Cayman
Showing 11701–11850 of 45550 results
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Betulinic aldehyde is a triterpenoid that has been found in Z. cambodiana and has diverse biological activities.{48464,48465,48466,48467} It is active against P. falciparum (IC50 = 6.5 μg/ml) and M. tuberculosis (MIC = 25 μg/ml) in vitro, as well as laboratory and clinical isolates of methicillin-resistant and -sensitive S. aureus (MICs = 128-512 and 8-512 μg/ml, respectively).{48464,48465} Betulinic aldehyde inhibits dengue virus non-structural protein 5 (NS5) RNA-dependent RNA polymerase (IC50 = 6.1 μM) and inhibits dengue virus type 2 replication by 20 and 55% when used at concentrations of 5 and 10 μg/ml, respectively.{48466} It also inhibits growth of leukemia, melanoma, neuroblastoma, and normal fibroblast cell lines (IC50s = 1.1-4.9, 9.6-10.6, 7.5-8.8, and 18.5 μM, respectively).{48467}
Brand:CaymanSKU:27810 - 25 mgAvailable on backorder
Betulinic aldehyde is a triterpenoid that has been found in Z. cambodiana and has diverse biological activities.{48464,48465,48466,48467} It is active against P. falciparum (IC50 = 6.5 μg/ml) and M. tuberculosis (MIC = 25 μg/ml) in vitro, as well as laboratory and clinical isolates of methicillin-resistant and -sensitive S. aureus (MICs = 128-512 and 8-512 μg/ml, respectively).{48464,48465} Betulinic aldehyde inhibits dengue virus non-structural protein 5 (NS5) RNA-dependent RNA polymerase (IC50 = 6.1 μM) and inhibits dengue virus type 2 replication by 20 and 55% when used at concentrations of 5 and 10 μg/ml, respectively.{48466} It also inhibits growth of leukemia, melanoma, neuroblastoma, and normal fibroblast cell lines (IC50s = 1.1-4.9, 9.6-10.6, 7.5-8.8, and 18.5 μM, respectively).{48467}
Brand:CaymanSKU:27810 - 5 mgAvailable on backorder
Betulonic acid is a triterpenoid that has been found in B. chinensis and has diverse biological activities, including antiparasitic, antiviral, and anticancer properties.{52273,52274,52275,52276} It is active against the chloroquine-resistant P. falciparum W2 clone (IC50 = 10.01 µM), as well as L. infantum and L. donovani promastigotes when used at a concentration of 50 µM.{52275,52274} Betulonic acid inhibits replication of herpes simplex virus I (HSV-I), echovirus 6, and the H7N1 strain of influenza A (EC50s = 0.9, 73.32, and 5.7 µM, respectively).{52276} It inhibits proliferation of MGC803, Bcap-37, MCF-7, PC3, and NIH3T3 cancer cells by 68.1, 44.9, 56.1, 52.4, and 22.1%, respectively, when used at a concentration of 20 µM.{52273}
Brand:CaymanSKU:29765 - 10 mgAvailable on backorder
Betulonic acid is a triterpenoid that has been found in B. chinensis and has diverse biological activities, including antiparasitic, antiviral, and anticancer properties.{52273,52274,52275,52276} It is active against the chloroquine-resistant P. falciparum W2 clone (IC50 = 10.01 µM), as well as L. infantum and L. donovani promastigotes when used at a concentration of 50 µM.{52275,52274} Betulonic acid inhibits replication of herpes simplex virus I (HSV-I), echovirus 6, and the H7N1 strain of influenza A (EC50s = 0.9, 73.32, and 5.7 µM, respectively).{52276} It inhibits proliferation of MGC803, Bcap-37, MCF-7, PC3, and NIH3T3 cancer cells by 68.1, 44.9, 56.1, 52.4, and 22.1%, respectively, when used at a concentration of 20 µM.{52273}
Brand:CaymanSKU:29765 - 25 mgAvailable on backorder
Betulonic acid is a triterpenoid that has been found in B. chinensis and has diverse biological activities, including antiparasitic, antiviral, and anticancer properties.{52273,52274,52275,52276} It is active against the chloroquine-resistant P. falciparum W2 clone (IC50 = 10.01 µM), as well as L. infantum and L. donovani promastigotes when used at a concentration of 50 µM.{52275,52274} Betulonic acid inhibits replication of herpes simplex virus I (HSV-I), echovirus 6, and the H7N1 strain of influenza A (EC50s = 0.9, 73.32, and 5.7 µM, respectively).{52276} It inhibits proliferation of MGC803, Bcap-37, MCF-7, PC3, and NIH3T3 cancer cells by 68.1, 44.9, 56.1, 52.4, and 22.1%, respectively, when used at a concentration of 20 µM.{52273}
Brand:CaymanSKU:29765 - 5 mgAvailable on backorder
Betulonic acid is a triterpenoid that has been found in B. chinensis and has diverse biological activities, including antiparasitic, antiviral, and anticancer properties.{52273,52274,52275,52276} It is active against the chloroquine-resistant P. falciparum W2 clone (IC50 = 10.01 µM), as well as L. infantum and L. donovani promastigotes when used at a concentration of 50 µM.{52275,52274} Betulonic acid inhibits replication of herpes simplex virus I (HSV-I), echovirus 6, and the H7N1 strain of influenza A (EC50s = 0.9, 73.32, and 5.7 µM, respectively).{52276} It inhibits proliferation of MGC803, Bcap-37, MCF-7, PC3, and NIH3T3 cancer cells by 68.1, 44.9, 56.1, 52.4, and 22.1%, respectively, when used at a concentration of 20 µM.{52273}
Brand:CaymanSKU:29765 - 50 mgAvailable on backorder
Bevantolol is an antagonist of the β1-adrenergic receptor (β1-AR; Ki = 14.79 nM in rat cortical membranes).{52361} It is selective for β1- over β2-ARs (Ki = 588.84 nM), as well as α2-ARs up to 100 μM, but is an antagonist of α1-ARs (Ki = 125.89 nM). Bevantolol inhibits low voltage-activated calcium currents (LVA-ICa) in dissociated rat ventro-medial hypothalamic neurons (IC50 = 40 μM).{52362} It inhibits norepinephrine-induced contraction of isolated rabbit thoracic aorta (pA2 = 4.77), isoprenaline-induced inotropic effects in isolated guinea pig right atria (pA2 = 7.74), and isoprenaline-induced relaxation of isolated guinea pig trachea (pA2 = 6.69).{52363} Bevantolol (250 mg/kg per day) prevents immobilization stress-induced increases in systolic blood pressure in a rat model of stress-induced hypertension.{52364}
Brand:CaymanSKU:29792 - 100 mgAvailable on backorder
Bevantolol is an antagonist of the β1-adrenergic receptor (β1-AR; Ki = 14.79 nM in rat cortical membranes).{52361} It is selective for β1- over β2-ARs (Ki = 588.84 nM), as well as α2-ARs up to 100 μM, but is an antagonist of α1-ARs (Ki = 125.89 nM). Bevantolol inhibits low voltage-activated calcium currents (LVA-ICa) in dissociated rat ventro-medial hypothalamic neurons (IC50 = 40 μM).{52362} It inhibits norepinephrine-induced contraction of isolated rabbit thoracic aorta (pA2 = 4.77), isoprenaline-induced inotropic effects in isolated guinea pig right atria (pA2 = 7.74), and isoprenaline-induced relaxation of isolated guinea pig trachea (pA2 = 6.69).{52363} Bevantolol (250 mg/kg per day) prevents immobilization stress-induced increases in systolic blood pressure in a rat model of stress-induced hypertension.{52364}
Brand:CaymanSKU:29792 - 250 mgAvailable on backorder
Bevantolol is an antagonist of the β1-adrenergic receptor (β1-AR; Ki = 14.79 nM in rat cortical membranes).{52361} It is selective for β1- over β2-ARs (Ki = 588.84 nM), as well as α2-ARs up to 100 μM, but is an antagonist of α1-ARs (Ki = 125.89 nM). Bevantolol inhibits low voltage-activated calcium currents (LVA-ICa) in dissociated rat ventro-medial hypothalamic neurons (IC50 = 40 μM).{52362} It inhibits norepinephrine-induced contraction of isolated rabbit thoracic aorta (pA2 = 4.77), isoprenaline-induced inotropic effects in isolated guinea pig right atria (pA2 = 7.74), and isoprenaline-induced relaxation of isolated guinea pig trachea (pA2 = 6.69).{52363} Bevantolol (250 mg/kg per day) prevents immobilization stress-induced increases in systolic blood pressure in a rat model of stress-induced hypertension.{52364}
Brand:CaymanSKU:29792 - 500 mgAvailable on backorder
Bexarotene is an agonist of retinoid X receptors (RXRs; EC50s = 28, 25, and 20 nM for RXRα, RXRβ, and RXRγ, respectively, in reporter assays).{20758} It is selective for RXRs over retinoic acid receptors (RARs; EC50s = >10 µM for RARα, RARβ, and RARγ). Bexarotene (10 µM) induces apoptosis in MJ, HuT 78, and HH cutaneous T cell lymphoma (CTCL) cells, as well as inhibits lung metastasis and angiogenesis in A549 and MDA-MB-231 mouse xenograft models when administered at a dose of 100 mg/kg per day.{58126,58127} It reduces increased brain interstitial fluid levels of amyloid-β (1-40) (Aβ40) and Aβ42 in the APP/PS1 transgenic mouse model of Alzheimer’s disease.{20759} It also reduces viral load in the culture supernatant of Vero E6 cells infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2; EC90 = 9.4 µM) and inhibits SARS-CoV-2 replication in a plaque reduction assay (EC50 = 2.01 µM).{59330} Formulations containing bexarotene have been used in the treatment of CTCL.
Brand:CaymanSKU:11571 - 10 mgAvailable on backorder
Bexarotene is an agonist of retinoid X receptors (RXRs; EC50s = 28, 25, and 20 nM for RXRα, RXRβ, and RXRγ, respectively, in reporter assays).{20758} It is selective for RXRs over retinoic acid receptors (RARs; EC50s = >10 µM for RARα, RARβ, and RARγ). Bexarotene (10 µM) induces apoptosis in MJ, HuT 78, and HH cutaneous T cell lymphoma (CTCL) cells, as well as inhibits lung metastasis and angiogenesis in A549 and MDA-MB-231 mouse xenograft models when administered at a dose of 100 mg/kg per day.{58126,58127} It reduces increased brain interstitial fluid levels of amyloid-β (1-40) (Aβ40) and Aβ42 in the APP/PS1 transgenic mouse model of Alzheimer’s disease.{20759} It also reduces viral load in the culture supernatant of Vero E6 cells infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2; EC90 = 9.4 µM) and inhibits SARS-CoV-2 replication in a plaque reduction assay (EC50 = 2.01 µM).{59330} Formulations containing bexarotene have been used in the treatment of CTCL.
Brand:CaymanSKU:11571 - 5 mgAvailable on backorder
Bexarotene is an agonist of retinoid X receptors (RXRs; EC50s = 28, 25, and 20 nM for RXRα, RXRβ, and RXRγ, respectively, in reporter assays).{20758} It is selective for RXRs over retinoic acid receptors (RARs; EC50s = >10 µM for RARα, RARβ, and RARγ). Bexarotene (10 µM) induces apoptosis in MJ, HuT 78, and HH cutaneous T cell lymphoma (CTCL) cells, as well as inhibits lung metastasis and angiogenesis in A549 and MDA-MB-231 mouse xenograft models when administered at a dose of 100 mg/kg per day.{58126,58127} It reduces increased brain interstitial fluid levels of amyloid-β (1-40) (Aβ40) and Aβ42 in the APP/PS1 transgenic mouse model of Alzheimer’s disease.{20759} It also reduces viral load in the culture supernatant of Vero E6 cells infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2; EC90 = 9.4 µM) and inhibits SARS-CoV-2 replication in a plaque reduction assay (EC50 = 2.01 µM).{59330} Formulations containing bexarotene have been used in the treatment of CTCL.
Brand:CaymanSKU:11571 - 50 mgAvailable on backorder
Bezafibrate is a non-selective agonist of peroxisome proliferator-activated receptors (PPARs; EC50s = 50, 60, and 20 μM for human PPARα, PPARγ, and PPARδ, respectively).{10670} It reduces triglyceride levels and the size of lipid droplets in an oleic acid-induced HepaRG hepatocyte model of steatosis when used at a concentration of 25 μM.{42456} Bezafibrate (10 mg/kg per day) reduces plasma VLDL and LDL mass and triglyceride and free fatty acid levels in a high-fructose plus lard diet-induced rat model of insulin resistance.{42937}
Brand:CaymanSKU:10009145 - 1 gAvailable on backorder
Bezafibrate is a non-selective agonist of peroxisome proliferator-activated receptors (PPARs; EC50s = 50, 60, and 20 μM for human PPARα, PPARγ, and PPARδ, respectively).{10670} It reduces triglyceride levels and the size of lipid droplets in an oleic acid-induced HepaRG hepatocyte model of steatosis when used at a concentration of 25 μM.{42456} Bezafibrate (10 mg/kg per day) reduces plasma VLDL and LDL mass and triglyceride and free fatty acid levels in a high-fructose plus lard diet-induced rat model of insulin resistance.{42937}
Brand:CaymanSKU:10009145 - 10 gAvailable on backorder
Bezafibrate is a non-selective agonist of peroxisome proliferator-activated receptors (PPARs; EC50s = 50, 60, and 20 μM for human PPARα, PPARγ, and PPARδ, respectively).{10670} It reduces triglyceride levels and the size of lipid droplets in an oleic acid-induced HepaRG hepatocyte model of steatosis when used at a concentration of 25 μM.{42456} Bezafibrate (10 mg/kg per day) reduces plasma VLDL and LDL mass and triglyceride and free fatty acid levels in a high-fructose plus lard diet-induced rat model of insulin resistance.{42937}
Brand:CaymanSKU:10009145 - 5 gAvailable on backorder
Bezafibrate is a non-selective agonist of peroxisome proliferator-activated receptors (PPARs; EC50s = 50, 60, and 20 μM for human PPARα, PPARγ, and PPARδ, respectively).{10670} It reduces triglyceride levels and the size of lipid droplets in an oleic acid-induced HepaRG hepatocyte model of steatosis when used at a concentration of 25 μM.{42456} Bezafibrate (10 mg/kg per day) reduces plasma VLDL and LDL mass and triglyceride and free fatty acid levels in a high-fructose plus lard diet-induced rat model of insulin resistance.{42937}
Brand:CaymanSKU:10009145 - 500 mgAvailable on backorder
Bezafibrate-d4 is intended for use as an internal standard for the quantification of bezafibrate (Item No. 10009145) by GC- or LC-MS. Bezafibrate is a non-selective agonist of peroxisome proliferator-activated receptors (PPARs; EC50s = 50, 60, and 20 μM for human PPARα, PPARγ, and PPARδ, respectively).{10670} It reduces triglyceride levels and the size of lipid droplets in an oleic acid-induced HepaRG hepatocyte model of steatosis when used at a concentration of 25 μM.{42456} Bezafibrate (10 mg/kg per day) reduces plasma VLDL and LDL mass and triglyceride and free fatty acid levels in a high-fructose plus lard diet-induced rat model of insulin resistance.{42937}
Brand:CaymanSKU:28526 - 1 mgAvailable on backorder
BFH772 is an inhibitor of VEGF receptor 2 (VEGFR2; IC50 = 0.0027 μM for the human receptor).{42999} It is selective for human VEGFR2 over mouse VEGFR2 and human VEGFR1 and VEGFR3 (IC50s = 1.5, 1.7, and 1.1 μM, respectively), as well as 40-fold selective over B-RAF, RET, and Tie2. BFH772 inhibits VEGF-induced proliferation of human umbilical vein endothelial cells (HUVECs; IC50 = <0.01 nM). It inhibits VEGF-induced increases in tissue weight and Tie2 levels in an angiogenesis chamber implant model in mice when administered at doses of 1 and 3 mg/kg per day. BFH772 (3 mg/kg per day) inhibits primary tumor and metastasis growth in a B16 melanoma mouse model.
Brand:CaymanSKU:21386 -Out of stock
BFH772 is an inhibitor of VEGF receptor 2 (VEGFR2; IC50 = 0.0027 μM for the human receptor).{42999} It is selective for human VEGFR2 over mouse VEGFR2 and human VEGFR1 and VEGFR3 (IC50s = 1.5, 1.7, and 1.1 μM, respectively), as well as 40-fold selective over B-RAF, RET, and Tie2. BFH772 inhibits VEGF-induced proliferation of human umbilical vein endothelial cells (HUVECs; IC50 = <0.01 nM). It inhibits VEGF-induced increases in tissue weight and Tie2 levels in an angiogenesis chamber implant model in mice when administered at doses of 1 and 3 mg/kg per day. BFH772 (3 mg/kg per day) inhibits primary tumor and metastasis growth in a B16 melanoma mouse model.
Brand:CaymanSKU:21386 -Out of stock
BFH772 is an inhibitor of VEGF receptor 2 (VEGFR2; IC50 = 0.0027 μM for the human receptor).{42999} It is selective for human VEGFR2 over mouse VEGFR2 and human VEGFR1 and VEGFR3 (IC50s = 1.5, 1.7, and 1.1 μM, respectively), as well as 40-fold selective over B-RAF, RET, and Tie2. BFH772 inhibits VEGF-induced proliferation of human umbilical vein endothelial cells (HUVECs; IC50 = <0.01 nM). It inhibits VEGF-induced increases in tissue weight and Tie2 levels in an angiogenesis chamber implant model in mice when administered at doses of 1 and 3 mg/kg per day. BFH772 (3 mg/kg per day) inhibits primary tumor and metastasis growth in a B16 melanoma mouse model.
Brand:CaymanSKU:21386 -Out of stock
BFH772 is an inhibitor of VEGF receptor 2 (VEGFR2; IC50 = 0.0027 μM for the human receptor).{42999} It is selective for human VEGFR2 over mouse VEGFR2 and human VEGFR1 and VEGFR3 (IC50s = 1.5, 1.7, and 1.1 μM, respectively), as well as 40-fold selective over B-RAF, RET, and Tie2. BFH772 inhibits VEGF-induced proliferation of human umbilical vein endothelial cells (HUVECs; IC50 = <0.01 nM). It inhibits VEGF-induced increases in tissue weight and Tie2 levels in an angiogenesis chamber implant model in mice when administered at doses of 1 and 3 mg/kg per day. BFH772 (3 mg/kg per day) inhibits primary tumor and metastasis growth in a B16 melanoma mouse model.
Brand:CaymanSKU:21386 -Out of stock
BG45 is an HDAC class I inhibitor with selectivity for HDAC3 (IC50 = 289 nM). It inhibits HDAC1, HDAC2, and HDAC6 with greatly reduced potency (IC50s = 2, 2.2, and >20 µM, respectively).{27757} At concentrations up to 50 mg/kg, BG45 alone or in combination with bortezomib has been shown to dose-dependently inhibit tumor growth in a mouse model of multiple myeloma.{27757}
Brand:CaymanSKU:-Out of stock
BG45 is an HDAC class I inhibitor with selectivity for HDAC3 (IC50 = 289 nM). It inhibits HDAC1, HDAC2, and HDAC6 with greatly reduced potency (IC50s = 2, 2.2, and >20 µM, respectively).{27757} At concentrations up to 50 mg/kg, BG45 alone or in combination with bortezomib has been shown to dose-dependently inhibit tumor growth in a mouse model of multiple myeloma.{27757}
Brand:CaymanSKU:-Out of stock
BG45 is an HDAC class I inhibitor with selectivity for HDAC3 (IC50 = 289 nM). It inhibits HDAC1, HDAC2, and HDAC6 with greatly reduced potency (IC50s = 2, 2.2, and >20 µM, respectively).{27757} At concentrations up to 50 mg/kg, BG45 alone or in combination with bortezomib has been shown to dose-dependently inhibit tumor growth in a mouse model of multiple myeloma.{27757}
Brand:CaymanSKU:-Out of stock
BG45 is an HDAC class I inhibitor with selectivity for HDAC3 (IC50 = 289 nM). It inhibits HDAC1, HDAC2, and HDAC6 with greatly reduced potency (IC50s = 2, 2.2, and >20 µM, respectively).{27757} At concentrations up to 50 mg/kg, BG45 alone or in combination with bortezomib has been shown to dose-dependently inhibit tumor growth in a mouse model of multiple myeloma.{27757}
Brand:CaymanSKU:-Out of stock
BGC 20-1531 is a potent and selective antagonist of the prostaglandin E2 (PGE2; Item No. 14010) receptor subtype 4 (EP4) with Ki values of 11.7, >10,000, and >10,000 nM for EP4, EP2, and EP3, respectively.{17141} It is selective for EP4, exhibiting 2-induced cAMP accumulation in a dose-dependent manner in HEK293 EBNA cells that stably express human EP4 receptors. It also reverses PGE2-induced vasorelaxation (Kb = 15.85 nM) in human middle cerebral and middle meningeal arterial rings. BGC 20-1531 prevents PGE2-induced increases in carotid blood flow and decreases in carotid resistance with an ID50 value of 5 mg/kg in dogs.
Brand:CaymanSKU:19742 -Available on backorder
BGC 20-1531 is a potent and selective antagonist of the prostaglandin E2 (PGE2; Item No. 14010) receptor subtype 4 (EP4) with Ki values of 11.7, >10,000, and >10,000 nM for EP4, EP2, and EP3, respectively.{17141} It is selective for EP4, exhibiting 2-induced cAMP accumulation in a dose-dependent manner in HEK293 EBNA cells that stably express human EP4 receptors. It also reverses PGE2-induced vasorelaxation (Kb = 15.85 nM) in human middle cerebral and middle meningeal arterial rings. BGC 20-1531 prevents PGE2-induced increases in carotid blood flow and decreases in carotid resistance with an ID50 value of 5 mg/kg in dogs.
Brand:CaymanSKU:19742 -Available on backorder
BGC 20-1531 is a potent and selective antagonist of the prostaglandin E2 (PGE2; Item No. 14010) receptor subtype 4 (EP4) with Ki values of 11.7, >10,000, and >10,000 nM for EP4, EP2, and EP3, respectively.{17141} It is selective for EP4, exhibiting 2-induced cAMP accumulation in a dose-dependent manner in HEK293 EBNA cells that stably express human EP4 receptors. It also reverses PGE2-induced vasorelaxation (Kb = 15.85 nM) in human middle cerebral and middle meningeal arterial rings. BGC 20-1531 prevents PGE2-induced increases in carotid blood flow and decreases in carotid resistance with an ID50 value of 5 mg/kg in dogs.
Brand:CaymanSKU:19742 -Available on backorder
BGC 20-1531 is a potent and selective antagonist of the prostaglandin E2 (PGE2; Item No. 14010) receptor subtype 4 (EP4) with Ki values of 11.7, >10,000, and >10,000 nM for EP4, EP2, and EP3, respectively.{17141} It is selective for EP4, exhibiting 2-induced cAMP accumulation in a dose-dependent manner in HEK293 EBNA cells that stably express human EP4 receptors. It also reverses PGE2-induced vasorelaxation (Kb = 15.85 nM) in human middle cerebral and middle meningeal arterial rings. BGC 20-1531 prevents PGE2-induced increases in carotid blood flow and decreases in carotid resistance with an ID50 value of 5 mg/kg in dogs.
Brand:CaymanSKU:19742 -Available on backorder
BGJ398 is an orally available inhibitor of human FGFRs (IC50s = 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively).{31102,30600} It inhibits FGFR4 and VEGFR2 with IC50 values of 60 and 180 nM, respectively, and displays comparatively little activity towards Abl, Fyn, Kit, Lck, Lyn, and Yes (IC50s = 0.3-2.5 µM).{31102} BGJ398 has been shown to suppress proliferation of cancer cells with wild-type FGFR3 overexpression (IC50s = 5, 30, 32, and 15 nM, for RT112, RT4, SW780, and JMSU1 cells, respectively).{31102} In an RT112 bladder cancer xenograft mouse model overexpressing wild-type FGFR3, BGJ398 inhibited tumor growth after oral administration of 10-30 mg/kg.{31102}
Brand:CaymanSKU:-Available on backorder
BGJ398 is an orally available inhibitor of human FGFRs (IC50s = 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively).{31102,30600} It inhibits FGFR4 and VEGFR2 with IC50 values of 60 and 180 nM, respectively, and displays comparatively little activity towards Abl, Fyn, Kit, Lck, Lyn, and Yes (IC50s = 0.3-2.5 µM).{31102} BGJ398 has been shown to suppress proliferation of cancer cells with wild-type FGFR3 overexpression (IC50s = 5, 30, 32, and 15 nM, for RT112, RT4, SW780, and JMSU1 cells, respectively).{31102} In an RT112 bladder cancer xenograft mouse model overexpressing wild-type FGFR3, BGJ398 inhibited tumor growth after oral administration of 10-30 mg/kg.{31102}
Brand:CaymanSKU:-Available on backorder
BGJ398 is an orally available inhibitor of human FGFRs (IC50s = 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively).{31102,30600} It inhibits FGFR4 and VEGFR2 with IC50 values of 60 and 180 nM, respectively, and displays comparatively little activity towards Abl, Fyn, Kit, Lck, Lyn, and Yes (IC50s = 0.3-2.5 µM).{31102} BGJ398 has been shown to suppress proliferation of cancer cells with wild-type FGFR3 overexpression (IC50s = 5, 30, 32, and 15 nM, for RT112, RT4, SW780, and JMSU1 cells, respectively).{31102} In an RT112 bladder cancer xenograft mouse model overexpressing wild-type FGFR3, BGJ398 inhibited tumor growth after oral administration of 10-30 mg/kg.{31102}
Brand:CaymanSKU:-Available on backorder
BGJ398 is an orally available inhibitor of human FGFRs (IC50s = 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively).{31102,30600} It inhibits FGFR4 and VEGFR2 with IC50 values of 60 and 180 nM, respectively, and displays comparatively little activity towards Abl, Fyn, Kit, Lck, Lyn, and Yes (IC50s = 0.3-2.5 µM).{31102} BGJ398 has been shown to suppress proliferation of cancer cells with wild-type FGFR3 overexpression (IC50s = 5, 30, 32, and 15 nM, for RT112, RT4, SW780, and JMSU1 cells, respectively).{31102} In an RT112 bladder cancer xenograft mouse model overexpressing wild-type FGFR3, BGJ398 inhibited tumor growth after oral administration of 10-30 mg/kg.{31102}
Brand:CaymanSKU:-Available on backorder
The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis.{22577} BGP-15 is a PARP inhibitor and insulin sensitizer. In perfused heart, it blocks self-ADP-ribosylation of nuclear PARP (Ki = 57 µM) and mono-ADP-ribosylation of GRP78, resulting in decreased levels of reactive oxygen species, lipid peroxidation, and single-strand DNA breaks.{29058,29060} BGP-15 acts as a co-inducer of heat shock protein 72, augmenting expression induced by heat shock factor 1 in adipocytes and skeletal muscles and improving insulin sensitivity.{29057,29059}
Brand:CaymanSKU:-Available on backorder
The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis.{22577} BGP-15 is a PARP inhibitor and insulin sensitizer. In perfused heart, it blocks self-ADP-ribosylation of nuclear PARP (Ki = 57 µM) and mono-ADP-ribosylation of GRP78, resulting in decreased levels of reactive oxygen species, lipid peroxidation, and single-strand DNA breaks.{29058,29060} BGP-15 acts as a co-inducer of heat shock protein 72, augmenting expression induced by heat shock factor 1 in adipocytes and skeletal muscles and improving insulin sensitivity.{29057,29059}
Brand:CaymanSKU:-Available on backorder
The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis.{22577} BGP-15 is a PARP inhibitor and insulin sensitizer. In perfused heart, it blocks self-ADP-ribosylation of nuclear PARP (Ki = 57 µM) and mono-ADP-ribosylation of GRP78, resulting in decreased levels of reactive oxygen species, lipid peroxidation, and single-strand DNA breaks.{29058,29060} BGP-15 acts as a co-inducer of heat shock protein 72, augmenting expression induced by heat shock factor 1 in adipocytes and skeletal muscles and improving insulin sensitivity.{29057,29059}
Brand:CaymanSKU:-Available on backorder
The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis.{22577} BGP-15 is a PARP inhibitor and insulin sensitizer. In perfused heart, it blocks self-ADP-ribosylation of nuclear PARP (Ki = 57 µM) and mono-ADP-ribosylation of GRP78, resulting in decreased levels of reactive oxygen species, lipid peroxidation, and single-strand DNA breaks.{29058,29060} BGP-15 acts as a co-inducer of heat shock protein 72, augmenting expression induced by heat shock factor 1 in adipocytes and skeletal muscles and improving insulin sensitivity.{29057,29059}
Brand:CaymanSKU:-Available on backorder
The family of Bcl-2 proteins plays pivotal roles in either promoting or preventing apoptosis. Bcl-2 family members contain one or more of four characteristic Bcl-2 homology (BH) domains, which are crucial for function. For example, anti-apoptotic Bcl-2 family proteins prevent death signaling by heterodimerizing with pro-death proteins at their BH3 domains.{24784} BH3I-1 is a cell permeable inhibitor that blocks the binding of BH3 peptides to Bcl-xL, inducing apoptosis.{30354} It inhibits interactions of BH3 domain-containing proteins with Bcl-xL, Bcl-2, and Bcl-W, inducing apoptosis in Bcl-2 or Bcl-W expressing cells with Ki values of 43.4 and 124 µM, respectively.{30356,30355} BH3I-1 enhances radiation sensitivity in non-small cell lung cancer cells.{30356}
Brand:CaymanSKU:-Available on backorder
The family of Bcl-2 proteins plays pivotal roles in either promoting or preventing apoptosis. Bcl-2 family members contain one or more of four characteristic Bcl-2 homology (BH) domains, which are crucial for function. For example, anti-apoptotic Bcl-2 family proteins prevent death signaling by heterodimerizing with pro-death proteins at their BH3 domains.{24784} BH3I-1 is a cell permeable inhibitor that blocks the binding of BH3 peptides to Bcl-xL, inducing apoptosis.{30354} It inhibits interactions of BH3 domain-containing proteins with Bcl-xL, Bcl-2, and Bcl-W, inducing apoptosis in Bcl-2 or Bcl-W expressing cells with Ki values of 43.4 and 124 µM, respectively.{30356,30355} BH3I-1 enhances radiation sensitivity in non-small cell lung cancer cells.{30356}
Brand:CaymanSKU:-Available on backorder
The family of Bcl-2 proteins plays pivotal roles in either promoting or preventing apoptosis. Bcl-2 family members contain one or more of four characteristic Bcl-2 homology (BH) domains, which are crucial for function. For example, anti-apoptotic Bcl-2 family proteins prevent death signaling by heterodimerizing with pro-death proteins at their BH3 domains.{24784} BH3I-1 is a cell permeable inhibitor that blocks the binding of BH3 peptides to Bcl-xL, inducing apoptosis.{30354} It inhibits interactions of BH3 domain-containing proteins with Bcl-xL, Bcl-2, and Bcl-W, inducing apoptosis in Bcl-2 or Bcl-W expressing cells with Ki values of 43.4 and 124 µM, respectively.{30356,30355} BH3I-1 enhances radiation sensitivity in non-small cell lung cancer cells.{30356}
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The family of Bcl-2 proteins plays pivotal roles in either promoting or preventing apoptosis. Bcl-2 family members contain one or more of four characteristic Bcl-2 homology (BH) domains, which are crucial for function. For example, anti-apoptotic Bcl-2 family proteins prevent death signaling by heterodimerizing with pro-death proteins at their BH3 domains.{24784} BH3I-1 is a cell permeable inhibitor that blocks the binding of BH3 peptides to Bcl-xL, inducing apoptosis.{30354} It inhibits interactions of BH3 domain-containing proteins with Bcl-xL, Bcl-2, and Bcl-W, inducing apoptosis in Bcl-2 or Bcl-W expressing cells with Ki values of 43.4 and 124 µM, respectively.{30356,30355} BH3I-1 enhances radiation sensitivity in non-small cell lung cancer cells.{30356}
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BHBM is an acylhydrazone with antifungal activity.{50810,53336} It is active against C. neoformans in vitro (MIC80 = 1 µg/ml).{53336} BHBM (0.25, 1, and 4 µg/ml) inhibits the synthesis of glucosylceramide, which is essential to fungal cell division, in C. neoformans but not J774 murine macrophages.{50810} In vivo, BHBM (1.2 mg/kg per day) increases survival in a mouse model of C. neoformans infection.
Brand:CaymanSKU:29817 - 1 mgAvailable on backorder
BHBM is an acylhydrazone with antifungal activity.{50810,53336} It is active against C. neoformans in vitro (MIC80 = 1 µg/ml).{53336} BHBM (0.25, 1, and 4 µg/ml) inhibits the synthesis of glucosylceramide, which is essential to fungal cell division, in C. neoformans but not J774 murine macrophages.{50810} In vivo, BHBM (1.2 mg/kg per day) increases survival in a mouse model of C. neoformans infection.
Brand:CaymanSKU:29817 - 10 mgAvailable on backorder
BHBM is an acylhydrazone with antifungal activity.{50810,53336} It is active against C. neoformans in vitro (MIC80 = 1 µg/ml).{53336} BHBM (0.25, 1, and 4 µg/ml) inhibits the synthesis of glucosylceramide, which is essential to fungal cell division, in C. neoformans but not J774 murine macrophages.{50810} In vivo, BHBM (1.2 mg/kg per day) increases survival in a mouse model of C. neoformans infection.
Brand:CaymanSKU:29817 - 25 mgAvailable on backorder
BHBM is an acylhydrazone with antifungal activity.{50810,53336} It is active against C. neoformans in vitro (MIC80 = 1 µg/ml).{53336} BHBM (0.25, 1, and 4 µg/ml) inhibits the synthesis of glucosylceramide, which is essential to fungal cell division, in C. neoformans but not J774 murine macrophages.{50810} In vivo, BHBM (1.2 mg/kg per day) increases survival in a mouse model of C. neoformans infection.
Brand:CaymanSKU:29817 - 5 mgAvailable on backorder
BHPI is an antagonist of estrogen receptor α (ERα) that blocks 17β-estradiol-induced proliferation of drug-resistant breast, endometrial, and ovarian cancer cell lines at concentrations ranging from 10 to 1,000 nM.{28679} It is effective in vivo, driving tumor regression in mice bearing MCF-7 xenografts at a dose of 15 mg/kg daily.{28679} BHPI specifically inhibits ERα-dependent gene expression and protein synthesis by activating the unfolded protein response in cells.{28679}
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BHPI is an antagonist of estrogen receptor α (ERα) that blocks 17β-estradiol-induced proliferation of drug-resistant breast, endometrial, and ovarian cancer cell lines at concentrations ranging from 10 to 1,000 nM.{28679} It is effective in vivo, driving tumor regression in mice bearing MCF-7 xenografts at a dose of 15 mg/kg daily.{28679} BHPI specifically inhibits ERα-dependent gene expression and protein synthesis by activating the unfolded protein response in cells.{28679}
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BHPI is an antagonist of estrogen receptor α (ERα) that blocks 17β-estradiol-induced proliferation of drug-resistant breast, endometrial, and ovarian cancer cell lines at concentrations ranging from 10 to 1,000 nM.{28679} It is effective in vivo, driving tumor regression in mice bearing MCF-7 xenografts at a dose of 15 mg/kg daily.{28679} BHPI specifically inhibits ERα-dependent gene expression and protein synthesis by activating the unfolded protein response in cells.{28679}
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BHT is a synthetic antioxidant.{56221,56222} It scavenges peroxide, 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805), superoxide, and ABTS (Item No. 27317) radicals in cell-free assays, as well as inhibits lipid peroxidation of linoleic acid (Item Nos. 90150 | 90150.1 | 21909) in vitro when used at a concentration of 45 µg/ml.{56221} BHT (0.025-3.2 mM) reduces freeze-thaw-induced malondialdehyde (MDA) production and increases sperm viability in boar spermatozoa preparations.{56222} Formulations containing BHT have been used as antioxidant cosmetic and food additives.
Brand:CaymanSKU:89910 - 1 gAvailable on backorder
BHT is a synthetic antioxidant.{56221,56222} It scavenges peroxide, 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805), superoxide, and ABTS (Item No. 27317) radicals in cell-free assays, as well as inhibits lipid peroxidation of linoleic acid (Item Nos. 90150 | 90150.1 | 21909) in vitro when used at a concentration of 45 µg/ml.{56221} BHT (0.025-3.2 mM) reduces freeze-thaw-induced malondialdehyde (MDA) production and increases sperm viability in boar spermatozoa preparations.{56222} Formulations containing BHT have been used as antioxidant cosmetic and food additives.
Brand:CaymanSKU:89910 - 500 mgAvailable on backorder
Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} BI-2536 is a 2-aminopyrimidine-containing inhibitor of Plk1 (IC50 = 0.83 nM).{29246,24210} It displays 4- and 11-fold selectivity for Plk1 over Plk2 and Plk3, respectively. BI-2536 induces mitotic arrest and apoptosis in diverse human cancer cell lines and drives regression of human tumor xenografts in nude mice.{29246} It shows good blood-brain barrier permeability and causes mitotic arrest in glioblastoma-derived neural stem cells but not normal neural stem cells.{29225} BI-2536 is also an inhibitor of BRD4 (IC50 = 25 nM), suppressing BRD4-dependent c-Myc expression in MM.1S multiple myeloma cells.{29245}
Brand:CaymanSKU:-Available on backorder
Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} BI-2536 is a 2-aminopyrimidine-containing inhibitor of Plk1 (IC50 = 0.83 nM).{29246,24210} It displays 4- and 11-fold selectivity for Plk1 over Plk2 and Plk3, respectively. BI-2536 induces mitotic arrest and apoptosis in diverse human cancer cell lines and drives regression of human tumor xenografts in nude mice.{29246} It shows good blood-brain barrier permeability and causes mitotic arrest in glioblastoma-derived neural stem cells but not normal neural stem cells.{29225} BI-2536 is also an inhibitor of BRD4 (IC50 = 25 nM), suppressing BRD4-dependent c-Myc expression in MM.1S multiple myeloma cells.{29245}
Brand:CaymanSKU:-Available on backorder
Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} BI-2536 is a 2-aminopyrimidine-containing inhibitor of Plk1 (IC50 = 0.83 nM).{29246,24210} It displays 4- and 11-fold selectivity for Plk1 over Plk2 and Plk3, respectively. BI-2536 induces mitotic arrest and apoptosis in diverse human cancer cell lines and drives regression of human tumor xenografts in nude mice.{29246} It shows good blood-brain barrier permeability and causes mitotic arrest in glioblastoma-derived neural stem cells but not normal neural stem cells.{29225} BI-2536 is also an inhibitor of BRD4 (IC50 = 25 nM), suppressing BRD4-dependent c-Myc expression in MM.1S multiple myeloma cells.{29245}
Brand:CaymanSKU:-Available on backorder
Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} BI-2536 is a 2-aminopyrimidine-containing inhibitor of Plk1 (IC50 = 0.83 nM).{29246,24210} It displays 4- and 11-fold selectivity for Plk1 over Plk2 and Plk3, respectively. BI-2536 induces mitotic arrest and apoptosis in diverse human cancer cell lines and drives regression of human tumor xenografts in nude mice.{29246} It shows good blood-brain barrier permeability and causes mitotic arrest in glioblastoma-derived neural stem cells but not normal neural stem cells.{29225} BI-2536 is also an inhibitor of BRD4 (IC50 = 25 nM), suppressing BRD4-dependent c-Myc expression in MM.1S multiple myeloma cells.{29245}
Brand:CaymanSKU:-Available on backorder
BI-409306 is a potent and selective phosphodiesterase 9A (PDE9A) inhibitor with IC50 values of 65 and 168 nM for the human and rat enzymes, respectively.{52498} It is selective for PDE9A over PDE2A, -3A, -4B, -5A, -6AB, -7A and -10A and 95 non-PDE targets at 10 µM but does inhibit human PDE1A and PDE1C (IC50s = 1.45 and 1.17 µM, respectively). BI-409306 (0.5 mg/kg), in combination with MK-801, an NMDA receptor antagonist that reduces cGMP levels, increases cGMP levels by 41% in mouse striatal tissue compared with MK-801 alone. BI 406306 enhances long-term potentiation (LTP) in hippocampal slices and reverses MK-801-induced working memory deficits in a T-maze task in mice when administered at doses ranging from 0.007 to 2.5 mg/kg.
Brand:CaymanSKU:30375 - 1 mgAvailable on backorder
BI-409306 is a potent and selective phosphodiesterase 9A (PDE9A) inhibitor with IC50 values of 65 and 168 nM for the human and rat enzymes, respectively.{52498} It is selective for PDE9A over PDE2A, -3A, -4B, -5A, -6AB, -7A and -10A and 95 non-PDE targets at 10 µM but does inhibit human PDE1A and PDE1C (IC50s = 1.45 and 1.17 µM, respectively). BI-409306 (0.5 mg/kg), in combination with MK-801, an NMDA receptor antagonist that reduces cGMP levels, increases cGMP levels by 41% in mouse striatal tissue compared with MK-801 alone. BI 406306 enhances long-term potentiation (LTP) in hippocampal slices and reverses MK-801-induced working memory deficits in a T-maze task in mice when administered at doses ranging from 0.007 to 2.5 mg/kg.
Brand:CaymanSKU:30375 - 10 mgAvailable on backorder
BI-409306 is a potent and selective phosphodiesterase 9A (PDE9A) inhibitor with IC50 values of 65 and 168 nM for the human and rat enzymes, respectively.{52498} It is selective for PDE9A over PDE2A, -3A, -4B, -5A, -6AB, -7A and -10A and 95 non-PDE targets at 10 µM but does inhibit human PDE1A and PDE1C (IC50s = 1.45 and 1.17 µM, respectively). BI-409306 (0.5 mg/kg), in combination with MK-801, an NMDA receptor antagonist that reduces cGMP levels, increases cGMP levels by 41% in mouse striatal tissue compared with MK-801 alone. BI 406306 enhances long-term potentiation (LTP) in hippocampal slices and reverses MK-801-induced working memory deficits in a T-maze task in mice when administered at doses ranging from 0.007 to 2.5 mg/kg.
Brand:CaymanSKU:30375 - 25 mgAvailable on backorder
BI-409306 is a potent and selective phosphodiesterase 9A (PDE9A) inhibitor with IC50 values of 65 and 168 nM for the human and rat enzymes, respectively.{52498} It is selective for PDE9A over PDE2A, -3A, -4B, -5A, -6AB, -7A and -10A and 95 non-PDE targets at 10 µM but does inhibit human PDE1A and PDE1C (IC50s = 1.45 and 1.17 µM, respectively). BI-409306 (0.5 mg/kg), in combination with MK-801, an NMDA receptor antagonist that reduces cGMP levels, increases cGMP levels by 41% in mouse striatal tissue compared with MK-801 alone. BI 406306 enhances long-term potentiation (LTP) in hippocampal slices and reverses MK-801-induced working memory deficits in a T-maze task in mice when administered at doses ranging from 0.007 to 2.5 mg/kg.
Brand:CaymanSKU:30375 - 5 mgAvailable on backorder
Hepatocyte nuclear factor 4α (HNF4α) is a nuclear receptor transcription factor that controls the expression of many genes including those involved in glucose and lipid homeostasis and maintenance of epithelial differentiation. BI-6015 is a small molecule antagonist of HNF4α that has been shown to repress the expression of known HNF4α target genes.{21357} At concentrations up to 20 μM, BI-6015 has been shown to reduce endogenous insulin gene expression by as much as 50-fold in T6PNE cells.{21357} The hepatocytes from livers of mice injected with 10 and 30 mg/kg BI-6015 exhibit marked, dose-dependent fat accumulation (steatosis).{21357} Additionally, at a daily dose of 30 mg/kg, BI-6015 induces apoptosis in a human hepatocellular carcinoma mouse model.{21357}
Brand:CaymanSKU:12032 - 10 mgAvailable on backorder
Hepatocyte nuclear factor 4α (HNF4α) is a nuclear receptor transcription factor that controls the expression of many genes including those involved in glucose and lipid homeostasis and maintenance of epithelial differentiation. BI-6015 is a small molecule antagonist of HNF4α that has been shown to repress the expression of known HNF4α target genes.{21357} At concentrations up to 20 μM, BI-6015 has been shown to reduce endogenous insulin gene expression by as much as 50-fold in T6PNE cells.{21357} The hepatocytes from livers of mice injected with 10 and 30 mg/kg BI-6015 exhibit marked, dose-dependent fat accumulation (steatosis).{21357} Additionally, at a daily dose of 30 mg/kg, BI-6015 induces apoptosis in a human hepatocellular carcinoma mouse model.{21357}
Brand:CaymanSKU:12032 - 5 mgAvailable on backorder
Hepatocyte nuclear factor 4α (HNF4α) is a nuclear receptor transcription factor that controls the expression of many genes including those involved in glucose and lipid homeostasis and maintenance of epithelial differentiation. BI-6015 is a small molecule antagonist of HNF4α that has been shown to repress the expression of known HNF4α target genes.{21357} At concentrations up to 20 μM, BI-6015 has been shown to reduce endogenous insulin gene expression by as much as 50-fold in T6PNE cells.{21357} The hepatocytes from livers of mice injected with 10 and 30 mg/kg BI-6015 exhibit marked, dose-dependent fat accumulation (steatosis).{21357} Additionally, at a daily dose of 30 mg/kg, BI-6015 induces apoptosis in a human hepatocellular carcinoma mouse model.{21357}
Brand:CaymanSKU:12032 - 50 mgAvailable on backorder
BI-605906 is an inhibitor of inhibitor of kappa B kinase subunit β (IKKβ; IC50 = 380 nM).{32502} It is selective for IKKβ over insulin-like growth factor 1 (IGF1; IC50 = 7.6 μM) and over 100 kinases in a panel up to 10 μM. BI-605906 partially inhibits IL-1-stimulated activation of IKKε/TBK1 in vitro. BI-605906 also inhibits TNF-α-dependent IkB degradation and expression of the proinflammatory cytokines IL-6, IL-1β, and C-X-C motif ligand 1/2 (CXCL1/2) without affecting lipogenic gene expression or glucose production in murine primary hepatocytes.{40150}
Brand:CaymanSKU:-Available on backorder
BI-605906 is an inhibitor of inhibitor of kappa B kinase subunit β (IKKβ; IC50 = 380 nM).{32502} It is selective for IKKβ over insulin-like growth factor 1 (IGF1; IC50 = 7.6 μM) and over 100 kinases in a panel up to 10 μM. BI-605906 partially inhibits IL-1-stimulated activation of IKKε/TBK1 in vitro. BI-605906 also inhibits TNF-α-dependent IkB degradation and expression of the proinflammatory cytokines IL-6, IL-1β, and C-X-C motif ligand 1/2 (CXCL1/2) without affecting lipogenic gene expression or glucose production in murine primary hepatocytes.{40150}
Brand:CaymanSKU:-Available on backorder
BI-605906 is an inhibitor of inhibitor of kappa B kinase subunit β (IKKβ; IC50 = 380 nM).{32502} It is selective for IKKβ over insulin-like growth factor 1 (IGF1; IC50 = 7.6 μM) and over 100 kinases in a panel up to 10 μM. BI-605906 partially inhibits IL-1-stimulated activation of IKKε/TBK1 in vitro. BI-605906 also inhibits TNF-α-dependent IkB degradation and expression of the proinflammatory cytokines IL-6, IL-1β, and C-X-C motif ligand 1/2 (CXCL1/2) without affecting lipogenic gene expression or glucose production in murine primary hepatocytes.{40150}
Brand:CaymanSKU:-Available on backorder
BI-671800 is an antagonist of the prostaglandin D2 (PGD2; Item No. 12010) receptor CRTH2/DP2 (IC50 = 42 nM in a radioligand binding assay).{17373} It binds selectively to CRTH2/DP2 over DP1, thromboxane, and prostacyclin receptors (IC50s = 25.6, 62.6, and >100 μM, respectively). BI-671800 inhibits PGD2-induced shape change in human eosinophils (IC50 = 744 nM).
Brand:CaymanSKU:27638 - 1 mgAvailable on backorder
BI-671800 is an antagonist of the prostaglandin D2 (PGD2; Item No. 12010) receptor CRTH2/DP2 (IC50 = 42 nM in a radioligand binding assay).{17373} It binds selectively to CRTH2/DP2 over DP1, thromboxane, and prostacyclin receptors (IC50s = 25.6, 62.6, and >100 μM, respectively). BI-671800 inhibits PGD2-induced shape change in human eosinophils (IC50 = 744 nM).
Brand:CaymanSKU:27638 - 10 mgAvailable on backorder
BI-671800 is an antagonist of the prostaglandin D2 (PGD2; Item No. 12010) receptor CRTH2/DP2 (IC50 = 42 nM in a radioligand binding assay).{17373} It binds selectively to CRTH2/DP2 over DP1, thromboxane, and prostacyclin receptors (IC50s = 25.6, 62.6, and >100 μM, respectively). BI-671800 inhibits PGD2-induced shape change in human eosinophils (IC50 = 744 nM).
Brand:CaymanSKU:27638 - 5 mgAvailable on backorder
Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} BI-6727 is a dihydropteridinone that inhibits Plk1, Plk2, and Plk3 (IC50s = 0.87, 5, and 56 nM, respectively), inducing mitotic arrest and apoptosis.{29375} It inhibits proliferation of multiple cancer cell lines with EC50 values ranging from 11-37 nM and prevents the growth of various human carcinoma xenografts in mice.{29375} BI-6727 was found to reverse ABC-efflux transporter-mediated multidrug resistance activity through its inhibition of the transport activity of ABCB1 and ABCG2, thus promoting mitotic arrest in resistant cancer cells.{29376}
Brand:CaymanSKU:-Available on backorder
Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} BI-6727 is a dihydropteridinone that inhibits Plk1, Plk2, and Plk3 (IC50s = 0.87, 5, and 56 nM, respectively), inducing mitotic arrest and apoptosis.{29375} It inhibits proliferation of multiple cancer cell lines with EC50 values ranging from 11-37 nM and prevents the growth of various human carcinoma xenografts in mice.{29375} BI-6727 was found to reverse ABC-efflux transporter-mediated multidrug resistance activity through its inhibition of the transport activity of ABCB1 and ABCG2, thus promoting mitotic arrest in resistant cancer cells.{29376}
Brand:CaymanSKU:-Available on backorder
Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} BI-6727 is a dihydropteridinone that inhibits Plk1, Plk2, and Plk3 (IC50s = 0.87, 5, and 56 nM, respectively), inducing mitotic arrest and apoptosis.{29375} It inhibits proliferation of multiple cancer cell lines with EC50 values ranging from 11-37 nM and prevents the growth of various human carcinoma xenografts in mice.{29375} BI-6727 was found to reverse ABC-efflux transporter-mediated multidrug resistance activity through its inhibition of the transport activity of ABCB1 and ABCG2, thus promoting mitotic arrest in resistant cancer cells.{29376}
Brand:CaymanSKU:-Available on backorder
Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} BI-6727 is a dihydropteridinone that inhibits Plk1, Plk2, and Plk3 (IC50s = 0.87, 5, and 56 nM, respectively), inducing mitotic arrest and apoptosis.{29375} It inhibits proliferation of multiple cancer cell lines with EC50 values ranging from 11-37 nM and prevents the growth of various human carcinoma xenografts in mice.{29375} BI-6727 was found to reverse ABC-efflux transporter-mediated multidrug resistance activity through its inhibition of the transport activity of ABCB1 and ABCG2, thus promoting mitotic arrest in resistant cancer cells.{29376}
Brand:CaymanSKU:-Available on backorder
BH3-interacting domain (Bid) is cleaved by caspase-8 to produce the truncated protein tBid, which facilitates cytochrome c release from mitochondria and drives apoptosis.{28610,28613} BI-6C9 is an inhibitor of tBid (Kd = 20 µM), blocking the release of both cytochrome c and second mitochondria-derived activator of caspase from mitochondria.{28607,28608} It prevents apoptosis in neurons treated with glutamate or oxygen-glucose deprivation.{28611,28609} BI-6C9 (10 µM) also inhibits the nuclear translocation of apoptosis-inducing factor AIF, preventing the death of ovarian OVCAR-3 cancer cells induced by IFN-α2a.{28612}
Brand:CaymanSKU:-Out of stock
BH3-interacting domain (Bid) is cleaved by caspase-8 to produce the truncated protein tBid, which facilitates cytochrome c release from mitochondria and drives apoptosis.{28610,28613} BI-6C9 is an inhibitor of tBid (Kd = 20 µM), blocking the release of both cytochrome c and second mitochondria-derived activator of caspase from mitochondria.{28607,28608} It prevents apoptosis in neurons treated with glutamate or oxygen-glucose deprivation.{28611,28609} BI-6C9 (10 µM) also inhibits the nuclear translocation of apoptosis-inducing factor AIF, preventing the death of ovarian OVCAR-3 cancer cells induced by IFN-α2a.{28612}
Brand:CaymanSKU:-Out of stock
BH3-interacting domain (Bid) is cleaved by caspase-8 to produce the truncated protein tBid, which facilitates cytochrome c release from mitochondria and drives apoptosis.{28610,28613} BI-6C9 is an inhibitor of tBid (Kd = 20 µM), blocking the release of both cytochrome c and second mitochondria-derived activator of caspase from mitochondria.{28607,28608} It prevents apoptosis in neurons treated with glutamate or oxygen-glucose deprivation.{28611,28609} BI-6C9 (10 µM) also inhibits the nuclear translocation of apoptosis-inducing factor AIF, preventing the death of ovarian OVCAR-3 cancer cells induced by IFN-α2a.{28612}
Brand:CaymanSKU:-Out of stock
BI-7273 is a potent BRD9 bromodomain inhibitor (Kd = 15.4 nM; IC50 = 19 nM) that less effectively inhibits the functionally and structurally related BRD7 bromodomain (IC50 = 117 nM).{30788} It is without effect against the bromodomains of BRD2 and BRD4, as well as a panel of kinases. BI-7273 inhibits the growth of EOL-1 acute myeloid leukemia cells in vitro (EC50 = 1.4 µM).{30788}
Brand:CaymanSKU:20311 -Available on backorder
BI-7273 is a potent BRD9 bromodomain inhibitor (Kd = 15.4 nM; IC50 = 19 nM) that less effectively inhibits the functionally and structurally related BRD7 bromodomain (IC50 = 117 nM).{30788} It is without effect against the bromodomains of BRD2 and BRD4, as well as a panel of kinases. BI-7273 inhibits the growth of EOL-1 acute myeloid leukemia cells in vitro (EC50 = 1.4 µM).{30788}
Brand:CaymanSKU:20311 -Available on backorder
BI-7273 is a potent BRD9 bromodomain inhibitor (Kd = 15.4 nM; IC50 = 19 nM) that less effectively inhibits the functionally and structurally related BRD7 bromodomain (IC50 = 117 nM).{30788} It is without effect against the bromodomains of BRD2 and BRD4, as well as a panel of kinases. BI-7273 inhibits the growth of EOL-1 acute myeloid leukemia cells in vitro (EC50 = 1.4 µM).{30788}
Brand:CaymanSKU:20311 -Available on backorder
BI-7273 is a potent BRD9 bromodomain inhibitor (Kd = 15.4 nM; IC50 = 19 nM) that less effectively inhibits the functionally and structurally related BRD7 bromodomain (IC50 = 117 nM).{30788} It is without effect against the bromodomains of BRD2 and BRD4, as well as a panel of kinases. BI-7273 inhibits the growth of EOL-1 acute myeloid leukemia cells in vitro (EC50 = 1.4 µM).{30788}
Brand:CaymanSKU:20311 -Available on backorder
BI-78D3 is an inhibitor of JNK (IC50 = 280 nM in a TR-FRET assay) that is competitive for JNK1 binding with pepJIP1, a JNK-interacting protein, with an IC50 value of 500 nM.{38279} It is selective for JNK, being 100-fold less active for the structurally similar MAPK family protein p38α and inactive at mammalian target of rapamycin (mTOR) or phosphatidylinositol 3-kinase α (PI3Kα). In a cell-based kinase assay, BI-78D3 inhibits c-Jun phosphorylation induced by TNF-α (EC50 = 12.4 µM). In a mouse model of type 2 diabetes, BI-78D3 (25 mg/kg) restores insulin sensitivity, reducing blood glucose levels when administered 30 minutes prior to insulin. BI-78D3 (30 µM) reduces contractions in human prostate strips induced by phenylephrine (Item Nos. 17205 | 18619) or norepinephrine (Item No. 16673) and reduces phosphorylation of c-Jun, a JNK substrate.{38280}
Brand:CaymanSKU:21183 -Out of stock
BI-78D3 is an inhibitor of JNK (IC50 = 280 nM in a TR-FRET assay) that is competitive for JNK1 binding with pepJIP1, a JNK-interacting protein, with an IC50 value of 500 nM.{38279} It is selective for JNK, being 100-fold less active for the structurally similar MAPK family protein p38α and inactive at mammalian target of rapamycin (mTOR) or phosphatidylinositol 3-kinase α (PI3Kα). In a cell-based kinase assay, BI-78D3 inhibits c-Jun phosphorylation induced by TNF-α (EC50 = 12.4 µM). In a mouse model of type 2 diabetes, BI-78D3 (25 mg/kg) restores insulin sensitivity, reducing blood glucose levels when administered 30 minutes prior to insulin. BI-78D3 (30 µM) reduces contractions in human prostate strips induced by phenylephrine (Item Nos. 17205 | 18619) or norepinephrine (Item No. 16673) and reduces phosphorylation of c-Jun, a JNK substrate.{38280}
Brand:CaymanSKU:21183 -Out of stock
BI-78D3 is an inhibitor of JNK (IC50 = 280 nM in a TR-FRET assay) that is competitive for JNK1 binding with pepJIP1, a JNK-interacting protein, with an IC50 value of 500 nM.{38279} It is selective for JNK, being 100-fold less active for the structurally similar MAPK family protein p38α and inactive at mammalian target of rapamycin (mTOR) or phosphatidylinositol 3-kinase α (PI3Kα). In a cell-based kinase assay, BI-78D3 inhibits c-Jun phosphorylation induced by TNF-α (EC50 = 12.4 µM). In a mouse model of type 2 diabetes, BI-78D3 (25 mg/kg) restores insulin sensitivity, reducing blood glucose levels when administered 30 minutes prior to insulin. BI-78D3 (30 µM) reduces contractions in human prostate strips induced by phenylephrine (Item Nos. 17205 | 18619) or norepinephrine (Item No. 16673) and reduces phosphorylation of c-Jun, a JNK substrate.{38280}
Brand:CaymanSKU:21183 -Out of stock