Cayman

Showing 12001–12150 of 45550 results

  • N-Hydroxysuccinimide (NHS) activates carboxylic acid groups (on biotin) to facilitate coupling reactions. Biotin-X-NHS is a compound used to attach biotin to primary amines under alkaline conditions (pH~8-9). For example, lysines on the surface of proteins, including antibodies, are ideal targets for biotinylation with this compound. Biotin-X-NHS is like Biotin-NHS (Item No. 13315), but contains a six-atom spacer arm to minimize steric effects.  

     

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  • N-Hydroxysuccinimide (NHS) activates carboxylic acid groups (on biotin) to facilitate coupling reactions. Biotin-X-NHS is a compound used to attach biotin to primary amines under alkaline conditions (pH~8-9). For example, lysines on the surface of proteins, including antibodies, are ideal targets for biotinylation with this compound. Biotin-X-NHS is like Biotin-NHS (Item No. 13315), but contains a six-atom spacer arm to minimize steric effects.  

     

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    Cayman
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  • N-Hydroxysuccinimide (NHS) activates carboxylic acid groups (on biotin) to facilitate coupling reactions. Biotin-X-NHS is a compound used to attach biotin to primary amines under alkaline conditions (pH~8-9). For example, lysines on the surface of proteins, including antibodies, are ideal targets for biotinylation with this compound. Biotin-X-NHS is like Biotin-NHS (Item No. 13315), but contains a six-atom spacer arm to minimize steric effects.  

     

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  • Biotin-XX hydrazide is a biotylating reagent for carbohydrates and carbonyl compounds that contains two aminohexanoic spacers to increase the efficiency of avidin-binding by alleviating steric hindrance.{17906}  

     

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  • Biotin-XX hydrazide is a biotylating reagent for carbohydrates and carbonyl compounds that contains two aminohexanoic spacers to increase the efficiency of avidin-binding by alleviating steric hindrance.{17906}  

     

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  • Biotin-XX hydrazide is a biotylating reagent for carbohydrates and carbonyl compounds that contains two aminohexanoic spacers to increase the efficiency of avidin-binding by alleviating steric hindrance.{17906}  

     

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  • Biotinidase is a peptidyl hydrolase that cleaves biocytin and biotinylated peptides in vivo to generate free biotin, an essential coenzyme for certain carboxylases involved in fatty acid, amino acid, and glucose metabolism.{32218,42936} Early-onset biotinidase deficiency is due to deletion, insertion, substitution, or missense mutations in the biotinidase gene, BTD, that affect the activity of multiple carboxylases. This profound biotinidase deficiency results in seizures, ataxia, sensorineural hearing loss or vision loss, eczema, and respiratory disruptions without treatment. Partial biotinidase deficiency is due to a substitution mutation in the BTD gene resulting in a 70-90% reduction in biotinidase activity leading to symptom manifestation that may not occur until adolescence and occurs only under biological stress. Many symptoms resolve with treatment, but retinal degeneration, sensorineural hearing loss, and developmental delays cannot be reversed. Early detection of biotinidase deficiency is imperative to avoid permanent damage.  

     

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    Cayman
    SKU:27544 - 1 ea

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  • Biotinyl tyramide is a reagent that has been used for tyramide signal amplification (TSA) via catalyzed reporter deposition (CARD).{45293} In CARD, a reporter enzyme, such as horseradish peroxidase (HRP) conjugated to a secondary antibody, is bound to the target of interest and catalyzes the covalent deposition of biotinyl tyramide to the sample. The sample is then probed by a detector, such as streptavidin-HRP, allowing detection via chromogenic or fluorescent methods. Biotinyl tyramide has been used in immunohistochemistry, ELISA, Western blot, and in situ hybridization applications.{45293,45294}  

     

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    Cayman
    SKU:27997 - 10 mg

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  • Biotinyl tyramide is a reagent that has been used for tyramide signal amplification (TSA) via catalyzed reporter deposition (CARD).{45293} In CARD, a reporter enzyme, such as horseradish peroxidase (HRP) conjugated to a secondary antibody, is bound to the target of interest and catalyzes the covalent deposition of biotinyl tyramide to the sample. The sample is then probed by a detector, such as streptavidin-HRP, allowing detection via chromogenic or fluorescent methods. Biotinyl tyramide has been used in immunohistochemistry, ELISA, Western blot, and in situ hybridization applications.{45293,45294}  

     

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    Cayman
    SKU:27997 - 25 mg

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  • Biotinyl tyramide is a reagent that has been used for tyramide signal amplification (TSA) via catalyzed reporter deposition (CARD).{45293} In CARD, a reporter enzyme, such as horseradish peroxidase (HRP) conjugated to a secondary antibody, is bound to the target of interest and catalyzes the covalent deposition of biotinyl tyramide to the sample. The sample is then probed by a detector, such as streptavidin-HRP, allowing detection via chromogenic or fluorescent methods. Biotinyl tyramide has been used in immunohistochemistry, ELISA, Western blot, and in situ hybridization applications.{45293,45294}  

     

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    Cayman
    SKU:27997 - 50 mg

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  • Apoptosis is induced by certain cytokines including TNF and Fas ligand in the TNF family through their death domain containing receptors. TNF-related apoptosis-inducing ligand (TRAIL or Apo2L), a member of this family, activates apoptosis in a variety of tumor cell lines by signaling through the death receptors, DR4 and DR5. Bioymifi directly activates DR5 (Kd = 1.2 µM; IC50 = 2 µM), inducing DR5 clustering, which leads to the initiation of FADD/caspase-8-dependent apoptosis in various cancer cells.{29884}  

     

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  • Apoptosis is induced by certain cytokines including TNF and Fas ligand in the TNF family through their death domain containing receptors. TNF-related apoptosis-inducing ligand (TRAIL or Apo2L), a member of this family, activates apoptosis in a variety of tumor cell lines by signaling through the death receptors, DR4 and DR5. Bioymifi directly activates DR5 (Kd = 1.2 µM; IC50 = 2 µM), inducing DR5 clustering, which leads to the initiation of FADD/caspase-8-dependent apoptosis in various cancer cells.{29884}  

     

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  • Apoptosis is induced by certain cytokines including TNF and Fas ligand in the TNF family through their death domain containing receptors. TNF-related apoptosis-inducing ligand (TRAIL or Apo2L), a member of this family, activates apoptosis in a variety of tumor cell lines by signaling through the death receptors, DR4 and DR5. Bioymifi directly activates DR5 (Kd = 1.2 µM; IC50 = 2 µM), inducing DR5 clustering, which leads to the initiation of FADD/caspase-8-dependent apoptosis in various cancer cells.{29884}  

     

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  • Apoptosis is induced by certain cytokines including TNF and Fas ligand in the TNF family through their death domain containing receptors. TNF-related apoptosis-inducing ligand (TRAIL or Apo2L), a member of this family, activates apoptosis in a variety of tumor cell lines by signaling through the death receptors, DR4 and DR5. Bioymifi directly activates DR5 (Kd = 1.2 µM; IC50 = 2 µM), inducing DR5 clustering, which leads to the initiation of FADD/caspase-8-dependent apoptosis in various cancer cells.{29884}  

     

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  • Biperiden is a muscarinic acetylcholine receptor antagonist of (Kis = 0.48, 6.3, 3.9, 2.4, and 6.3 nM for M1-5 receptors, respectively, in CHO-K1 cells expressing cloned receptors).{22786} It inhibits binding of [3H]quinuclidinyl benzilate (QNB) to muscarinic receptors in tissue homogenates (IC50s = 79, 52, and 38 nM for rat heart, rat lung, and guinea pig lung, respectively) and in vivo (IC50s = 2.5, 1.1, and 1.2 mg/kg for mouse cerebral cortex, cerebellum, and heart, respectively).{39393,39394} Biperiden (1 μM) increases spontaneous and electrically-evoked dopamine (DA) and electrically-evoked acetylcholine (ACh) release from rabbit caudate nucleus slices preincubated with dopamine in vitro.{39395} It is also an uncompetitive NMDA receptor antagonist and inhibits NMDA-evoked ACh release at a concentration of 10 μM.{39396} Biperiden (0.01-1.0 mg/kg) reduces physostigmine-induced tremor in rats in a dose-dependent manner.{39397} Formulations containing biperiden have been used as an adjuvant treatment for Parkinson’s disease.  

     

    Brand:
    Cayman
    SKU:23775 - 10 mg

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  • Biperiden is a muscarinic acetylcholine receptor antagonist of (Kis = 0.48, 6.3, 3.9, 2.4, and 6.3 nM for M1-5 receptors, respectively, in CHO-K1 cells expressing cloned receptors).{22786} It inhibits binding of [3H]quinuclidinyl benzilate (QNB) to muscarinic receptors in tissue homogenates (IC50s = 79, 52, and 38 nM for rat heart, rat lung, and guinea pig lung, respectively) and in vivo (IC50s = 2.5, 1.1, and 1.2 mg/kg for mouse cerebral cortex, cerebellum, and heart, respectively).{39393,39394} Biperiden (1 μM) increases spontaneous and electrically-evoked dopamine (DA) and electrically-evoked acetylcholine (ACh) release from rabbit caudate nucleus slices preincubated with dopamine in vitro.{39395} It is also an uncompetitive NMDA receptor antagonist and inhibits NMDA-evoked ACh release at a concentration of 10 μM.{39396} Biperiden (0.01-1.0 mg/kg) reduces physostigmine-induced tremor in rats in a dose-dependent manner.{39397} Formulations containing biperiden have been used as an adjuvant treatment for Parkinson’s disease.  

     

    Brand:
    Cayman
    SKU:23775 - 25 mg

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  • Biperiden is a muscarinic acetylcholine receptor antagonist of (Kis = 0.48, 6.3, 3.9, 2.4, and 6.3 nM for M1-5 receptors, respectively, in CHO-K1 cells expressing cloned receptors).{22786} It inhibits binding of [3H]quinuclidinyl benzilate (QNB) to muscarinic receptors in tissue homogenates (IC50s = 79, 52, and 38 nM for rat heart, rat lung, and guinea pig lung, respectively) and in vivo (IC50s = 2.5, 1.1, and 1.2 mg/kg for mouse cerebral cortex, cerebellum, and heart, respectively).{39393,39394} Biperiden (1 μM) increases spontaneous and electrically-evoked dopamine (DA) and electrically-evoked acetylcholine (ACh) release from rabbit caudate nucleus slices preincubated with dopamine in vitro.{39395} It is also an uncompetitive NMDA receptor antagonist and inhibits NMDA-evoked ACh release at a concentration of 10 μM.{39396} Biperiden (0.01-1.0 mg/kg) reduces physostigmine-induced tremor in rats in a dose-dependent manner.{39397} Formulations containing biperiden have been used as an adjuvant treatment for Parkinson’s disease.  

     

    Brand:
    Cayman
    SKU:23775 - 5 mg

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  • Biperiden is a muscarinic acetylcholine receptor antagonist of (Kis = 0.48, 6.3, 3.9, 2.4, and 6.3 nM for M1-5 receptors, respectively, in CHO-K1 cells expressing cloned receptors).{22786} It inhibits binding of [3H]quinuclidinyl benzilate (QNB) to muscarinic receptors in tissue homogenates (IC50s = 79, 52, and 38 nM for rat heart, rat lung, and guinea pig lung, respectively) and in vivo (IC50s = 2.5, 1.1, and 1.2 mg/kg for mouse cerebral cortex, cerebellum, and heart, respectively).{39393,39394} Biperiden (1 μM) increases spontaneous and electrically-evoked dopamine (DA) and electrically-evoked acetylcholine (ACh) release from rabbit caudate nucleus slices preincubated with dopamine in vitro.{39395} It is also an uncompetitive NMDA receptor antagonist and inhibits NMDA-evoked ACh release at a concentration of 10 μM.{39396} Biperiden (0.01-1.0 mg/kg) reduces physostigmine-induced tremor in rats in a dose-dependent manner.{39397} Formulations containing biperiden have been used as an adjuvant treatment for Parkinson’s disease.  

     

    Brand:
    Cayman
    SKU:23775 - 50 mg

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  • Biphenyl-4-amidoxime is a synthetic intermediate useful for pharmaceutical synthesis.  

     

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    SKU:11054 - 1 g

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  • Biphenyl-4-amidoxime is a synthetic intermediate useful for pharmaceutical synthesis.  

     

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    SKU:11054 - 5 g

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  • Biphenyl-4-amidoxime is a synthetic intermediate useful for pharmaceutical synthesis.  

     

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    SKU:11054 - 500 mg

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  • The metabotropic glutamate receptor 2 (mGluR2) is a Gi/o-coupled receptor which is expressed on presynaptic nerve terminals and modulates the release of neurotransmitters like glutamate and GABA.{21987} Biphenylindanone A (BINA) is a positive allosteric modulator of mGluR2, stimulating the human and rat receptors with EC50 values of 33.2 and 96 nM, respectively.{21984} It has no effect on glutamate-induced activation of other mGluR types.{21984} BINA can be used on cells, tissues, or animals.{21984,21983} Because of its selectivity for mGluR2, robust in vivo activity, and brain penetrance, BINA can be used to elucidate the role of mGluR2 in such diverse processes as psychosis, schizophrenia, and drug addiction.{21982,21985,21986}  

     

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    Cayman
    SKU:11986 - 10 mg

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  • The metabotropic glutamate receptor 2 (mGluR2) is a Gi/o-coupled receptor which is expressed on presynaptic nerve terminals and modulates the release of neurotransmitters like glutamate and GABA.{21987} Biphenylindanone A (BINA) is a positive allosteric modulator of mGluR2, stimulating the human and rat receptors with EC50 values of 33.2 and 96 nM, respectively.{21984} It has no effect on glutamate-induced activation of other mGluR types.{21984} BINA can be used on cells, tissues, or animals.{21984,21983} Because of its selectivity for mGluR2, robust in vivo activity, and brain penetrance, BINA can be used to elucidate the role of mGluR2 in such diverse processes as psychosis, schizophrenia, and drug addiction.{21982,21985,21986}  

     

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    Cayman
    SKU:11986 - 25 mg

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  • The metabotropic glutamate receptor 2 (mGluR2) is a Gi/o-coupled receptor which is expressed on presynaptic nerve terminals and modulates the release of neurotransmitters like glutamate and GABA.{21987} Biphenylindanone A (BINA) is a positive allosteric modulator of mGluR2, stimulating the human and rat receptors with EC50 values of 33.2 and 96 nM, respectively.{21984} It has no effect on glutamate-induced activation of other mGluR types.{21984} BINA can be used on cells, tissues, or animals.{21984,21983} Because of its selectivity for mGluR2, robust in vivo activity, and brain penetrance, BINA can be used to elucidate the role of mGluR2 in such diverse processes as psychosis, schizophrenia, and drug addiction.{21982,21985,21986}  

     

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    SKU:11986 - 5 mg

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  • Birinapant is a bivalent mimetic of the Diablo homolog known as second mitochondria-derived activator of caspase (Smac). It is an antagonist of cellular inhibitor of apoptosis 1 (cIAP1, or BIRC2), cIAP2 (BIRC3), and XIAP (BIRC4), binding each at nanomolar concentrations.{34146} Birinapant causes rapid cIAP1 degradation, caspase activation, PARP cleavage, and NF-κB activation in breast cancer cells.{34146} It shows in vivo antitumor activity, inducing apoptosis in several types of cancer xenografts in mice.{34147,34148}  

     

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    SKU:19699 -

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  • Birinapant is a bivalent mimetic of the Diablo homolog known as second mitochondria-derived activator of caspase (Smac). It is an antagonist of cellular inhibitor of apoptosis 1 (cIAP1, or BIRC2), cIAP2 (BIRC3), and XIAP (BIRC4), binding each at nanomolar concentrations.{34146} Birinapant causes rapid cIAP1 degradation, caspase activation, PARP cleavage, and NF-κB activation in breast cancer cells.{34146} It shows in vivo antitumor activity, inducing apoptosis in several types of cancer xenografts in mice.{34147,34148}  

     

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    Cayman
    SKU:19699 -

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  • Birinapant is a bivalent mimetic of the Diablo homolog known as second mitochondria-derived activator of caspase (Smac). It is an antagonist of cellular inhibitor of apoptosis 1 (cIAP1, or BIRC2), cIAP2 (BIRC3), and XIAP (BIRC4), binding each at nanomolar concentrations.{34146} Birinapant causes rapid cIAP1 degradation, caspase activation, PARP cleavage, and NF-κB activation in breast cancer cells.{34146} It shows in vivo antitumor activity, inducing apoptosis in several types of cancer xenografts in mice.{34147,34148}  

     

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    Cayman
    SKU:19699 -

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  • Birinapant is a bivalent mimetic of the Diablo homolog known as second mitochondria-derived activator of caspase (Smac). It is an antagonist of cellular inhibitor of apoptosis 1 (cIAP1, or BIRC2), cIAP2 (BIRC3), and XIAP (BIRC4), binding each at nanomolar concentrations.{34146} Birinapant causes rapid cIAP1 degradation, caspase activation, PARP cleavage, and NF-κB activation in breast cancer cells.{34146} It shows in vivo antitumor activity, inducing apoptosis in several types of cancer xenografts in mice.{34147,34148}  

     

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    Cayman
    SKU:19699 -

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  • Bis-(2-chloroisopropyl) ether is a byproduct in the synthesis of ethylene and propylene glycol that has been found in municipal drinking water in the United States and waterways in the Netherlands where it is considered a persistent organic pollutant (POP).{42284} It is mutagenic in the S. typhimurium strains TA 1535 and TA 100 but lacks mutagenic activity in mice.  

     

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    Cayman
    SKU:20683 -

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  • Bis-(2-chloroisopropyl) ether is a byproduct in the synthesis of ethylene and propylene glycol that has been found in municipal drinking water in the United States and waterways in the Netherlands where it is considered a persistent organic pollutant (POP).{42284} It is mutagenic in the S. typhimurium strains TA 1535 and TA 100 but lacks mutagenic activity in mice.  

     

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    Cayman
    SKU:20683 -

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  • Bis-(2-chloroisopropyl) ether is a byproduct in the synthesis of ethylene and propylene glycol that has been found in municipal drinking water in the United States and waterways in the Netherlands where it is considered a persistent organic pollutant (POP).{42284} It is mutagenic in the S. typhimurium strains TA 1535 and TA 100 but lacks mutagenic activity in mice.  

     

    Brand:
    Cayman
    SKU:20683 -

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  • Bis-(2-chloroisopropyl) ether is a byproduct in the synthesis of ethylene and propylene glycol that has been found in municipal drinking water in the United States and waterways in the Netherlands where it is considered a persistent organic pollutant (POP).{42284} It is mutagenic in the S. typhimurium strains TA 1535 and TA 100 but lacks mutagenic activity in mice.  

     

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    SKU:20683 -

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  • bis-ANS is a high-affinity non-covalent extrinsic fluorescent dye used to analyze protein conformation.{33937} Its predominant interaction with proteins is through its hydrophobic phenyl and naphthyl rings.{33952} bis-ANS has an excitation maxima of 390 nm.{14908} It has an emission maximum of 523 nm when free in solution but undergoes a blue shift with an increase in fluorescence intensity when bound to protein; for example, when bound to intestinal fatty acid binding protein (FAPB2) it has emission maxima of 484-496 nm. bis-ANS has been used to label mechanically damaged neurons in acute brain slices.{33940} It also potently inhibits microtubule assembly.{33938,33939}  

     

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    SKU:21820 -

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  • bis-ANS is a high-affinity non-covalent extrinsic fluorescent dye used to analyze protein conformation.{33937} Its predominant interaction with proteins is through its hydrophobic phenyl and naphthyl rings.{33952} bis-ANS has an excitation maxima of 390 nm.{14908} It has an emission maximum of 523 nm when free in solution but undergoes a blue shift with an increase in fluorescence intensity when bound to protein; for example, when bound to intestinal fatty acid binding protein (FAPB2) it has emission maxima of 484-496 nm. bis-ANS has been used to label mechanically damaged neurons in acute brain slices.{33940} It also potently inhibits microtubule assembly.{33938,33939}  

     

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    SKU:21820 -

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  • bis-ANS is a high-affinity non-covalent extrinsic fluorescent dye used to analyze protein conformation.{33937} Its predominant interaction with proteins is through its hydrophobic phenyl and naphthyl rings.{33952} bis-ANS has an excitation maxima of 390 nm.{14908} It has an emission maximum of 523 nm when free in solution but undergoes a blue shift with an increase in fluorescence intensity when bound to protein; for example, when bound to intestinal fatty acid binding protein (FAPB2) it has emission maxima of 484-496 nm. bis-ANS has been used to label mechanically damaged neurons in acute brain slices.{33940} It also potently inhibits microtubule assembly.{33938,33939}  

     

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    Cayman
    SKU:21820 -

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  • Tacrine is an amino acridine compound that inhibits acetylcholinesterase (AChE), and has been proposed as a clinical treatment for Alzheimer’s disease.{6603} bis(7)-Tacrine is a tacrine dimer, linked via a 7-carbon alkyl spacer. It inhibits AChE with an IC50 of 0.40 nM, making it more than 1,000 times more potent than tacrine.{12097} bis(7)-Tacrine also protects against hydrogen peroxide induced apoptosis in rat pheochromocytoma cells.{12095}  

     

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    SKU:10005836 - 10 mg

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  • Tacrine is an amino acridine compound that inhibits acetylcholinesterase (AChE), and has been proposed as a clinical treatment for Alzheimer’s disease.{6603} bis(7)-Tacrine is a tacrine dimer, linked via a 7-carbon alkyl spacer. It inhibits AChE with an IC50 of 0.40 nM, making it more than 1,000 times more potent than tacrine.{12097} bis(7)-Tacrine also protects against hydrogen peroxide induced apoptosis in rat pheochromocytoma cells.{12095}  

     

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    Cayman
    SKU:10005836 - 100 mg

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  • Tacrine is an amino acridine compound that inhibits acetylcholinesterase (AChE), and has been proposed as a clinical treatment for Alzheimer’s disease.{6603} bis(7)-Tacrine is a tacrine dimer, linked via a 7-carbon alkyl spacer. It inhibits AChE with an IC50 of 0.40 nM, making it more than 1,000 times more potent than tacrine.{12097} bis(7)-Tacrine also protects against hydrogen peroxide induced apoptosis in rat pheochromocytoma cells.{12095}  

     

    Brand:
    Cayman
    SKU:10005836 - 5 mg

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  • Tacrine is an amino acridine compound that inhibits acetylcholinesterase (AChE), and has been proposed as a clinical treatment for Alzheimer’s disease.{6603} bis(7)-Tacrine is a tacrine dimer, linked via a 7-carbon alkyl spacer. It inhibits AChE with an IC50 of 0.40 nM, making it more than 1,000 times more potent than tacrine.{12097} bis(7)-Tacrine also protects against hydrogen peroxide induced apoptosis in rat pheochromocytoma cells.{12095}  

     

    Brand:
    Cayman
    SKU:10005836 - 50 mg

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  • Bis(methylthio)gliotoxin is a fungal metabolite originally isolated from G. deliquescens that has diverse biological activities.{36971} It inhibits PAF- and collagen-induced platelet aggregation in rabbit platelet-rich plasma (IC50s = 8.4 and 84.2 µM, respectively) but has no effect on arachidonic acid- or ADP-induced platelet aggregation (IC50s = >400 µM).{36972} Bis(methylthio)gliotoxin inhibits growth of HCT116 colon cancer cells (IC50 = 23.56 µM).{36973} It inhibits PAF-induced bronchoconstriction in guinea pigs when administered at a dose of 0.1 mg/kg and is less toxic to mice (LD50 = >500 mg/kg) than gliotoxin (Item No. 11433).{36972,36974} Bis(methylthio)gliotoxin has been used as a serum biomarker in patients infected with invasive aspergillosis.{36975}  

     

    Brand:
    Cayman
    SKU:26271 - 1 mg

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  • Bis(methylthio)gliotoxin is a fungal metabolite originally isolated from G. deliquescens that has diverse biological activities.{36971} It inhibits PAF- and collagen-induced platelet aggregation in rabbit platelet-rich plasma (IC50s = 8.4 and 84.2 µM, respectively) but has no effect on arachidonic acid- or ADP-induced platelet aggregation (IC50s = >400 µM).{36972} Bis(methylthio)gliotoxin inhibits growth of HCT116 colon cancer cells (IC50 = 23.56 µM).{36973} It inhibits PAF-induced bronchoconstriction in guinea pigs when administered at a dose of 0.1 mg/kg and is less toxic to mice (LD50 = >500 mg/kg) than gliotoxin (Item No. 11433).{36972,36974} Bis(methylthio)gliotoxin has been used as a serum biomarker in patients infected with invasive aspergillosis.{36975}  

     

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    Cayman
    SKU:26271 - 500 µg

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  • Bisacodyl is a prodrug form of the stimulant laxative desacetyl bisacodyl (Item No. 20928).{33529} It reduces the activity of Na+/K+-ATPases in isolated rat colon following administration in the drinking water at a concentration of 83 µM.{48734} Bisacodyl (20 mg/kg) decreases colonic aquaporin-3 levels and increases stool water content in rats, effects that are reversed by the COX inhibitor indomethacin (Item No. 70270).{33527} Formulations containing bisacodyl have been used in the treatment of constipation.  

     

    Brand:
    Cayman
    SKU:28826 - 10 g

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  • Bisacodyl is a prodrug form of the stimulant laxative desacetyl bisacodyl (Item No. 20928).{33529} It reduces the activity of Na+/K+-ATPases in isolated rat colon following administration in the drinking water at a concentration of 83 µM.{48734} Bisacodyl (20 mg/kg) decreases colonic aquaporin-3 levels and increases stool water content in rats, effects that are reversed by the COX inhibitor indomethacin (Item No. 70270).{33527} Formulations containing bisacodyl have been used in the treatment of constipation.  

     

    Brand:
    Cayman
    SKU:28826 - 100 g

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  • Bisacodyl is a prodrug form of the stimulant laxative desacetyl bisacodyl (Item No. 20928).{33529} It reduces the activity of Na+/K+-ATPases in isolated rat colon following administration in the drinking water at a concentration of 83 µM.{48734} Bisacodyl (20 mg/kg) decreases colonic aquaporin-3 levels and increases stool water content in rats, effects that are reversed by the COX inhibitor indomethacin (Item No. 70270).{33527} Formulations containing bisacodyl have been used in the treatment of constipation.  

     

    Brand:
    Cayman
    SKU:28826 - 25 g

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  • Bisacodyl is a prodrug form of the stimulant laxative desacetyl bisacodyl (Item No. 20928).{33529} It reduces the activity of Na+/K+-ATPases in isolated rat colon following administration in the drinking water at a concentration of 83 µM.{48734} Bisacodyl (20 mg/kg) decreases colonic aquaporin-3 levels and increases stool water content in rats, effects that are reversed by the COX inhibitor indomethacin (Item No. 70270).{33527} Formulations containing bisacodyl have been used in the treatment of constipation.  

     

    Brand:
    Cayman
    SKU:28826 - 50 g

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  • Bacterial type II fatty acid synthesis (FAS-II) is mediated by a series of enzymes, each of which may be targeted by potential antibiotics.{31077} Bischloroanthrabenzoxocinone (BABX) is an inhibitor of FAS-II, blocking fatty acid synthesis in S. aureus and E. coli with IC50 values of 11.4 and 35.3 µg/ml, respectively.{31076} It inhibits the growth of S. aureus and permeable E. coli strains with minimum inhibitory concentrations ranging from 0.2-0.4 µg/ml.{31076,31075} BABX also displays binding to liver X receptors (LXRs), inhibiting agonist binding in an LXRα-scintillation proximity assay (IC50 = 10 µM).{31075}  

     

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  • Bacterial type II fatty acid synthesis (FAS-II) is mediated by a series of enzymes, each of which may be targeted by potential antibiotics.{31077} Bischloroanthrabenzoxocinone (BABX) is an inhibitor of FAS-II, blocking fatty acid synthesis in S. aureus and E. coli with IC50 values of 11.4 and 35.3 µg/ml, respectively.{31076} It inhibits the growth of S. aureus and permeable E. coli strains with minimum inhibitory concentrations ranging from 0.2-0.4 µg/ml.{31076,31075} BABX also displays binding to liver X receptors (LXRs), inhibiting agonist binding in an LXRα-scintillation proximity assay (IC50 = 10 µM).{31075}  

     

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    Cayman
    SKU:-

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  • Bisdemethoxycurcumin (BDMC) is a natural demethoxy derivative of curcumin. It is a potent activator of macrophage phagocytosis, interacting with 1α,25-dihydroxy vitamin D3 to stimulate amyloid-β clearance by macrophages (optimal stimulation at 100 nM BDMC).{19781,19788,19791} More stable than curcumin in physiological media, BDMC suppresses proliferation in cancer cells.{19787,19792} It down-regulates the transcriptional coactivator p300, suppressing the Wnt/β-catenin pathway, and inhibits LPS induction of iNOS expression.{19784,19789}  

     

    Brand:
    Cayman
    SKU:10960 - 10 mg

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  • Bisdemethoxycurcumin (BDMC) is a natural demethoxy derivative of curcumin. It is a potent activator of macrophage phagocytosis, interacting with 1α,25-dihydroxy vitamin D3 to stimulate amyloid-β clearance by macrophages (optimal stimulation at 100 nM BDMC).{19781,19788,19791} More stable than curcumin in physiological media, BDMC suppresses proliferation in cancer cells.{19787,19792} It down-regulates the transcriptional coactivator p300, suppressing the Wnt/β-catenin pathway, and inhibits LPS induction of iNOS expression.{19784,19789}  

     

    Brand:
    Cayman
    SKU:10960 - 25 mg

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  • Bisdemethoxycurcumin (BDMC) is a natural demethoxy derivative of curcumin. It is a potent activator of macrophage phagocytosis, interacting with 1α,25-dihydroxy vitamin D3 to stimulate amyloid-β clearance by macrophages (optimal stimulation at 100 nM BDMC).{19781,19788,19791} More stable than curcumin in physiological media, BDMC suppresses proliferation in cancer cells.{19787,19792} It down-regulates the transcriptional coactivator p300, suppressing the Wnt/β-catenin pathway, and inhibits LPS induction of iNOS expression.{19784,19789}  

     

    Brand:
    Cayman
    SKU:10960 - 5 mg

    Available on backorder

  • Bisdemethoxycurcumin (BDMC) is a natural demethoxy derivative of curcumin. It is a potent activator of macrophage phagocytosis, interacting with 1α,25-dihydroxy vitamin D3 to stimulate amyloid-β clearance by macrophages (optimal stimulation at 100 nM BDMC).{19781,19788,19791} More stable than curcumin in physiological media, BDMC suppresses proliferation in cancer cells.{19787,19792} It down-regulates the transcriptional coactivator p300, suppressing the Wnt/β-catenin pathway, and inhibits LPS induction of iNOS expression.{19784,19789}  

     

    Brand:
    Cayman
    SKU:10960 - 50 mg

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  • Bisindolylmaleimide I (BIM I) is a highly selective, cell-permeable, and reversible PKC inhibitor (Ki = 14 nM) that is structurally similar to the poorly selective PKC inhibitor staurosporine (Item No. 81590).{17275} It acts as a competitive inhibitor for the ATP binding site of PKC and shows high selectivity for PKCα, β1, β2, γ, δ, and ε isozymes. BIM I directly inhibits glycogen synthase kinase 3 (GSK3) in primary adipocyte lysates (IC50 = 360 nM) and in GSK3β immunoprecipitates derived from rat epididymal adipocytes (IC50 = 170 nM).{17379} It also competitively antagonizes the serotonin (5-HT) receptor subtype 5-HT3 with a Ki value of 61 nM.{17380}  

     

    Brand:
    Cayman
    SKU:-
  • Bisindolylmaleimide I (BIM I) is a highly selective, cell-permeable, and reversible PKC inhibitor (Ki = 14 nM) that is structurally similar to the poorly selective PKC inhibitor staurosporine (Item No. 81590).{17275} It acts as a competitive inhibitor for the ATP binding site of PKC and shows high selectivity for PKCα, β1, β2, γ, δ, and ε isozymes. BIM I directly inhibits glycogen synthase kinase 3 (GSK3) in primary adipocyte lysates (IC50 = 360 nM) and in GSK3β immunoprecipitates derived from rat epididymal adipocytes (IC50 = 170 nM).{17379} It also competitively antagonizes the serotonin (5-HT) receptor subtype 5-HT3 with a Ki value of 61 nM.{17380}  

     

    Brand:
    Cayman
    SKU:-
  • Bisindolylmaleimide I (BIM I) is a highly selective, cell-permeable, and reversible PKC inhibitor (Ki = 14 nM) that is structurally similar to the poorly selective PKC inhibitor staurosporine (Item No. 81590).{17275} It acts as a competitive inhibitor for the ATP binding site of PKC and shows high selectivity for PKCα, β1, β2, γ, δ, and ε isozymes. BIM I directly inhibits glycogen synthase kinase 3 (GSK3) in primary adipocyte lysates (IC50 = 360 nM) and in GSK3β immunoprecipitates derived from rat epididymal adipocytes (IC50 = 170 nM).{17379} It also competitively antagonizes the serotonin (5-HT) receptor subtype 5-HT3 with a Ki value of 61 nM.{17380}  

     

    Brand:
    Cayman
    SKU:-
  • Bisindolylmaleimide I (BIM I) is a highly selective, cell-permeable, and reversible PKC inhibitor (Ki = 14 nM) that is structurally similar to the poorly selective PKC inhibitor staurosporine (Item No. 81590).{17275} It acts as a competitive inhibitor for the ATP binding site of PKC and shows high selectivity for PKCα, β1, β2, γ, δ, and ε isozymes. BIM I directly inhibits glycogen synthase kinase 3 (GSK3) in primary adipocyte lysates (IC50 = 360 nM) and in GSK3β immunoprecipitates derived from rat epididymal adipocytes (IC50 = 170 nM).{17379} It also competitively antagonizes the serotonin (5-HT) receptor subtype 5-HT3 with a Ki value of 61 nM.{17380}  

     

    Brand:
    Cayman
    SKU:-
  • Bisindolylmaleimide I (BIM I) is a highly selective, cell-permeable, and reversible PKC inhibitor (Ki = 14 nM) that is structurally similar to the poorly selective PKC inhibitor staurosporine (Item No. 81590).{17275} It acts as a competitive inhibitor for the ATP binding site of PKC and shows high selectivity for PKCα, β1, β2, γ, δ, and ε isozymes. BIM I directly inhibits glycogen synthase kinase 3 (GSK3) in primary adipocyte lysates (IC50 = 360 nM) and in GSK3β immunoprecipitates derived from rat epididymal adipocytes (IC50 = 170 nM).{17379} It also competitively antagonizes the serotonin (5-HT) receptor subtype 5-HT3 with a Ki value of 61 nM.{17380}  

     

    Brand:
    Cayman
    SKU:21180 -

    Out of stock

  • Bisindolylmaleimide I (BIM I) is a highly selective, cell-permeable, and reversible PKC inhibitor (Ki = 14 nM) that is structurally similar to the poorly selective PKC inhibitor staurosporine (Item No. 81590).{17275} It acts as a competitive inhibitor for the ATP binding site of PKC and shows high selectivity for PKCα, β1, β2, γ, δ, and ε isozymes. BIM I directly inhibits glycogen synthase kinase 3 (GSK3) in primary adipocyte lysates (IC50 = 360 nM) and in GSK3β immunoprecipitates derived from rat epididymal adipocytes (IC50 = 170 nM).{17379} It also competitively antagonizes the serotonin (5-HT) receptor subtype 5-HT3 with a Ki value of 61 nM.{17380}  

     

    Brand:
    Cayman
    SKU:21180 -

    Out of stock

  • Bisindolylmaleimide I (BIM I) is a highly selective, cell-permeable, and reversible PKC inhibitor (Ki = 14 nM) that is structurally similar to the poorly selective PKC inhibitor staurosporine (Item No. 81590).{17275} It acts as a competitive inhibitor for the ATP binding site of PKC and shows high selectivity for PKCα, β1, β2, γ, δ, and ε isozymes. BIM I directly inhibits glycogen synthase kinase 3 (GSK3) in primary adipocyte lysates (IC50 = 360 nM) and in GSK3β immunoprecipitates derived from rat epididymal adipocytes (IC50 = 170 nM).{17379} It also competitively antagonizes the serotonin (5-HT) receptor subtype 5-HT3 with a Ki value of 61 nM.{17380}  

     

    Brand:
    Cayman
    SKU:21180 -

    Out of stock

  • Bisindolylmaleimide II (BIM II) is a general inhibitor of all protein kinase C (PKC) subtypes with structural similarity to the nonspecific PKC inhibitor staurosporine.{17276,17275} At 10 μM, BIM II inhibits 98% of PKCα kinase activity.{20731} Additionally, it inhibits PDK1 (IC50 = 14 μM), an important kinase in the insulin signaling pathway, and PKA (IC50 = 2.94 μM).{20731,20730} Studies of structure-activity relationships of BIM II in complex with PDK1 and PKA kinase binding domains has led to useful insights into kinase/ligand binding for the rational design of inhibitors as potential therapeutic agents.{20731,20730}  

     

    Brand:
    Cayman
    SKU:11020 - 1 mg

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  • Bisindolylmaleimide II (BIM II) is a general inhibitor of all protein kinase C (PKC) subtypes with structural similarity to the nonspecific PKC inhibitor staurosporine.{17276,17275} At 10 μM, BIM II inhibits 98% of PKCα kinase activity.{20731} Additionally, it inhibits PDK1 (IC50 = 14 μM), an important kinase in the insulin signaling pathway, and PKA (IC50 = 2.94 μM).{20731,20730} Studies of structure-activity relationships of BIM II in complex with PDK1 and PKA kinase binding domains has led to useful insights into kinase/ligand binding for the rational design of inhibitors as potential therapeutic agents.{20731,20730}  

     

    Brand:
    Cayman
    SKU:11020 - 5 mg

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  • Bisindolylmaleimide III was developed as a protein kinase C (PKC) inhibitor with structural similarity to the nonspecific PKC inhibitor staurosporine.{17276,17275} At 1 μM, bisindolylmaleimide III inhibits 93% of PKCα kinase activity and also inhibits many other protein kinases including, S6K1, MAPKAP-K1, RSK2 and MSK1 with similar potency.{12847} Additionally, it inhibits PDK1, an important kinase in the insulin signaling pathway, with an IC50 value of 3.8 μM.  

     

    Brand:
    Cayman
    SKU:11072 - 1 mg

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  • Bisindolylmaleimide III was developed as a protein kinase C (PKC) inhibitor with structural similarity to the nonspecific PKC inhibitor staurosporine.{17276,17275} At 1 μM, bisindolylmaleimide III inhibits 93% of PKCα kinase activity and also inhibits many other protein kinases including, S6K1, MAPKAP-K1, RSK2 and MSK1 with similar potency.{12847} Additionally, it inhibits PDK1, an important kinase in the insulin signaling pathway, with an IC50 value of 3.8 μM.  

     

    Brand:
    Cayman
    SKU:11072 - 5 mg

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  • Bisindolylmaleimide IV (BIM IV) is a cell permeable inhibitor of protein kinase C (PKC) with IC50 values reported to range from 0.10 to 0.55 µM.{17276,17275,17277,17278} BIM IV was designed to be more discriminative than its parent compound, the non-selective PKC inhibitor, staurosporine (Item No. 81590). However, BIM IV also inhibits protein kinase A with IC50 values ranging from 2 to 11.8 µM.{17276,17275}  

     

    Brand:
    Cayman
    SKU:-
  • Bisindolylmaleimide IV (BIM IV) is a cell permeable inhibitor of protein kinase C (PKC) with IC50 values reported to range from 0.10 to 0.55 µM.{17276,17275,17277,17278} BIM IV was designed to be more discriminative than its parent compound, the non-selective PKC inhibitor, staurosporine (Item No. 81590). However, BIM IV also inhibits protein kinase A with IC50 values ranging from 2 to 11.8 µM.{17276,17275}  

     

    Brand:
    Cayman
    SKU:-
  • Bisindolylmaleimide IV (BIM IV) is a cell permeable inhibitor of protein kinase C (PKC) with IC50 values reported to range from 0.10 to 0.55 µM.{17276,17275,17277,17278} BIM IV was designed to be more discriminative than its parent compound, the non-selective PKC inhibitor, staurosporine (Item No. 81590). However, BIM IV also inhibits protein kinase A with IC50 values ranging from 2 to 11.8 µM.{17276,17275}  

     

    Brand:
    Cayman
    SKU:-
  • Bisindolylmaleimide IV (BIM IV) is a cell permeable inhibitor of protein kinase C (PKC) with IC50 values reported to range from 0.10 to 0.55 µM.{17276,17275,17277,17278} BIM IV was designed to be more discriminative than its parent compound, the non-selective PKC inhibitor, staurosporine (Item No. 81590). However, BIM IV also inhibits protein kinase A with IC50 values ranging from 2 to 11.8 µM.{17276,17275}  

     

    Brand:
    Cayman
    SKU:-
  • Bisindolylmaleimide IX (BIM IX) is a potent, cell-permeable inhibitor of protein kinase C (PKC) isoforms (IC50 = 5, 24, 14, 27, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively).{17342} It is a poor inhibitor of protein kinase A (PKA, IC50 = 0.9 μM) and calcium/calmodulin kinase II (IC50 = 17 μM). BIM IX also inhibits glycogen synthase kinase 3 (IC50 = 6.8 nM).{17379}  

     

    Brand:
    Cayman
    SKU:-
  • Bisindolylmaleimide IX (BIM IX) is a potent, cell-permeable inhibitor of protein kinase C (PKC) isoforms (IC50 = 5, 24, 14, 27, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively).{17342} It is a poor inhibitor of protein kinase A (PKA, IC50 = 0.9 μM) and calcium/calmodulin kinase II (IC50 = 17 μM). BIM IX also inhibits glycogen synthase kinase 3 (IC50 = 6.8 nM).{17379}  

     

    Brand:
    Cayman
    SKU:-
  • Bisindolylmaleimide IX (BIM IX) is a potent, cell-permeable inhibitor of protein kinase C (PKC) isoforms (IC50 = 5, 24, 14, 27, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively).{17342} It is a poor inhibitor of protein kinase A (PKA, IC50 = 0.9 μM) and calcium/calmodulin kinase II (IC50 = 17 μM). BIM IX also inhibits glycogen synthase kinase 3 (IC50 = 6.8 nM).{17379}  

     

    Brand:
    Cayman
    SKU:-
  • Bisindolylmaleimide V (BIM V) is a weak inhibitor of protein kinase C (PKC) demonstrating an IC50 value >100 µM.{17278,17275,17276} While effectively inactive as a PKC inhibitor, BIM V blocks the activation of mitogen-stimulated protein kinase p70s6k/p85s6k (S6K) in vivo with an IC50 value of 8 µM.{17279}  

     

    Brand:
    Cayman
    SKU:-
  • Bisindolylmaleimide V (BIM V) is a weak inhibitor of protein kinase C (PKC) demonstrating an IC50 value >100 µM.{17278,17275,17276} While effectively inactive as a PKC inhibitor, BIM V blocks the activation of mitogen-stimulated protein kinase p70s6k/p85s6k (S6K) in vivo with an IC50 value of 8 µM.{17279}  

     

    Brand:
    Cayman
    SKU:-
  • Bisindolylmaleimide V (BIM V) is a weak inhibitor of protein kinase C (PKC) demonstrating an IC50 value >100 µM.{17278,17275,17276} While effectively inactive as a PKC inhibitor, BIM V blocks the activation of mitogen-stimulated protein kinase p70s6k/p85s6k (S6K) in vivo with an IC50 value of 8 µM.{17279}  

     

    Brand:
    Cayman
    SKU:-
  • Bisindolylmaleimide V (BIM V) is a weak inhibitor of protein kinase C (PKC) demonstrating an IC50 value >100 µM.{17278,17275,17276} While effectively inactive as a PKC inhibitor, BIM V blocks the activation of mitogen-stimulated protein kinase p70s6k/p85s6k (S6K) in vivo with an IC50 value of 8 µM.{17279}  

     

    Brand:
    Cayman
    SKU:-
  • Bisindolylmaleimide VIII (BIM VIII) is a selective protein kinase C (PKC) inhibitor (IC50 = 158 nM for rat brain PKC) that acts at the ATP binding site of PKC.{17342,17339} This compound exhibits some degree of PKC isozyme specificity with preference for PKCα over PKCβI, PKCβII, PKCγ, or PKCε (IC50s = 53, 195, 163, 213, and 175 nM, respectively).{17342} At 10 µM BIM VIII does not inhibit the tyrosine phosphorylation or the activation of phospholipase C γ1.{17340} BIM VIII inhibits carbachol-evoked noradrenaline release from human SH-SY5Y neuroblastoma cells with an IC50 value of 600 nM.{17341}  

     

    Brand:
    Cayman
    SKU:-
  • Bisindolylmaleimide VIII (BIM VIII) is a selective protein kinase C (PKC) inhibitor (IC50 = 158 nM for rat brain PKC) that acts at the ATP binding site of PKC.{17342,17339} This compound exhibits some degree of PKC isozyme specificity with preference for PKCα over PKCβI, PKCβII, PKCγ, or PKCε (IC50s = 53, 195, 163, 213, and 175 nM, respectively).{17342} At 10 µM BIM VIII does not inhibit the tyrosine phosphorylation or the activation of phospholipase C γ1.{17340} BIM VIII inhibits carbachol-evoked noradrenaline release from human SH-SY5Y neuroblastoma cells with an IC50 value of 600 nM.{17341}  

     

    Brand:
    Cayman
    SKU:-
  • Bisindolylmaleimide VIII (BIM VIII) is a selective protein kinase C (PKC) inhibitor (IC50 = 158 nM for rat brain PKC) that acts at the ATP binding site of PKC.{17342,17339} This compound exhibits some degree of PKC isozyme specificity with preference for PKCα over PKCβI, PKCβII, PKCγ, or PKCε (IC50s = 53, 195, 163, 213, and 175 nM, respectively).{17342} At 10 µM BIM VIII does not inhibit the tyrosine phosphorylation or the activation of phospholipase C γ1.{17340} BIM VIII inhibits carbachol-evoked noradrenaline release from human SH-SY5Y neuroblastoma cells with an IC50 value of 600 nM.{17341}  

     

    Brand:
    Cayman
    SKU:-
  • Bisindolylmaleimide X is a cell-permeable, reversible, ATP-competitive protein kinase C (PKC) inhibitor (IC50 = 15 nM, rat brain PKC).{17342} It has been shown to inhibit PKCα, βI, βII, γ, and ε with IC50 values of 8, 8, 14, 13, and 39 nM, respectively.{17342} It has also been identified as an inhibitor of Cdk2 (IC50 = 200 nM) and GSK3α/β.{28472} This compound has been used to activate mesenchymal stem cells, increase the surface expression of homing ligands that bind to intercellular adhesion molecule 1, and target delivery of these cells to sites of inflammation.{28473}  

     

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    Cayman
    SKU:-

    Available on backorder

  • Bisindolylmaleimide X is a cell-permeable, reversible, ATP-competitive protein kinase C (PKC) inhibitor (IC50 = 15 nM, rat brain PKC).{17342} It has been shown to inhibit PKCα, βI, βII, γ, and ε with IC50 values of 8, 8, 14, 13, and 39 nM, respectively.{17342} It has also been identified as an inhibitor of Cdk2 (IC50 = 200 nM) and GSK3α/β.{28472} This compound has been used to activate mesenchymal stem cells, increase the surface expression of homing ligands that bind to intercellular adhesion molecule 1, and target delivery of these cells to sites of inflammation.{28473}  

     

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    Cayman
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  • Bisindolylmaleimide XI (BIM XI) is a selective, cell-permeable protein kinase C (PKC) inhibitor that displays 10-fold greater selectivity for PKCα (IC50 = 9 nM) and 4-fold greater selectivity for PKCβI (IC50 = 28 nM) over Ca2+-independent PKCε (IC50 = 108 nM).{17342} Inhibition of PKCα by BIM XI and other similar PKC inhibitors has been associated with enhanced cardiac contractility and protection from heart failure.{20732} BIM XI prevents T-cell activation and proliferation (with IC50s ranging from 30-150 nM) associated with chronic inflammatory responses in vivo.{20748}  

     

    Brand:
    Cayman
    SKU:11073 - 1 mg

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  • Bisindolylmaleimide XI (BIM XI) is a selective, cell-permeable protein kinase C (PKC) inhibitor that displays 10-fold greater selectivity for PKCα (IC50 = 9 nM) and 4-fold greater selectivity for PKCβI (IC50 = 28 nM) over Ca2+-independent PKCε (IC50 = 108 nM).{17342} Inhibition of PKCα by BIM XI and other similar PKC inhibitors has been associated with enhanced cardiac contractility and protection from heart failure.{20732} BIM XI prevents T-cell activation and proliferation (with IC50s ranging from 30-150 nM) associated with chronic inflammatory responses in vivo.{20748}  

     

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    Cayman
    SKU:11073 - 5 mg

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  • Bisoprolol is a potent β-adrenergic receptor (β-AR) antagonist that is selective for β1-ARs over β2-ARs (Kis = 25 and 480 nM, respectively in S49 cells overexpressing the human receptors).{39505} It also selectively binds to β1-ARs over β2-ARs in human myocardium (Kis = 75.8 and 991 nM, respectively).{39506} Bisoprolol binds to rat ventricular myocytes and heart membrane (Kis = 20 and 38.1 nM, respectively) and to rat β1-AR in salivary glands and β2-AR in reticulocytes (Kis = 24 and 1,945 nM, respectively).{39507,39508} In vivo, it inhibits increases in heart rate induced by isoproterenol (Item No. 15592) in guinea pigs.{39509} Bisoprolol (0.3 mg/kg) inhibits isoproterenol-induced increases in heart rate and myocardial contractility in conscious dogs. It also decreases blood pressure and heart rate in spontaneously hypertensive rats (SHRs) when chronically administered at a dose of 7.5 mg/kg twice per day over 19 weeks. Formulations containing bisoprolol have been used in the treatment of heart failure, angina pectoris, mild to moderate hypertension, and for secondary prevention of myocardial infarction.  

     

    Brand:
    Cayman
    SKU:23827 - 100 mg

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  • Bisoprolol is a potent β-adrenergic receptor (β-AR) antagonist that is selective for β1-ARs over β2-ARs (Kis = 25 and 480 nM, respectively in S49 cells overexpressing the human receptors).{39505} It also selectively binds to β1-ARs over β2-ARs in human myocardium (Kis = 75.8 and 991 nM, respectively).{39506} Bisoprolol binds to rat ventricular myocytes and heart membrane (Kis = 20 and 38.1 nM, respectively) and to rat β1-AR in salivary glands and β2-AR in reticulocytes (Kis = 24 and 1,945 nM, respectively).{39507,39508} In vivo, it inhibits increases in heart rate induced by isoproterenol (Item No. 15592) in guinea pigs.{39509} Bisoprolol (0.3 mg/kg) inhibits isoproterenol-induced increases in heart rate and myocardial contractility in conscious dogs. It also decreases blood pressure and heart rate in spontaneously hypertensive rats (SHRs) when chronically administered at a dose of 7.5 mg/kg twice per day over 19 weeks. Formulations containing bisoprolol have been used in the treatment of heart failure, angina pectoris, mild to moderate hypertension, and for secondary prevention of myocardial infarction.  

     

    Brand:
    Cayman
    SKU:23827 - 250 mg

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  • Bisoprolol is a potent β-adrenergic receptor (β-AR) antagonist that is selective for β1-ARs over β2-ARs (Kis = 25 and 480 nM, respectively in S49 cells overexpressing the human receptors).{39505} It also selectively binds to β1-ARs over β2-ARs in human myocardium (Kis = 75.8 and 991 nM, respectively).{39506} Bisoprolol binds to rat ventricular myocytes and heart membrane (Kis = 20 and 38.1 nM, respectively) and to rat β1-AR in salivary glands and β2-AR in reticulocytes (Kis = 24 and 1,945 nM, respectively).{39507,39508} In vivo, it inhibits increases in heart rate induced by isoproterenol (Item No. 15592) in guinea pigs.{39509} Bisoprolol (0.3 mg/kg) inhibits isoproterenol-induced increases in heart rate and myocardial contractility in conscious dogs. It also decreases blood pressure and heart rate in spontaneously hypertensive rats (SHRs) when chronically administered at a dose of 7.5 mg/kg twice per day over 19 weeks. Formulations containing bisoprolol have been used in the treatment of heart failure, angina pectoris, mild to moderate hypertension, and for secondary prevention of myocardial infarction.  

     

    Brand:
    Cayman
    SKU:23827 - 50 mg

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  • Bitertanol is a broad-spectrum triazole fungicide that is active against a variety of fungi, including V. inaequalis and V. pirina, which are responsible for apple and pear scab, respectively, as well as S. mors-uvae and P. ribis, which are responsible for American gooseberry mildew and leaf spot in black currants, respectively.{39670} It is active against isolates of V. inaequalis (MICs = 0.6 and 1 µg/ml) but repeated use leads to resistance and cross-resistance (MICs = 9.8-13 µg/ml for bitertanol-resistant isolates).{39671} Bitertanol inhibits the cytochrome P450 (CYP450) isoform CYP3A4 (IC50 = 2.74 µM) and inhibits androgenic activity induced by the androgen receptor agonist DHT (Item No. 15874) in a yeast two-hybrid assay (IC50 = 79.85 µM).{39672} In rats, bitertanol (10-300 mg/kg, i.p.) increases operant responding on one- and five-minute fixed interval schedules with no effect on motor activity.{39673}  

     

    Brand:
    Cayman
    SKU:24054 - 25 mg

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  • Bitertanol is a broad-spectrum triazole fungicide that is active against a variety of fungi, including V. inaequalis and V. pirina, which are responsible for apple and pear scab, respectively, as well as S. mors-uvae and P. ribis, which are responsible for American gooseberry mildew and leaf spot in black currants, respectively.{39670} It is active against isolates of V. inaequalis (MICs = 0.6 and 1 µg/ml) but repeated use leads to resistance and cross-resistance (MICs = 9.8-13 µg/ml for bitertanol-resistant isolates).{39671} Bitertanol inhibits the cytochrome P450 (CYP450) isoform CYP3A4 (IC50 = 2.74 µM) and inhibits androgenic activity induced by the androgen receptor agonist DHT (Item No. 15874) in a yeast two-hybrid assay (IC50 = 79.85 µM).{39672} In rats, bitertanol (10-300 mg/kg, i.p.) increases operant responding on one- and five-minute fixed interval schedules with no effect on motor activity.{39673}  

     

    Brand:
    Cayman
    SKU:24054 - 50 mg

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  • Bithionol is an anthelmintic drug. Formulations containing bithionol have demonstrated efficacy against cestodes and trematodes, as well as other parasitic worms.{34401,34402,34403} Bithionol inhibits host caspases, including caspases-1, -3, -6, -7, and -9, which act as hub proteins that mediate the lethality of multiple pathogenic agents.{34404} By blocking host caspases, bithionol reduces the detrimental effects of anthrax lethal toxin, diphtheria toxin, cholera toxin, P. aeruginosa exotoxin A, Botulinum neurotoxin, ricin, and Zika virus.{34404} Bithionol also inhibits NF-κB activation by blocking phosphorylation of IκBα (IC50 = 15.8 µM in a reporter gene assay).{31081}  

     

    Brand:
    Cayman
    SKU:21844 -

    Out of stock

  • Bithionol is an anthelmintic drug. Formulations containing bithionol have demonstrated efficacy against cestodes and trematodes, as well as other parasitic worms.{34401,34402,34403} Bithionol inhibits host caspases, including caspases-1, -3, -6, -7, and -9, which act as hub proteins that mediate the lethality of multiple pathogenic agents.{34404} By blocking host caspases, bithionol reduces the detrimental effects of anthrax lethal toxin, diphtheria toxin, cholera toxin, P. aeruginosa exotoxin A, Botulinum neurotoxin, ricin, and Zika virus.{34404} Bithionol also inhibits NF-κB activation by blocking phosphorylation of IκBα (IC50 = 15.8 µM in a reporter gene assay).{31081}  

     

    Brand:
    Cayman
    SKU:21844 -

    Out of stock

  • Bithionol is an anthelmintic drug. Formulations containing bithionol have demonstrated efficacy against cestodes and trematodes, as well as other parasitic worms.{34401,34402,34403} Bithionol inhibits host caspases, including caspases-1, -3, -6, -7, and -9, which act as hub proteins that mediate the lethality of multiple pathogenic agents.{34404} By blocking host caspases, bithionol reduces the detrimental effects of anthrax lethal toxin, diphtheria toxin, cholera toxin, P. aeruginosa exotoxin A, Botulinum neurotoxin, ricin, and Zika virus.{34404} Bithionol also inhibits NF-κB activation by blocking phosphorylation of IκBα (IC50 = 15.8 µM in a reporter gene assay).{31081}  

     

    Brand:
    Cayman
    SKU:21844 -

    Out of stock

  • Bithionol is an anthelmintic drug. Formulations containing bithionol have demonstrated efficacy against cestodes and trematodes, as well as other parasitic worms.{34401,34402,34403} Bithionol inhibits host caspases, including caspases-1, -3, -6, -7, and -9, which act as hub proteins that mediate the lethality of multiple pathogenic agents.{34404} By blocking host caspases, bithionol reduces the detrimental effects of anthrax lethal toxin, diphtheria toxin, cholera toxin, P. aeruginosa exotoxin A, Botulinum neurotoxin, ricin, and Zika virus.{34404} Bithionol also inhibits NF-κB activation by blocking phosphorylation of IκBα (IC50 = 15.8 µM in a reporter gene assay).{31081}  

     

    Brand:
    Cayman
    SKU:21844 -

    Out of stock

  • Bitopertin is an inhibitor of the glycine transporter 1 (GlyT1; IC50 = 30 nM) that increases levels of glycine by inhibiting its reuptake.{33096} It is selective for GlyT1, inhibiting GlyT2 and off-target ERG channels with IC50 values of >30 and 17 µM, respectively.{33096} Bitopertin was examined in clinical trials on persistent negative symptoms associated with schizophrenia but failed to meet the primary endpoints set forth in these studies.{33097}  

     

    Brand:
    Cayman
    SKU:19896 -

    Available on backorder

  • Bitopertin is an inhibitor of the glycine transporter 1 (GlyT1; IC50 = 30 nM) that increases levels of glycine by inhibiting its reuptake.{33096} It is selective for GlyT1, inhibiting GlyT2 and off-target ERG channels with IC50 values of >30 and 17 µM, respectively.{33096} Bitopertin was examined in clinical trials on persistent negative symptoms associated with schizophrenia but failed to meet the primary endpoints set forth in these studies.{33097}  

     

    Brand:
    Cayman
    SKU:19896 -

    Available on backorder

  • Bitopertin is an inhibitor of the glycine transporter 1 (GlyT1; IC50 = 30 nM) that increases levels of glycine by inhibiting its reuptake.{33096} It is selective for GlyT1, inhibiting GlyT2 and off-target ERG channels with IC50 values of >30 and 17 µM, respectively.{33096} Bitopertin was examined in clinical trials on persistent negative symptoms associated with schizophrenia but failed to meet the primary endpoints set forth in these studies.{33097}  

     

    Brand:
    Cayman
    SKU:19896 -

    Available on backorder

  • Bitopertin is an inhibitor of the glycine transporter 1 (GlyT1; IC50 = 30 nM) that increases levels of glycine by inhibiting its reuptake.{33096} It is selective for GlyT1, inhibiting GlyT2 and off-target ERG channels with IC50 values of >30 and 17 µM, respectively.{33096} Bitopertin was examined in clinical trials on persistent negative symptoms associated with schizophrenia but failed to meet the primary endpoints set forth in these studies.{33097}  

     

    Brand:
    Cayman
    SKU:19896 -

    Available on backorder

  • Bivalirudin is an inhibitor of α- and ζ-thrombin (Kis = 2.56 and 1.84 nM, respectively), enzymes that exhibit high fibrinogen-clotting activities.{36230} It is selective for α- and ζ-thrombin, lacking activity at trypsin and γ-thrombin, which lacks clotting activity, at a >1,000-fold excess of bivalirudin. Bivalirudin inhibits α-thrombin-stimulated activation of the clotting factors Factor X, Factor V, and prothrombin in contact-activated plasma at a concentration of 0.1 μM.{36231} Administration of bivalirudin (0.5-1.5 mg/kg, i.v.) reduces platelet deposition in a rat carotid endarterectomy model in a dose-dependent manner.{36232} Formulations containing bivalirudin have been used to prevent ischemic events during angioplasty for thrombus-containing lesions.{36233}  

     

    Brand:
    Cayman
    SKU:23035 - 10 mg

    Available on backorder

  • Bivalirudin is an inhibitor of α- and ζ-thrombin (Kis = 2.56 and 1.84 nM, respectively), enzymes that exhibit high fibrinogen-clotting activities.{36230} It is selective for α- and ζ-thrombin, lacking activity at trypsin and γ-thrombin, which lacks clotting activity, at a >1,000-fold excess of bivalirudin. Bivalirudin inhibits α-thrombin-stimulated activation of the clotting factors Factor X, Factor V, and prothrombin in contact-activated plasma at a concentration of 0.1 μM.{36231} Administration of bivalirudin (0.5-1.5 mg/kg, i.v.) reduces platelet deposition in a rat carotid endarterectomy model in a dose-dependent manner.{36232} Formulations containing bivalirudin have been used to prevent ischemic events during angioplasty for thrombus-containing lesions.{36233}  

     

    Brand:
    Cayman
    SKU:23035 - 25 mg

    Available on backorder

  • Bivalirudin is an inhibitor of α- and ζ-thrombin (Kis = 2.56 and 1.84 nM, respectively), enzymes that exhibit high fibrinogen-clotting activities.{36230} It is selective for α- and ζ-thrombin, lacking activity at trypsin and γ-thrombin, which lacks clotting activity, at a >1,000-fold excess of bivalirudin. Bivalirudin inhibits α-thrombin-stimulated activation of the clotting factors Factor X, Factor V, and prothrombin in contact-activated plasma at a concentration of 0.1 μM.{36231} Administration of bivalirudin (0.5-1.5 mg/kg, i.v.) reduces platelet deposition in a rat carotid endarterectomy model in a dose-dependent manner.{36232} Formulations containing bivalirudin have been used to prevent ischemic events during angioplasty for thrombus-containing lesions.{36233}  

     

    Brand:
    Cayman
    SKU:23035 - 5 mg

    Available on backorder

  • Bivalirudin is an inhibitor of α- and ζ-thrombin (Kis = 2.56 and 1.84 nM, respectively), enzymes that exhibit high fibrinogen-clotting activities.{36230} It is selective for α- and ζ-thrombin, lacking activity at trypsin and γ-thrombin, which lacks clotting activity, at a >1,000-fold excess of bivalirudin. Bivalirudin inhibits α-thrombin-stimulated activation of the clotting factors Factor X, Factor V, and prothrombin in contact-activated plasma at a concentration of 0.1 μM.{36231} Administration of bivalirudin (0.5-1.5 mg/kg, i.v.) reduces platelet deposition in a rat carotid endarterectomy model in a dose-dependent manner.{36232} Formulations containing bivalirudin have been used to prevent ischemic events during angioplasty for thrombus-containing lesions.{36233}  

     

    Brand:
    Cayman
    SKU:23035 - 50 mg

    Available on backorder

  • The 90 kDa ribosomal S6 kinases (RSKs) are a group of serine/threonine kinases involved in diverse cellular processes, including growth, survival, and motility. Phosphorylation of the sodium-hydrogen exchanger (NHE) in cardiac tissue by RSK has been shown to activate NHE during cellular stresses, such as myocardial infarction, as a mechanism to maintain pH. BIX 02565 is a RSK2 inhibitor with an IC50 value of 1.1 nM.{30925,30924} It also demonstrates off-target binding at multiple adrenergic receptor subtypes that are important for vascular tone and cardiac function (IC50s = 0.052-1.820 μM for adrenergic α1A, α1B, α1D, α2A, β2, and imidazoline I2 receptors.{30925,30924} BIX 02565 can also inhibit LRRK2 and PRKD1 with IC50 values of 16 and 35 nM, respectively).{30925} In rats, BIX 02565 at 1, 3, and 10 mg/kg was shown to significantly decrease heart rate and mean arterial pressure.{30924}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • The 90 kDa ribosomal S6 kinases (RSKs) are a group of serine/threonine kinases involved in diverse cellular processes, including growth, survival, and motility. Phosphorylation of the sodium-hydrogen exchanger (NHE) in cardiac tissue by RSK has been shown to activate NHE during cellular stresses, such as myocardial infarction, as a mechanism to maintain pH. BIX 02565 is a RSK2 inhibitor with an IC50 value of 1.1 nM.{30925,30924} It also demonstrates off-target binding at multiple adrenergic receptor subtypes that are important for vascular tone and cardiac function (IC50s = 0.052-1.820 μM for adrenergic α1A, α1B, α1D, α2A, β2, and imidazoline I2 receptors.{30925,30924} BIX 02565 can also inhibit LRRK2 and PRKD1 with IC50 values of 16 and 35 nM, respectively).{30925} In rats, BIX 02565 at 1, 3, and 10 mg/kg was shown to significantly decrease heart rate and mean arterial pressure.{30924}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • The 90 kDa ribosomal S6 kinases (RSKs) are a group of serine/threonine kinases involved in diverse cellular processes, including growth, survival, and motility. Phosphorylation of the sodium-hydrogen exchanger (NHE) in cardiac tissue by RSK has been shown to activate NHE during cellular stresses, such as myocardial infarction, as a mechanism to maintain pH. BIX 02565 is a RSK2 inhibitor with an IC50 value of 1.1 nM.{30925,30924} It also demonstrates off-target binding at multiple adrenergic receptor subtypes that are important for vascular tone and cardiac function (IC50s = 0.052-1.820 μM for adrenergic α1A, α1B, α1D, α2A, β2, and imidazoline I2 receptors.{30925,30924} BIX 02565 can also inhibit LRRK2 and PRKD1 with IC50 values of 16 and 35 nM, respectively).{30925} In rats, BIX 02565 at 1, 3, and 10 mg/kg was shown to significantly decrease heart rate and mean arterial pressure.{30924}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} BIX01294 (hydrochloride hydrate) is a selective inhibitor of G9a HMTase (IC50 = 1.7 μM).{17550} It less effectively inhibits the HMTase G9a-like protein (GLP; IC50 = 38 μM) and has no effect on other known HMTases.{17550} BIX01294 has been used in combination with the calcium channel activator BayK8644 to facilitate the generation of induced pluripotent stem cells from somatic cells in vitro.{17549}  

     

    Brand:
    Cayman
    SKU:-
  • The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} BIX01294 (hydrochloride hydrate) is a selective inhibitor of G9a HMTase (IC50 = 1.7 μM).{17550} It less effectively inhibits the HMTase G9a-like protein (GLP; IC50 = 38 μM) and has no effect on other known HMTases.{17550} BIX01294 has been used in combination with the calcium channel activator BayK8644 to facilitate the generation of induced pluripotent stem cells from somatic cells in vitro.{17549}  

     

    Brand:
    Cayman
    SKU:-
  • The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} BIX01294 (hydrochloride hydrate) is a selective inhibitor of G9a HMTase (IC50 = 1.7 μM).{17550} It less effectively inhibits the HMTase G9a-like protein (GLP; IC50 = 38 μM) and has no effect on other known HMTases.{17550} BIX01294 has been used in combination with the calcium channel activator BayK8644 to facilitate the generation of induced pluripotent stem cells from somatic cells in vitro.{17549}  

     

    Brand:
    Cayman
    SKU:-
  • The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.{17548,17546,17547} BIX01294 (hydrochloride hydrate) is a selective inhibitor of G9a HMTase (IC50 = 1.7 μM).{17550} It less effectively inhibits the HMTase G9a-like protein (GLP; IC50 = 38 μM) and has no effect on other known HMTases.{17550} BIX01294 has been used in combination with the calcium channel activator BayK8644 to facilitate the generation of induced pluripotent stem cells from somatic cells in vitro.{17549}  

     

    Brand:
    Cayman
    SKU:-
  • BIX02188 is a potent inhibitor of MEK5 (IC50 = 4.3 nM) with reduced activity towards inhibition of ERK5 and TGFβR1 (IC50s = 810 and 1,800 nM, respectively).{27914} It does not inhibit the closely related kinases MEK1, MEK2, ERK2, and JNK2 (IC50s = > 6,300 nM).{27914} BIX02188 inhibits phosphorylation of ERK5 in a dose-dependent manner without affecting phosphorylation of ERK1/2, p38 MAPK, or JNK1/2.{27914}  

     

    Brand:
    Cayman
    SKU:-
  • BIX02188 is a potent inhibitor of MEK5 (IC50 = 4.3 nM) with reduced activity towards inhibition of ERK5 and TGFβR1 (IC50s = 810 and 1,800 nM, respectively).{27914} It does not inhibit the closely related kinases MEK1, MEK2, ERK2, and JNK2 (IC50s = > 6,300 nM).{27914} BIX02188 inhibits phosphorylation of ERK5 in a dose-dependent manner without affecting phosphorylation of ERK1/2, p38 MAPK, or JNK1/2.{27914}  

     

    Brand:
    Cayman
    SKU:-
  • BIX02188 is a potent inhibitor of MEK5 (IC50 = 4.3 nM) with reduced activity towards inhibition of ERK5 and TGFβR1 (IC50s = 810 and 1,800 nM, respectively).{27914} It does not inhibit the closely related kinases MEK1, MEK2, ERK2, and JNK2 (IC50s = > 6,300 nM).{27914} BIX02188 inhibits phosphorylation of ERK5 in a dose-dependent manner without affecting phosphorylation of ERK1/2, p38 MAPK, or JNK1/2.{27914}  

     

    Brand:
    Cayman
    SKU:-
  • BIX02188 is a potent inhibitor of MEK5 (IC50 = 4.3 nM) with reduced activity towards inhibition of ERK5 and TGFβR1 (IC50s = 810 and 1,800 nM, respectively).{27914} It does not inhibit the closely related kinases MEK1, MEK2, ERK2, and JNK2 (IC50s = > 6,300 nM).{27914} BIX02188 inhibits phosphorylation of ERK5 in a dose-dependent manner without affecting phosphorylation of ERK1/2, p38 MAPK, or JNK1/2.{27914}  

     

    Brand:
    Cayman
    SKU:-
  • MEK5, also known as MAP2K5, phosphorylates ERK5 (MAPK7) in signaling pathways involved in stress-induced apoptosis, neuronal survival, cardiac development, and angiogenesis.{15424,27915} BIX02189 is a potent inhibitor of both MEK5 and ERK5 (IC50s = 1.5 and 59 nM, respectively), preventing transcriptional activation of the downstream target MEF2C.{27914} It minimally inhibits a panel of related kinases, including MEK1/2 and ERK1/2.{27914} BIX02189 blocks sorbitol-induced phosphorylation of ERK5, without affecting phosphorylation of ERK1/2, in HeLa cells.{27914} It has been used to investigate the roles of MEK5/ERK5 signaling in nerve growth factor-mediated neurite outgrowth and myeloid cell differentiation.{27915,27913}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • MEK5, also known as MAP2K5, phosphorylates ERK5 (MAPK7) in signaling pathways involved in stress-induced apoptosis, neuronal survival, cardiac development, and angiogenesis.{15424,27915} BIX02189 is a potent inhibitor of both MEK5 and ERK5 (IC50s = 1.5 and 59 nM, respectively), preventing transcriptional activation of the downstream target MEF2C.{27914} It minimally inhibits a panel of related kinases, including MEK1/2 and ERK1/2.{27914} BIX02189 blocks sorbitol-induced phosphorylation of ERK5, without affecting phosphorylation of ERK1/2, in HeLa cells.{27914} It has been used to investigate the roles of MEK5/ERK5 signaling in nerve growth factor-mediated neurite outgrowth and myeloid cell differentiation.{27915,27913}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • MEK5, also known as MAP2K5, phosphorylates ERK5 (MAPK7) in signaling pathways involved in stress-induced apoptosis, neuronal survival, cardiac development, and angiogenesis.{15424,27915} BIX02189 is a potent inhibitor of both MEK5 and ERK5 (IC50s = 1.5 and 59 nM, respectively), preventing transcriptional activation of the downstream target MEF2C.{27914} It minimally inhibits a panel of related kinases, including MEK1/2 and ERK1/2.{27914} BIX02189 blocks sorbitol-induced phosphorylation of ERK5, without affecting phosphorylation of ERK1/2, in HeLa cells.{27914} It has been used to investigate the roles of MEK5/ERK5 signaling in nerve growth factor-mediated neurite outgrowth and myeloid cell differentiation.{27915,27913}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Bizine is a phenelzine analog that inhibits lysine-specific demethylase 1 (LSD1; Ki(inact) = 59 nM).{32531} It is 23-fold, 63-fold, and >100-fold selective for LSD-1 over monoamine oxidase (MAO) A, MAOB, and LSD2, respectively.{32531} Bizine has been shown to induce bulk histone H3 lysine 4 dimethylation in LNCaP cancer cells (EC50 = ~2 µM) and, at 0.5 µM, to protect neurons exposed to oxidative stress.{32531}  

     

    Brand:
    Cayman
    SKU:19705 -

    Available on backorder

  • Bizine is a phenelzine analog that inhibits lysine-specific demethylase 1 (LSD1; Ki(inact) = 59 nM).{32531} It is 23-fold, 63-fold, and >100-fold selective for LSD-1 over monoamine oxidase (MAO) A, MAOB, and LSD2, respectively.{32531} Bizine has been shown to induce bulk histone H3 lysine 4 dimethylation in LNCaP cancer cells (EC50 = ~2 µM) and, at 0.5 µM, to protect neurons exposed to oxidative stress.{32531}  

     

    Brand:
    Cayman
    SKU:19705 -

    Available on backorder

  • Bizine is a phenelzine analog that inhibits lysine-specific demethylase 1 (LSD1; Ki(inact) = 59 nM).{32531} It is 23-fold, 63-fold, and >100-fold selective for LSD-1 over monoamine oxidase (MAO) A, MAOB, and LSD2, respectively.{32531} Bizine has been shown to induce bulk histone H3 lysine 4 dimethylation in LNCaP cancer cells (EC50 = ~2 µM) and, at 0.5 µM, to protect neurons exposed to oxidative stress.{32531}  

     

    Brand:
    Cayman
    SKU:19705 -

    Available on backorder

  • bk-MDDMA (hydrochloride) (exempt preparation) (Item No. 22879) is a potential psychotropic designer drug of the phenethylamine, amphetamine, and cathinone chemical classes. This product is intended for forensic purposes.  

     

    Brand:
    Cayman
    SKU:22879 - 1 mg

    Available on backorder

  • BKT 140 is an antagonist of chemokine (C-X-C motif) receptor 4 (CXCR4; IC50 = 0.91 nM).{54472} It inhibits HIV-1-induced cytopathogenicity in MT-4 cells with an EC50 value of 4 nM. BKT 140 (100 nM) reduces migration of SUP-T1 leukemia and MDA-MB-231 breast cancer cells induced by chemokine (C-X-C) ligand 12 (CXCL12).{54472} It induces apoptosis in NB4 leukemia and RPMI-8226 multiple myeloma cancer cells when used at concentrations 8 and 40 µM.{54473} BKT 140 reduces pulmonary metastasis in an MDA-MB-231 mouse xenograft model.{54472} It also reduces the incidence of arthritis in a mouse model of collagen-induced arthritis.{54474}  

     

    Brand:
    Cayman
    SKU:30689 - 1 mg

    Available on backorder

  • BKT 140 is an antagonist of chemokine (C-X-C motif) receptor 4 (CXCR4; IC50 = 0.91 nM).{54472} It inhibits HIV-1-induced cytopathogenicity in MT-4 cells with an EC50 value of 4 nM. BKT 140 (100 nM) reduces migration of SUP-T1 leukemia and MDA-MB-231 breast cancer cells induced by chemokine (C-X-C) ligand 12 (CXCL12).{54472} It induces apoptosis in NB4 leukemia and RPMI-8226 multiple myeloma cancer cells when used at concentrations 8 and 40 µM.{54473} BKT 140 reduces pulmonary metastasis in an MDA-MB-231 mouse xenograft model.{54472} It also reduces the incidence of arthritis in a mouse model of collagen-induced arthritis.{54474}  

     

    Brand:
    Cayman
    SKU:30689 - 10 mg

    Available on backorder

  • BKT 140 is an antagonist of chemokine (C-X-C motif) receptor 4 (CXCR4; IC50 = 0.91 nM).{54472} It inhibits HIV-1-induced cytopathogenicity in MT-4 cells with an EC50 value of 4 nM. BKT 140 (100 nM) reduces migration of SUP-T1 leukemia and MDA-MB-231 breast cancer cells induced by chemokine (C-X-C) ligand 12 (CXCL12).{54472} It induces apoptosis in NB4 leukemia and RPMI-8226 multiple myeloma cancer cells when used at concentrations 8 and 40 µM.{54473} BKT 140 reduces pulmonary metastasis in an MDA-MB-231 mouse xenograft model.{54472} It also reduces the incidence of arthritis in a mouse model of collagen-induced arthritis.{54474}  

     

    Brand:
    Cayman
    SKU:30689 - 5 mg

    Available on backorder

  • BKT 140 is an antagonist of chemokine (C-X-C motif) receptor 4 (CXCR4; IC50 = 0.91 nM).{54472} It inhibits HIV-1-induced cytopathogenicity in MT-4 cells with an EC50 value of 4 nM. BKT 140 (100 nM) reduces migration of SUP-T1 leukemia and MDA-MB-231 breast cancer cells induced by chemokine (C-X-C) ligand 12 (CXCL12).{54472} It induces apoptosis in NB4 leukemia and RPMI-8226 multiple myeloma cancer cells when used at concentrations 8 and 40 µM.{54473} BKT 140 reduces pulmonary metastasis in an MDA-MB-231 mouse xenograft model.{54472} It also reduces the incidence of arthritis in a mouse model of collagen-induced arthritis.{54474}  

     

    Brand:
    Cayman
    SKU:30689 - 500 µg

    Available on backorder

  • Blasticidin A is a bacterial metabolite originally isolated from S. resistomycificus strain 2A-327.{36727} It inhibits aflatoxin production by A. parasiticus without affecting fungal growth (IC50s = 0.25 and 1.6 μM, respectively).{36728} Blasticidin A also decreases ribosomal protein levels and inhibits protein synthesis in S. cerevisiae.  

     

    Brand:
    Cayman
    SKU:25519 - 1 mg

    Available on backorder

  • Blasticidin A is a bacterial metabolite originally isolated from S. resistomycificus strain 2A-327.{36727} It inhibits aflatoxin production by A. parasiticus without affecting fungal growth (IC50s = 0.25 and 1.6 μM, respectively).{36728} Blasticidin A also decreases ribosomal protein levels and inhibits protein synthesis in S. cerevisiae.  

     

    Brand:
    Cayman
    SKU:25519 - 5 mg

    Available on backorder

  • Bleomycin is a glycopeptide antitumor antibiotic produced by the bacterium S. verticillus. Its mechanism of action causes single- and double-strand DNA breaks in tumor cells, which interrupts the cell cycle.{21617} Bleomycin is thought to achieve this by chelating metal ions, producing a pseudoenzyme that reacts with oxygen to produce superoxide and hydroxide free radicals that cleave DNA.{21617} Bleomycin has been used for the treatment of Hodgkin’s lymphoma in combination with doxorubicin, squamous cell carcinomas, testicular cancer, as well as in animal models of pulmonary fibrosis.{21618, 21616}  

     

    Brand:
    Cayman
    SKU:-
  • Bleomycin is a glycopeptide antitumor antibiotic produced by the bacterium S. verticillus. Its mechanism of action causes single- and double-strand DNA breaks in tumor cells, which interrupts the cell cycle.{21617} Bleomycin is thought to achieve this by chelating metal ions, producing a pseudoenzyme that reacts with oxygen to produce superoxide and hydroxide free radicals that cleave DNA.{21617} Bleomycin has been used for the treatment of Hodgkin’s lymphoma in combination with doxorubicin, squamous cell carcinomas, testicular cancer, as well as in animal models of pulmonary fibrosis.{21618, 21616}  

     

    Brand:
    Cayman
    SKU:-
  • Bleomycin is a glycopeptide antitumor antibiotic produced by the bacterium S. verticillus. Its mechanism of action causes single- and double-strand DNA breaks in tumor cells, which interrupts the cell cycle.{21617} Bleomycin is thought to achieve this by chelating metal ions, producing a pseudoenzyme that reacts with oxygen to produce superoxide and hydroxide free radicals that cleave DNA.{21617} Bleomycin has been used for the treatment of Hodgkin’s lymphoma in combination with doxorubicin, squamous cell carcinomas, testicular cancer, as well as in animal models of pulmonary fibrosis.{21618, 21616}  

     

    Brand:
    Cayman
    SKU:-
  • Bleomycin is a glycopeptide antitumor antibiotic produced by the bacterium S. verticillus. Its mechanism of action causes single- and double-strand DNA breaks in tumor cells, which interrupts the cell cycle.{21617} Bleomycin is thought to achieve this by chelating metal ions, producing a pseudoenzyme that reacts with oxygen to produce superoxide and hydroxide free radicals that cleave DNA.{21617} Bleomycin has been used for the treatment of Hodgkin’s lymphoma in combination with doxorubicin, squamous cell carcinomas, testicular cancer, as well as in animal models of pulmonary fibrosis.{21618, 21616}  

     

    Brand:
    Cayman
    SKU:-
  • Bleomycin A5 is one of a family of glycopeptide antibiotics first isolated from S. verticillus. As a family, the bleomycins consist of carbohydrate and metal binding domains joined to a variable C-terminal tail through a linker domain.{21617,32411} The metal binding domain and C-terminal tail mediate DNA and RNA binding that, in the presence of oxygen, generates free radicals leading to nucleic acid cleavage.{21617,32411} Bleomycin A5 has a C-terminal that mimics polyamines, facilitating its import into cells via the carnitine transporter SLC22A16.{29262} Cells expressing this transporter are ~300-fold more sensitive to bleomycin A5 than cells lacking this transporter, suggesting that cancer cells that overexpress SCL22A16 might be selectively targeted by this form of bleomycin.{29262}  

     

    Brand:
    Cayman
    SKU:19692 -

    Available on backorder

  • Bleomycin A5 is one of a family of glycopeptide antibiotics first isolated from S. verticillus. As a family, the bleomycins consist of carbohydrate and metal binding domains joined to a variable C-terminal tail through a linker domain.{21617,32411} The metal binding domain and C-terminal tail mediate DNA and RNA binding that, in the presence of oxygen, generates free radicals leading to nucleic acid cleavage.{21617,32411} Bleomycin A5 has a C-terminal that mimics polyamines, facilitating its import into cells via the carnitine transporter SLC22A16.{29262} Cells expressing this transporter are ~300-fold more sensitive to bleomycin A5 than cells lacking this transporter, suggesting that cancer cells that overexpress SCL22A16 might be selectively targeted by this form of bleomycin.{29262}  

     

    Brand:
    Cayman
    SKU:19692 -

    Available on backorder

  • Bleomycin A5 is one of a family of glycopeptide antibiotics first isolated from S. verticillus. As a family, the bleomycins consist of carbohydrate and metal binding domains joined to a variable C-terminal tail through a linker domain.{21617,32411} The metal binding domain and C-terminal tail mediate DNA and RNA binding that, in the presence of oxygen, generates free radicals leading to nucleic acid cleavage.{21617,32411} Bleomycin A5 has a C-terminal that mimics polyamines, facilitating its import into cells via the carnitine transporter SLC22A16.{29262} Cells expressing this transporter are ~300-fold more sensitive to bleomycin A5 than cells lacking this transporter, suggesting that cancer cells that overexpress SCL22A16 might be selectively targeted by this form of bleomycin.{29262}  

     

    Brand:
    Cayman
    SKU:19692 -

    Available on backorder

  • Bleomycin A5 is one of a family of glycopeptide antibiotics first isolated from S. verticillus. As a family, the bleomycins consist of carbohydrate and metal binding domains joined to a variable C-terminal tail through a linker domain.{21617,32411} The metal binding domain and C-terminal tail mediate DNA and RNA binding that, in the presence of oxygen, generates free radicals leading to nucleic acid cleavage.{21617,32411} Bleomycin A5 has a C-terminal that mimics polyamines, facilitating its import into cells via the carnitine transporter SLC22A16.{29262} Cells expressing this transporter are ~300-fold more sensitive to bleomycin A5 than cells lacking this transporter, suggesting that cancer cells that overexpress SCL22A16 might be selectively targeted by this form of bleomycin.{29262}  

     

    Brand:
    Cayman
    SKU:19692 -

    Available on backorder

  • Blinin is a diterpene originally isolated from C. blini with antiulcerogenic activity.{60084,60086} In vivo, blinin decreases gastric mucosal levels of malondialdehyde (MDA) and ulcer area in a rat model of pyloric ligation-induced ulcers.{60086}  

     

    Brand:
    Cayman
    SKU:30945 - 1 mg

    Available on backorder

  • Blinin is a diterpene originally isolated from C. blini with antiulcerogenic activity.{60084,60086} In vivo, blinin decreases gastric mucosal levels of malondialdehyde (MDA) and ulcer area in a rat model of pyloric ligation-induced ulcers.{60086}  

     

    Brand:
    Cayman
    SKU:30945 - 10 mg

    Available on backorder

  • Blinin is a diterpene originally isolated from C. blini with antiulcerogenic activity.{60084,60086} In vivo, blinin decreases gastric mucosal levels of malondialdehyde (MDA) and ulcer area in a rat model of pyloric ligation-induced ulcers.{60086}  

     

    Brand:
    Cayman
    SKU:30945 - 5 mg

    Available on backorder

  • Blinin is a diterpene originally isolated from C. blini with antiulcerogenic activity.{60084,60086} In vivo, blinin decreases gastric mucosal levels of malondialdehyde (MDA) and ulcer area in a rat model of pyloric ligation-induced ulcers.{60086}  

     

    Brand:
    Cayman
    SKU:30945 - 500 µg

    Available on backorder

  • Blonanserin is a 4-phenyl-2-(1-piperazinyl) pyridine that acts as an antagonist at dopamine D2, D3, and serotonin 5-HT2A receptors (Kis = 0.14, 0.49, and 0.81 nM, respectively).{26905} It binds to 5-HT6 with a Ki value of 11.7 nM and demonstrates relatively low affinity for 5-HT2C (Ki = 26.4 nM), adrenergic α1 (Ki = 26.7 nM), histamine H1 (Ki = 765 nM), and muscarinic M1 receptors (Ki = 100 nM).{26905} Blonanserin was developed in Japan as a novel antipsychotic that displays 20- and 94-fold higher affinity for D2 receptors compared to haloperidol (Item No. 12014) and risperidone (Item No. 13629), respectively.{26905}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Blonanserin is a 4-phenyl-2-(1-piperazinyl) pyridine that acts as an antagonist at dopamine D2, D3, and serotonin 5-HT2A receptors (Kis = 0.14, 0.49, and 0.81 nM, respectively).{26905} It binds to 5-HT6 with a Ki value of 11.7 nM and demonstrates relatively low affinity for 5-HT2C (Ki = 26.4 nM), adrenergic α1 (Ki = 26.7 nM), histamine H1 (Ki = 765 nM), and muscarinic M1 receptors (Ki = 100 nM).{26905} Blonanserin was developed in Japan as a novel antipsychotic that displays 20- and 94-fold higher affinity for D2 receptors compared to haloperidol (Item No. 12014) and risperidone (Item No. 13629), respectively.{26905}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Blonanserin is a 4-phenyl-2-(1-piperazinyl) pyridine that acts as an antagonist at dopamine D2, D3, and serotonin 5-HT2A receptors (Kis = 0.14, 0.49, and 0.81 nM, respectively).{26905} It binds to 5-HT6 with a Ki value of 11.7 nM and demonstrates relatively low affinity for 5-HT2C (Ki = 26.4 nM), adrenergic α1 (Ki = 26.7 nM), histamine H1 (Ki = 765 nM), and muscarinic M1 receptors (Ki = 100 nM).{26905} Blonanserin was developed in Japan as a novel antipsychotic that displays 20- and 94-fold higher affinity for D2 receptors compared to haloperidol (Item No. 12014) and risperidone (Item No. 13629), respectively.{26905}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Blonanserin is a 4-phenyl-2-(1-piperazinyl) pyridine that acts as an antagonist at dopamine D2, D3, and serotonin 5-HT2A receptors (Kis = 0.14, 0.49, and 0.81 nM, respectively).{26905} It binds to 5-HT6 with a Ki value of 11.7 nM and demonstrates relatively low affinity for 5-HT2C (Ki = 26.4 nM), adrenergic α1 (Ki = 26.7 nM), histamine H1 (Ki = 765 nM), and muscarinic M1 receptors (Ki = 100 nM).{26905} Blonanserin was developed in Japan as a novel antipsychotic that displays 20- and 94-fold higher affinity for D2 receptors compared to haloperidol (Item No. 12014) and risperidone (Item No. 13629), respectively.{26905}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Immunogen: HeLa cells transfected with human BLT1 • Clone designation: 7B1 • Host: Mouse • Cross-Reactivity: (+) BLT1; (−) BLT2, CysLT1, and CysLT2 receptors • Species Reactivity: (+) Human • Isotype: IgG2a • Application(s): FC, IF, and IHC of frozen sections • The human BLT1 receptor is a GPCR that mediates the proinflammatory effects of leukotriene B4 (LTB4). Northern blotting reveals that the BLT1 receptor is highly expressed in leukocytes, U937 cells, and to a much lower extent in spleen and thymus.  

     

    Brand:
    Cayman
    SKU:120111- 1 ea

    Available on backorder

  • Immunogen: HeLa cells transfected with human BLT1 • Clone designation: 7B1 • Host: Mouse • Cross-Reactivity: (+) BLT1; (−) BLT2, CysLT1, and CysLT2 receptors • Species Reactivity: (+) Human • Isotype: IgG2a • Application(s): FC, IF, and IHC of frozen sections • The human BLT1 receptor is a GPCR that mediates the proinflammatory effects of leukotriene B4 (LTB4). Northern blotting reveals that the BLT1 receptor is highly expressed in leukocytes, U937 cells, and to a much lower extent in spleen and thymus.  

     

    Brand:
    Cayman
    SKU:120111- 1 ea
  • The human BLT1 receptor is a G protein-coupled receptor that mediates the proinflammatory effects of leukotriene B4 (LTB4).{4425} Northern blotting reveals that the BLT1 receptor is highly expressed in leukocytes, U937 cells, and to a much lower extent in spleen and thymus.{4425} Sheep lung membranes have also been identified as a rich source for receptor isolation and purification.{4640} A second, low-affinity LTB4 receptor, BLT2, has also been cloned and characterized.{8280,8525,8743} Cayman Chemical’s BLT1 Receptor Monoclonal Antibody is a useful tool for the detection of human BLT1 by flow cytometry, immunofluorescence, and immunohistochemistry. The antibody does not cross react with the other leukotriene receptors (BLT2, CysLT1, or CysLT2) and does not work for Western blot analysis of BLT1.  

     

    Brand:
    Cayman
    SKU:120111 - 1 ea

    Available on backorder

  • Immunogen: Synthetic peptide from the C-terminal region of human BLT1 • Host: Rabbit • Cross Reactivity: (-) BLT2, CysLT1, and CysLT2 Receptors 1 • Species Reactivity (+) human, bovine, and mouse BLT1 receptor • Application(s): FC, ICC, IHC, and WB • The human BLT1 receptor is a GPCR that mediates the proinflammatory effects of leukotriene B4 (LTB4). Northern blotting reveals that the BLT1 receptor is highly expressed in leukocytes, U937 cells, and to a much lower extent in spleen and thymus.  

     

    Brand:
    Cayman
    SKU:120114- 500 µl

    Available on backorder

  • Immunogen: Synthetic peptide from the C-terminal region of human BLT1 • Host: Rabbit • Cross Reactivity: (-) BLT2, CysLT1, and CysLT2 Receptors 1 • Species Reactivity (+) human, bovine, and mouse BLT1 receptor • Application(s): FC, ICC, IHC, and WB • The human BLT1 receptor is a GPCR that mediates the proinflammatory effects of leukotriene B4 (LTB4). Northern blotting reveals that the BLT1 receptor is highly expressed in leukocytes, U937 cells, and to a much lower extent in spleen and thymus.  

     

    Brand:
    Cayman
    SKU:120114- 500 µl
  • The leukotriene B4 receptor 1 (BLT1 receptor), cloned from HL-60 human leukemia cells, has 352 amino acids and seven putative membrane-spanning domains.{4425} The primary structure of the receptor is identical to that of a putative purinoceptor, P2Y7, which binds to micromolar concentrations of ATP.{4424} Northern blotting reveals that the BLT1 receptor is highly expressed in leukocytes, U937 cells, and to a much lower extent in spleen and thymus.{4425} Sheep lung membranes have also been identified as a rich source for receptor isolation and purification.{4640} A second LTB4 receptor, BLT2, has recently been cloned and characterized.{8280,8525,8743} This antibody was made against a peptide from the C-terminus of the BLT1 receptor, which is located on the intracellular side of the plasma membrane. Therefore, when performing studies on whole cells, permeabilization of the cells is required for the antibody to enter the cytosol.  

     

    Brand:
    Cayman
    SKU:120114 - 500 µl

    Available on backorder

  • Immunogen: peptide from the C-terminal region of human BLT2 • Host: Rabbit • Species Reactivity: (+) Human and mouse • Application(s): WB  

     

    Brand:
    Cayman
    SKU:120124- 1 ea

    Available on backorder

  • Immunogen: peptide from the C-terminal region of human BLT2 • Host: Rabbit • Species Reactivity: (+) Human and mouse • Application(s): WB  

     

    Brand:
    Cayman
    SKU:120124- 1 ea
  • Leukotriene B4 (LTB4) promotes a number of leukocyte functions including aggregation, stimulation of ion fluxes, superoxide anion production, chemotaxis, and chemokinesis. Two G-protein coupled receptors, BLT1 and BLT2, which mediate the actions of LTB4 have been cloned and characterized.{8280,8743,8525,4425} The BLT1 receptor is expressed in leukocytes, U937 cells, and to a much lower extent in spleen and thymus.{4425} The human BLT2 receptor is a 358 amino acid protein with approximately 40% homology to BLT1 at the amino acid level.{8280,8743,8525} The BLT2 receptor is more broadly expressed than the BLT1 receptor, with highest levels observed in liver, spleen, ovary, intestine, and peripheral blood leukocytes.{8280,8743,8525} Activation of the BLT2 receptor by LTB4 leads to Ca2+ mobilization as well as decreases in cyclic AMP, indicating interaction of the receptor with Gq and Gi classes of G-proteins.{8743}  

     

    Brand:
    Cayman
    SKU:120124 - 1 ea

    Available on backorder

  • BLU-285 is a dual inhibitor of KIT receptor and platelet-derived growth factor receptor α (PDGFRα) tyrosine kinases with activating loop mutations (IC50s = 0.27 and 0.24 nM for KITD816V and PDGFRαD842V, respectively).{40523} It is >150-fold selective for KITD816V and PDGFRαD842V over a kinase panel at a concentration of 3 μM. BLU-285 also has activity against a panel of KIT and PDGFRα loop mutants identified in patients with gastrointestinal stromal tumors (GISTs; IC50s = D814Y mastocytoma allograft mouse model and a GIST patient-derived mouse xenograft model in a dose-dependent manner. Formulations containing BLU-285 have been used to treat KIT- and PDGFRα-driven malignancies.  

     

    Brand:
    Cayman
    SKU:22985 - 1 mg

    Available on backorder

  • BLU-285 is a dual inhibitor of KIT receptor and platelet-derived growth factor receptor α (PDGFRα) tyrosine kinases with activating loop mutations (IC50s = 0.27 and 0.24 nM for KITD816V and PDGFRαD842V, respectively).{40523} It is >150-fold selective for KITD816V and PDGFRαD842V over a kinase panel at a concentration of 3 μM. BLU-285 also has activity against a panel of KIT and PDGFRα loop mutants identified in patients with gastrointestinal stromal tumors (GISTs; IC50s = D814Y mastocytoma allograft mouse model and a GIST patient-derived mouse xenograft model in a dose-dependent manner. Formulations containing BLU-285 have been used to treat KIT- and PDGFRα-driven malignancies.  

     

    Brand:
    Cayman
    SKU:22985 - 10 mg

    Available on backorder

  • BLU-285 is a dual inhibitor of KIT receptor and platelet-derived growth factor receptor α (PDGFRα) tyrosine kinases with activating loop mutations (IC50s = 0.27 and 0.24 nM for KITD816V and PDGFRαD842V, respectively).{40523} It is >150-fold selective for KITD816V and PDGFRαD842V over a kinase panel at a concentration of 3 μM. BLU-285 also has activity against a panel of KIT and PDGFRα loop mutants identified in patients with gastrointestinal stromal tumors (GISTs; IC50s = D814Y mastocytoma allograft mouse model and a GIST patient-derived mouse xenograft model in a dose-dependent manner. Formulations containing BLU-285 have been used to treat KIT- and PDGFRα-driven malignancies.  

     

    Brand:
    Cayman
    SKU:22985 - 25 mg

    Available on backorder

  • BLU-285 is a dual inhibitor of KIT receptor and platelet-derived growth factor receptor α (PDGFRα) tyrosine kinases with activating loop mutations (IC50s = 0.27 and 0.24 nM for KITD816V and PDGFRαD842V, respectively).{40523} It is >150-fold selective for KITD816V and PDGFRαD842V over a kinase panel at a concentration of 3 μM. BLU-285 also has activity against a panel of KIT and PDGFRα loop mutants identified in patients with gastrointestinal stromal tumors (GISTs; IC50s = D814Y mastocytoma allograft mouse model and a GIST patient-derived mouse xenograft model in a dose-dependent manner. Formulations containing BLU-285 have been used to treat KIT- and PDGFRα-driven malignancies.  

     

    Brand:
    Cayman
    SKU:22985 - 5 mg

    Available on backorder