman
    SKU:27640 - 10 mg

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  • BI-9627 is an inhibitor of sodium-hydrogen exchanger isoform 1 (NHE1), with IC50 values of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively.{48743} It is greater than 30-fold selective for NHE1 over NHE2 and is inactive at NHE3 up to 16 μM in a pHi assay. BI-9627 inhibits phenylephrine-induced hypertrophy in neonatal rat cardiomyocytes.{48744} It increases recovery of left ventricular developed pressure and inhibits increases in left ventricular end-diastolic pressure (LVEDP) in a Langendorff isolated perfused rat heart model of ischemia-reperfusion injury when used at a concentration of 100 nM.{48743} BI-9627 (45 and 150 ppm in the diet) also attenuates decreases in left ventricular end-systolic pressure and increases in LVEDP in coronary artery-ligated rats.{48744}  

     

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    Cayman
    SKU:27640 - 5 mg

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  • The 90 kDa ribosomal S6 kinases (RSKs) are a group of serine/threonine kinases involved in diverse cellular processes, including growth, survival, and motility.{24631} BI-D1870 is a cell permeable, ATP-competitive inhibitor of the four vertebrate isoforms of RSK, RSK1-4 (IC50s = 31, 24, 18, and 15 nM, respectively).{24632} At 100 nM, it also significantly inhibits polo-like kinase 1, Aurora B, maternal embryonic leucine zipper kinase, and mammalian STE20-like kinase 2.{24632,17331} BI-D1870 acts at the N-terminal kinase domain, but not the C-terminal domain, of RSK.{24632,17331}  

     

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  • The 90 kDa ribosomal S6 kinases (RSKs) are a group of serine/threonine kinases involved in diverse cellular processes, including growth, survival, and motility.{24631} BI-D1870 is a cell permeable, ATP-competitive inhibitor of the four vertebrate isoforms of RSK, RSK1-4 (IC50s = 31, 24, 18, and 15 nM, respectively).{24632} At 100 nM, it also significantly inhibits polo-like kinase 1, Aurora B, maternal embryonic leucine zipper kinase, and mammalian STE20-like kinase 2.{24632,17331} BI-D1870 acts at the N-terminal kinase domain, but not the C-terminal domain, of RSK.{24632,17331}  

     

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    Cayman
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  • The 90 kDa ribosomal S6 kinases (RSKs) are a group of serine/threonine kinases involved in diverse cellular processes, including growth, survival, and motility.{24631} BI-D1870 is a cell permeable, ATP-competitive inhibitor of the four vertebrate isoforms of RSK, RSK1-4 (IC50s = 31, 24, 18, and 15 nM, respectively).{24632} At 100 nM, it also significantly inhibits polo-like kinase 1, Aurora B, maternal embryonic leucine zipper kinase, and mammalian STE20-like kinase 2.{24632,17331} BI-D1870 acts at the N-terminal kinase domain, but not the C-terminal domain, of RSK.{24632,17331}  

     

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  • BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH; IC50 = 4.9 nM in HEK293T cells expressing the human recombinant enzyme).{40060} It also inhibits FAAH2, α/β-hydrolase domain-containing protein 6 (ABHD6), carboxylesterase 2 (CES2), and patatin-like phospholipase domain 6 (PNPLA6) with IC50 values of 0.4, 0.081, 2, and 11 μM, respectively. BIA 10-2474 alters expression of 161 lipid species, including FAAH substrates as well as other lipid classes, in human cortical neuron cultures indicating compound promiscuity. Formulations containing BIA 10-2474 were previously investigated clinically for the management of chronic pain but use was halted due to development of significant neurotoxicity.  

     

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    Cayman
    SKU:23157 - 10 mg

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  • BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH; IC50 = 4.9 nM in HEK293T cells expressing the human recombinant enzyme).{40060} It also inhibits FAAH2, α/β-hydrolase domain-containing protein 6 (ABHD6), carboxylesterase 2 (CES2), and patatin-like phospholipase domain 6 (PNPLA6) with IC50 values of 0.4, 0.081, 2, and 11 μM, respectively. BIA 10-2474 alters expression of 161 lipid species, including FAAH substrates as well as other lipid classes, in human cortical neuron cultures indicating compound promiscuity. Formulations containing BIA 10-2474 were previously investigated clinically for the management of chronic pain but use was halted due to development of significant neurotoxicity.  

     

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    Cayman
    SKU:23157 - 25 mg

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  • BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH; IC50 = 4.9 nM in HEK293T cells expressing the human recombinant enzyme).{40060} It also inhibits FAAH2, α/β-hydrolase domain-containing protein 6 (ABHD6), carboxylesterase 2 (CES2), and patatin-like phospholipase domain 6 (PNPLA6) with IC50 values of 0.4, 0.081, 2, and 11 μM, respectively. BIA 10-2474 alters expression of 161 lipid species, including FAAH substrates as well as other lipid classes, in human cortical neuron cultures indicating compound promiscuity. Formulations containing BIA 10-2474 were previously investigated clinically for the management of chronic pain but use was halted due to development of significant neurotoxicity.  

     

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    Cayman
    SKU:23157 - 5 mg

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  • Bialaphos is a natural non-selective phytotoxin produced by certain Streptomyces species. It is a pro-toxin, a tripeptide that is converted in vivo to the active agent phosphinothricin, which is a glutamine analog.{27463} L-Phosphinothricin inhibits glutamine synthetase (Ki = 6.1 µM), resulting in accumulation of ammonium and disruption of primary metabolism.{27463,27464} The bacterial bar gene encodes a phosphinothricin acetyltransferase, which confers resistance to phosphinothricin.{27244} Bialaphos is used in the selection of transgenic plants that express the bar gene, usually under the control of a constitutively active viral promoter.{27244}  

     

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    Cayman
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