Chemicals
Showing 16501–16650 of 41137 results
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Daprodustat is an inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase that increases HIF stability and action. It is orally bioavailable, induces an effective erythropoietin (EPO) response, and stimulates non-EPO mechanisms of erythropoiesis in animal models. Daprodustat and related HIF prolyl hydroxylase inhibitors are in clinical trials for the treatment of anemia associated with chronic kidney disease.{31861,31862}
Brand:CaymanSKU:19915 -Available on backorder
Daprodustat is an inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase that increases HIF stability and action. It is orally bioavailable, induces an effective erythropoietin (EPO) response, and stimulates non-EPO mechanisms of erythropoiesis in animal models. Daprodustat and related HIF prolyl hydroxylase inhibitors are in clinical trials for the treatment of anemia associated with chronic kidney disease.{31861,31862}
Brand:CaymanSKU:19915 -Available on backorder
Daprodustat is an inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase that increases HIF stability and action. It is orally bioavailable, induces an effective erythropoietin (EPO) response, and stimulates non-EPO mechanisms of erythropoiesis in animal models. Daprodustat and related HIF prolyl hydroxylase inhibitors are in clinical trials for the treatment of anemia associated with chronic kidney disease.{31861,31862}
Brand:CaymanSKU:19915 -Available on backorder
Dapsone is an anti-inflammatory, antimalarial, and antibacterial compound.{28213} In vivo, dapsone (34 μg/animal per day) reduces epidermal hyperproliferation and epithelial thickness in the esophagus in a mouse model of proliferative dermatitis.{38501} It reduces lipid peroxidation, myeloperoxidase activity, and cellular apoptosis in the striatum of rats following ischemia and reperfusion injury.{38502} Dapsone reduces growth of M. leprae in the footpad of mice (MIC = 0.01-0.03 μg/ml in sera) and induces clearance of P. knowlesi infections in macaques.{38503,38504} It also reduces the number of P. gallinaceum sporozoites in a mosquito population allowed to feed on dapsone-treated chicks.{38504} Formulations containing dapsone have been used in the treatment of malaria, acne, dermatitis, and leprosy.
Brand:CaymanSKU:23743 - 100 gAvailable on backorder
Dapsone is an anti-inflammatory, antimalarial, and antibacterial compound.{28213} In vivo, dapsone (34 μg/animal per day) reduces epidermal hyperproliferation and epithelial thickness in the esophagus in a mouse model of proliferative dermatitis.{38501} It reduces lipid peroxidation, myeloperoxidase activity, and cellular apoptosis in the striatum of rats following ischemia and reperfusion injury.{38502} Dapsone reduces growth of M. leprae in the footpad of mice (MIC = 0.01-0.03 μg/ml in sera) and induces clearance of P. knowlesi infections in macaques.{38503,38504} It also reduces the number of P. gallinaceum sporozoites in a mosquito population allowed to feed on dapsone-treated chicks.{38504} Formulations containing dapsone have been used in the treatment of malaria, acne, dermatitis, and leprosy.
Brand:CaymanSKU:23743 - 50 gAvailable on backorder
Dapsone-d8 is intended for use as an internal standard for the quantification of dapsone by GC- or LC-MS. Dapsone is an anti-inflammatory and antibacterial compound that is widely used in the treatment of leprosy, malaria, acne, and various immune disorders.{28213} Dapsone is acetylated in the liver to monoacetyldapsone, the major metabolite, and other mono and diacetyl derivatives, and subsequently deacetylated back to diaminodiphenylsulfone (dapsone) until a state of equilibrium is achieved.
Brand:CaymanSKU:22113 -Out of stock
Dapsone-d8 is intended for use as an internal standard for the quantification of dapsone by GC- or LC-MS. Dapsone is an anti-inflammatory and antibacterial compound that is widely used in the treatment of leprosy, malaria, acne, and various immune disorders.{28213} Dapsone is acetylated in the liver to monoacetyldapsone, the major metabolite, and other mono and diacetyl derivatives, and subsequently deacetylated back to diaminodiphenylsulfone (dapsone) until a state of equilibrium is achieved.
Brand:CaymanSKU:22113 -Out of stock
γ-Secretase is a multi-subunit aspartyl protease that cleaves amyloid precursor protein (APP) and many other type 1 transmembrane proteins, including Notch, E-cadherin, and ErbB4. The proteolysis of APP by secretases produces beta amyloid (Aβ), a 39- to 42-amino acid peptide which forms the amyloid plaques that are characteristic of Alzheimer’s disease. DAPT is an inhibitor of γ-secretase, blocking the production of total Aβ in human primary neuronal cultures with an IC50 value of 115 nM and Aβ42 with an IC50 value of 200 nM.{18537} DAPT is also effective in vivo, reducing brain levels of Aβ when given orally to mice that are transgenic for human APPV717F or to rats.{18537,18534,18535} Through its effects on γ-secretase, DAPT indirectly inhibits Notch, affecting cell signaling and cell differentiation.{18536,18538}
Brand:CaymanSKU:- γ-Secretase is a multi-subunit aspartyl protease that cleaves amyloid precursor protein (APP) and many other type 1 transmembrane proteins, including Notch, E-cadherin, and ErbB4. The proteolysis of APP by secretases produces beta amyloid (Aβ), a 39- to 42-amino acid peptide which forms the amyloid plaques that are characteristic of Alzheimer’s disease. DAPT is an inhibitor of γ-secretase, blocking the production of total Aβ in human primary neuronal cultures with an IC50 value of 115 nM and Aβ42 with an IC50 value of 200 nM.{18537} DAPT is also effective in vivo, reducing brain levels of Aβ when given orally to mice that are transgenic for human APPV717F or to rats.{18537,18534,18535} Through its effects on γ-secretase, DAPT indirectly inhibits Notch, affecting cell signaling and cell differentiation.{18536,18538}
Brand:CaymanSKU:- γ-Secretase is a multi-subunit aspartyl protease that cleaves amyloid precursor protein (APP) and many other type 1 transmembrane proteins, including Notch, E-cadherin, and ErbB4. The proteolysis of APP by secretases produces beta amyloid (Aβ), a 39- to 42-amino acid peptide which forms the amyloid plaques that are characteristic of Alzheimer’s disease. DAPT is an inhibitor of γ-secretase, blocking the production of total Aβ in human primary neuronal cultures with an IC50 value of 115 nM and Aβ42 with an IC50 value of 200 nM.{18537} DAPT is also effective in vivo, reducing brain levels of Aβ when given orally to mice that are transgenic for human APPV717F or to rats.{18537,18534,18535} Through its effects on γ-secretase, DAPT indirectly inhibits Notch, affecting cell signaling and cell differentiation.{18536,18538}
Brand:CaymanSKU:- γ-Secretase is a multi-subunit aspartyl protease that cleaves amyloid precursor protein (APP) and many other type 1 transmembrane proteins, including Notch, E-cadherin, and ErbB4. The proteolysis of APP by secretases produces beta amyloid (Aβ), a 39- to 42-amino acid peptide which forms the amyloid plaques that are characteristic of Alzheimer’s disease. DAPT is an inhibitor of γ-secretase, blocking the production of total Aβ in human primary neuronal cultures with an IC50 value of 115 nM and Aβ42 with an IC50 value of 200 nM.{18537} DAPT is also effective in vivo, reducing brain levels of Aβ when given orally to mice that are transgenic for human APPV717F or to rats.{18537,18534,18535} Through its effects on γ-secretase, DAPT indirectly inhibits Notch, affecting cell signaling and cell differentiation.{18536,18538}
Brand:CaymanSKU:-
Daptomycin is a naturally occurring cyclic lipopeptide produced by the soil saprotroph S. roseosporus that is effective against resistant Gram-positive bacteria (MIC90s range from 0.25-16 mg/L).{25676,25675} It binds to bacterial plasma membranes to disrupt multiple aspects of function, including altering membrane potential and redirecting proteins essential for cell division and cell wall synthesis.{25675,25674}
Brand:CaymanSKU:- Daptomycin is a naturally occurring cyclic lipopeptide produced by the soil saprotroph S. roseosporus that is effective against resistant Gram-positive bacteria (MIC90s range from 0.25-16 mg/L).{25676,25675} It binds to bacterial plasma membranes to disrupt multiple aspects of function, including altering membrane potential and redirecting proteins essential for cell division and cell wall synthesis.{25675,25674}
Brand:CaymanSKU:- Daptomycin is a naturally occurring cyclic lipopeptide produced by the soil saprotroph S. roseosporus that is effective against resistant Gram-positive bacteria (MIC90s range from 0.25-16 mg/L).{25676,25675} It binds to bacterial plasma membranes to disrupt multiple aspects of function, including altering membrane potential and redirecting proteins essential for cell division and cell wall synthesis.{25675,25674}
Brand:CaymanSKU:- Daptomycin is a naturally occurring cyclic lipopeptide produced by the soil saprotroph S. roseosporus that is effective against resistant Gram-positive bacteria (MIC90s range from 0.25-16 mg/L).{25676,25675} It binds to bacterial plasma membranes to disrupt multiple aspects of function, including altering membrane potential and redirecting proteins essential for cell division and cell wall synthesis.{25675,25674}
Brand:CaymanSKU:-
Lipoprotein-associated phospholipase A2 (Lp-PLA2), also known as platelet activating factor acetylhydrolase (PAF-AH) or phospholipase A2 group 7 (PLA2G7), hydrolyzes glycerophospholipids to produce lyso-PAF/lyso-phosphatidylcholine and short and/or oxidized fatty acids, many of which have pro-inflammatory or pro-oxidative activities.{26682,26483} Darapladib is a reversible inhibitor of Lp-PLA2 (IC50 = 0.25 nM).{27391} It produces sustained inhibition of plasma Lp-PLA2 activity in humans receiving intensive atorvastatin therapy.{27387} Lp-PLA2 inhibition with darapladib also reduces the development of coronary atherosclerotic plaques.{27388,27390}
Brand:CaymanSKU:-Out of stock
Lipoprotein-associated phospholipase A2 (Lp-PLA2), also known as platelet activating factor acetylhydrolase (PAF-AH) or phospholipase A2 group 7 (PLA2G7), hydrolyzes glycerophospholipids to produce lyso-PAF/lyso-phosphatidylcholine and short and/or oxidized fatty acids, many of which have pro-inflammatory or pro-oxidative activities.{26682,26483} Darapladib is a reversible inhibitor of Lp-PLA2 (IC50 = 0.25 nM).{27391} It produces sustained inhibition of plasma Lp-PLA2 activity in humans receiving intensive atorvastatin therapy.{27387} Lp-PLA2 inhibition with darapladib also reduces the development of coronary atherosclerotic plaques.{27388,27390}
Brand:CaymanSKU:-Out of stock
Lipoprotein-associated phospholipase A2 (Lp-PLA2), also known as platelet activating factor acetylhydrolase (PAF-AH) or phospholipase A2 group 7 (PLA2G7), hydrolyzes glycerophospholipids to produce lyso-PAF/lyso-phosphatidylcholine and short and/or oxidized fatty acids, many of which have pro-inflammatory or pro-oxidative activities.{26682,26483} Darapladib is a reversible inhibitor of Lp-PLA2 (IC50 = 0.25 nM).{27391} It produces sustained inhibition of plasma Lp-PLA2 activity in humans receiving intensive atorvastatin therapy.{27387} Lp-PLA2 inhibition with darapladib also reduces the development of coronary atherosclerotic plaques.{27388,27390}
Brand:CaymanSKU:-Out of stock
Lipoprotein-associated phospholipase A2 (Lp-PLA2), also known as platelet activating factor acetylhydrolase (PAF-AH) or phospholipase A2 group 7 (PLA2G7), hydrolyzes glycerophospholipids to produce lyso-PAF/lyso-phosphatidylcholine and short and/or oxidized fatty acids, many of which have pro-inflammatory or pro-oxidative activities.{26682,26483} Darapladib is a reversible inhibitor of Lp-PLA2 (IC50 = 0.25 nM).{27391} It produces sustained inhibition of plasma Lp-PLA2 activity in humans receiving intensive atorvastatin therapy.{27387} Lp-PLA2 inhibition with darapladib also reduces the development of coronary atherosclerotic plaques.{27388,27390}
Brand:CaymanSKU:-Out of stock
Darifenacin is a receptor antagonist acting at the muscarinic receptors (Ki = 5.5, 47, 0.84, 8.6, and 2.3 nM for M1 through M5, respectively).{22962,22960} It is effective in treating problems related to the lower urinary tract, including incontinence and overactive bladder.{22959,22961}
Brand:CaymanSKU:- Darifenacin is a receptor antagonist acting at the muscarinic receptors (Ki = 5.5, 47, 0.84, 8.6, and 2.3 nM for M1 through M5, respectively).{22962,22960} It is effective in treating problems related to the lower urinary tract, including incontinence and overactive bladder.{22959,22961}
Brand:CaymanSKU:- Darifenacin is a receptor antagonist acting at the muscarinic receptors (Ki = 5.5, 47, 0.84, 8.6, and 2.3 nM for M1 through M5, respectively).{22962,22960} It is effective in treating problems related to the lower urinary tract, including incontinence and overactive bladder.{22959,22961}
Brand:CaymanSKU:- Darifenacin is a receptor antagonist acting at the muscarinic receptors (Ki = 5.5, 47, 0.84, 8.6, and 2.3 nM for M1 through M5, respectively).{22962,22960} It is effective in treating problems related to the lower urinary tract, including incontinence and overactive bladder.{22959,22961}
Brand:CaymanSKU:-
Darinaparsin is a dimethylated arsenic linked to glutathione. It is cytotoxic to DU145, LNCaP, and PC3 prostate cancer cells (IC50s = 5-10 µM) and patient-derived primary prostate cancer cells (IC50s = 2.5-20 µM), as well as Jurkat T cell lymphoma and L540 Hodgkin lymphoma cells (IC50s = 2.7 and 1.3 µM, respectively).{39852,39851} It decreases the tumor-initiating subpopulation in DU145 and PC3 cells and halts the cell cycle in the G2/M phase.{39852} Darinaparsin decreases transcription of Gli-2, a transcription factor that mediates Sonic hedgehog signaling, when used at a concentration of 1.5 but not 3 µM. It decreases SHP1 phosphatase activity and increases ERK phosphorylation.{39851} Darinaparsin reduces tumor growth in DU145 and PC3 prostate cancer mouse xenograft models when administered at a dose of 100 mg/kg every other day.{39852}
Brand:CaymanSKU:21659 -Out of stock
Darinaparsin is a dimethylated arsenic linked to glutathione. It is cytotoxic to DU145, LNCaP, and PC3 prostate cancer cells (IC50s = 5-10 µM) and patient-derived primary prostate cancer cells (IC50s = 2.5-20 µM), as well as Jurkat T cell lymphoma and L540 Hodgkin lymphoma cells (IC50s = 2.7 and 1.3 µM, respectively).{39852,39851} It decreases the tumor-initiating subpopulation in DU145 and PC3 cells and halts the cell cycle in the G2/M phase.{39852} Darinaparsin decreases transcription of Gli-2, a transcription factor that mediates Sonic hedgehog signaling, when used at a concentration of 1.5 but not 3 µM. It decreases SHP1 phosphatase activity and increases ERK phosphorylation.{39851} Darinaparsin reduces tumor growth in DU145 and PC3 prostate cancer mouse xenograft models when administered at a dose of 100 mg/kg every other day.{39852}
Brand:CaymanSKU:21659 -Out of stock
Darinaparsin is a dimethylated arsenic linked to glutathione. It is cytotoxic to DU145, LNCaP, and PC3 prostate cancer cells (IC50s = 5-10 µM) and patient-derived primary prostate cancer cells (IC50s = 2.5-20 µM), as well as Jurkat T cell lymphoma and L540 Hodgkin lymphoma cells (IC50s = 2.7 and 1.3 µM, respectively).{39852,39851} It decreases the tumor-initiating subpopulation in DU145 and PC3 cells and halts the cell cycle in the G2/M phase.{39852} Darinaparsin decreases transcription of Gli-2, a transcription factor that mediates Sonic hedgehog signaling, when used at a concentration of 1.5 but not 3 µM. It decreases SHP1 phosphatase activity and increases ERK phosphorylation.{39851} Darinaparsin reduces tumor growth in DU145 and PC3 prostate cancer mouse xenograft models when administered at a dose of 100 mg/kg every other day.{39852}
Brand:CaymanSKU:21659 -Out of stock
Darinaparsin is a dimethylated arsenic linked to glutathione. It is cytotoxic to DU145, LNCaP, and PC3 prostate cancer cells (IC50s = 5-10 µM) and patient-derived primary prostate cancer cells (IC50s = 2.5-20 µM), as well as Jurkat T cell lymphoma and L540 Hodgkin lymphoma cells (IC50s = 2.7 and 1.3 µM, respectively).{39852,39851} It decreases the tumor-initiating subpopulation in DU145 and PC3 cells and halts the cell cycle in the G2/M phase.{39852} Darinaparsin decreases transcription of Gli-2, a transcription factor that mediates Sonic hedgehog signaling, when used at a concentration of 1.5 but not 3 µM. It decreases SHP1 phosphatase activity and increases ERK phosphorylation.{39851} Darinaparsin reduces tumor growth in DU145 and PC3 prostate cancer mouse xenograft models when administered at a dose of 100 mg/kg every other day.{39852}
Brand:CaymanSKU:21659 -Out of stock
Darunavir is an HIV-1 protease inhibitor.{26076} It is active against HIV-1LAI in MT-2 cells (IC50 = 3 nM) with a cytotoxic concentration (CC50) of 74.4 μM. Darunavir is also active against wild-type and multidrug-resistant clinical isolates of HIV-1 in phytohemagglutinin-activated peripheral blood mononuclear cells (PHA-PBMCs; IC50s = 3 and 3-29 nM, respectively). It inhibits cell-free diffusion and cell-to-cell spread of HIV-1 in Jurkat cell populations (IC50s = 2.5 and 2.8 nM, respectively).{26075} Formulations containing darunavir have been used in combination therapy for the treatment of HIV.
Brand:CaymanSKU:- Darunavir is an HIV-1 protease inhibitor.{26076} It is active against HIV-1LAI in MT-2 cells (IC50 = 3 nM) with a cytotoxic concentration (CC50) of 74.4 μM. Darunavir is also active against wild-type and multidrug-resistant clinical isolates of HIV-1 in phytohemagglutinin-activated peripheral blood mononuclear cells (PHA-PBMCs; IC50s = 3 and 3-29 nM, respectively). It inhibits cell-free diffusion and cell-to-cell spread of HIV-1 in Jurkat cell populations (IC50s = 2.5 and 2.8 nM, respectively).{26075} Formulations containing darunavir have been used in combination therapy for the treatment of HIV.
Brand:CaymanSKU:- Darunavir is an HIV-1 protease inhibitor.{26076} It is active against HIV-1LAI in MT-2 cells (IC50 = 3 nM) with a cytotoxic concentration (CC50) of 74.4 μM. Darunavir is also active against wild-type and multidrug-resistant clinical isolates of HIV-1 in phytohemagglutinin-activated peripheral blood mononuclear cells (PHA-PBMCs; IC50s = 3 and 3-29 nM, respectively). It inhibits cell-free diffusion and cell-to-cell spread of HIV-1 in Jurkat cell populations (IC50s = 2.5 and 2.8 nM, respectively).{26075} Formulations containing darunavir have been used in combination therapy for the treatment of HIV.
Brand:CaymanSKU:-
Darunavir is an HIV-1 protease inhibitor.{26076} It is active against HIV-1LAI in MT-2 cells (IC50 = 3 nM) with a cytotoxic concentration (CC50) of 74.4 μM. Darunavir is also active against wild-type and multidrug-resistant clinical isolates of HIV-1 in phytohemagglutinin-activated peripheral blood mononuclear cells (PHA-PBMCs; IC50s = 3 and 3-29 nM, respectively). It inhibits cell-free diffusion and cell-to-cell spread of HIV-1 in Jurkat cell populations (IC50s = 2.5 and 2.8 nM, respectively).{26075} Formulations containing darunavir have been used in combination therapy for the treatment of HIV.
Brand:CaymanSKU:31083 - 10 mgAvailable on backorder
Darunavir is an HIV-1 protease inhibitor.{26076} It is active against HIV-1LAI in MT-2 cells (IC50 = 3 nM) with a cytotoxic concentration (CC50) of 74.4 μM. Darunavir is also active against wild-type and multidrug-resistant clinical isolates of HIV-1 in phytohemagglutinin-activated peripheral blood mononuclear cells (PHA-PBMCs; IC50s = 3 and 3-29 nM, respectively). It inhibits cell-free diffusion and cell-to-cell spread of HIV-1 in Jurkat cell populations (IC50s = 2.5 and 2.8 nM, respectively).{26075} Formulations containing darunavir have been used in combination therapy for the treatment of HIV.
Brand:CaymanSKU:31083 - 100 mgAvailable on backorder
Darunavir is an HIV-1 protease inhibitor.{26076} It is active against HIV-1LAI in MT-2 cells (IC50 = 3 nM) with a cytotoxic concentration (CC50) of 74.4 μM. Darunavir is also active against wild-type and multidrug-resistant clinical isolates of HIV-1 in phytohemagglutinin-activated peripheral blood mononuclear cells (PHA-PBMCs; IC50s = 3 and 3-29 nM, respectively). It inhibits cell-free diffusion and cell-to-cell spread of HIV-1 in Jurkat cell populations (IC50s = 2.5 and 2.8 nM, respectively).{26075} Formulations containing darunavir have been used in combination therapy for the treatment of HIV.
Brand:CaymanSKU:31083 - 25 mgAvailable on backorder
Darunavir is an HIV-1 protease inhibitor.{26076} It is active against HIV-1LAI in MT-2 cells (IC50 = 3 nM) with a cytotoxic concentration (CC50) of 74.4 μM. Darunavir is also active against wild-type and multidrug-resistant clinical isolates of HIV-1 in phytohemagglutinin-activated peripheral blood mononuclear cells (PHA-PBMCs; IC50s = 3 and 3-29 nM, respectively). It inhibits cell-free diffusion and cell-to-cell spread of HIV-1 in Jurkat cell populations (IC50s = 2.5 and 2.8 nM, respectively).{26075} Formulations containing darunavir have been used in combination therapy for the treatment of HIV.
Brand:CaymanSKU:31083 - 50 mgAvailable on backorder
Darunavir-d9 is intended for use as an internal standard for the quantification of darunavir (Item Nos. 15866 | 31083) by GC- or LC-MS. Darunavir is an HIV-1 protease inhibitor.{26076} It is active against HIV-1LAI in MT-2 cells (IC50 = 3 nM) with a cytotoxic concentration (CC50) of 74.4 μM. Darunavir is also active against wild-type and multidrug-resistant clinical isolates of HIV-1 in phytohemagglutinin-activated peripheral blood mononuclear cells (PHA-PBMCs; IC50s = 3 and 3-29 nM, respectively). It inhibits cell-free diffusion and cell-to-cell spread of HIV-1 in Jurkat cell populations (IC50s = 2.5 and 2.8 nM, respectively).{26075} Formulations containing darunavir have been used in combination therapy for the treatment of HIV.
Brand:CaymanSKU:25220 - 1 mgAvailable on backorder
DASA-58 is a selective activator of pyruvate kinase M2 (PKM2; AC50 = 38 nM in vitro, EC50 = 19.6 µM in cells).{21504} DASA-58 converts PKM2 to a constitutively active enzyme state that is resistant to inhibition by tyrosine-phosphorylated proteins.{21504} Through its effects on PKM2, DASA-58 blocks the induction of HIF-1α by lipopolysaccharide in bone marrow-derived macrophages, suppressing the expression of several HIF-1α-dependent targets, including IL-1β.{31878} It also impairs metastatic dissemination of prostate cancer PCa cells in SCID mice.{31877}
Brand:CaymanSKU:- DASA-58 is a selective activator of pyruvate kinase M2 (PKM2; AC50 = 38 nM in vitro, EC50 = 19.6 µM in cells).{21504} DASA-58 converts PKM2 to a constitutively active enzyme state that is resistant to inhibition by tyrosine-phosphorylated proteins.{21504} Through its effects on PKM2, DASA-58 blocks the induction of HIF-1α by lipopolysaccharide in bone marrow-derived macrophages, suppressing the expression of several HIF-1α-dependent targets, including IL-1β.{31878} It also impairs metastatic dissemination of prostate cancer PCa cells in SCID mice.{31877}
Brand:CaymanSKU:- DASA-58 is a selective activator of pyruvate kinase M2 (PKM2; AC50 = 38 nM in vitro, EC50 = 19.6 µM in cells).{21504} DASA-58 converts PKM2 to a constitutively active enzyme state that is resistant to inhibition by tyrosine-phosphorylated proteins.{21504} Through its effects on PKM2, DASA-58 blocks the induction of HIF-1α by lipopolysaccharide in bone marrow-derived macrophages, suppressing the expression of several HIF-1α-dependent targets, including IL-1β.{31878} It also impairs metastatic dissemination of prostate cancer PCa cells in SCID mice.{31877}
Brand:CaymanSKU:-
Dasatinib is a potent inhibitor of the non-receptor tyrosine kinases Abl and Src as well as other members of the Src family.{24166,24167} It is effective at sub-nanomolar concentrations, inhibiting Src, Abl, and Lck with IC50 values of 0.05, 0.5, and 0.4 nM, respectively.{24166,24156,24168} At nanomolar concentrations, dasatinib also blocks the activity of several other receptor and non-receptor tyrosine kinases, plus drug resistant mutants.{24156,24168} Because of these activities, dasatinib has potential therapeutic value in diseases that are characterized by elevated levels of these kinases, including some forms of cancer and fibrotic disease.{24166,24164,17350,17482}
Brand:CaymanSKU:11498 - 10 mgAvailable on backorder
Dasatinib is a potent inhibitor of the non-receptor tyrosine kinases Abl and Src as well as other members of the Src family.{24166,24167} It is effective at sub-nanomolar concentrations, inhibiting Src, Abl, and Lck with IC50 values of 0.05, 0.5, and 0.4 nM, respectively.{24166,24156,24168} At nanomolar concentrations, dasatinib also blocks the activity of several other receptor and non-receptor tyrosine kinases, plus drug resistant mutants.{24156,24168} Because of these activities, dasatinib has potential therapeutic value in diseases that are characterized by elevated levels of these kinases, including some forms of cancer and fibrotic disease.{24166,24164,17350,17482}
Brand:CaymanSKU:11498 - 100 mgAvailable on backorder
Dasatinib is a potent inhibitor of the non-receptor tyrosine kinases Abl and Src as well as other members of the Src family.{24166,24167} It is effective at sub-nanomolar concentrations, inhibiting Src, Abl, and Lck with IC50 values of 0.05, 0.5, and 0.4 nM, respectively.{24166,24156,24168} At nanomolar concentrations, dasatinib also blocks the activity of several other receptor and non-receptor tyrosine kinases, plus drug resistant mutants.{24156,24168} Because of these activities, dasatinib has potential therapeutic value in diseases that are characterized by elevated levels of these kinases, including some forms of cancer and fibrotic disease.{24166,24164,17350,17482}
Brand:CaymanSKU:11498 - 250 mgAvailable on backorder
Dasatinib is a potent inhibitor of the non-receptor tyrosine kinases Abl and Src as well as other members of the Src family.{24166,24167} It is effective at sub-nanomolar concentrations, inhibiting Src, Abl, and Lck with IC50 values of 0.05, 0.5, and 0.4 nM, respectively.{24166,24156,24168} At nanomolar concentrations, dasatinib also blocks the activity of several other receptor and non-receptor tyrosine kinases, plus drug resistant mutants.{24156,24168} Because of these activities, dasatinib has potential therapeutic value in diseases that are characterized by elevated levels of these kinases, including some forms of cancer and fibrotic disease.{24166,24164,17350,17482}
Brand:CaymanSKU:11498 - 50 mgAvailable on backorder
Dasatinib N-oxide is a major metabolite of the Abl and Src kinase inhibitor dasatinib (Item No. 11498).{45424} It is also a potential impurity in commercial preparations of dasatinib.{45425}
Brand:CaymanSKU:27845 - 1 mgAvailable on backorder
Dasatinib N-oxide is a major metabolite of the Abl and Src kinase inhibitor dasatinib (Item No. 11498).{45424} It is also a potential impurity in commercial preparations of dasatinib.{45425}
Brand:CaymanSKU:27845 - 10 mgAvailable on backorder
Dasatinib N-oxide is a major metabolite of the Abl and Src kinase inhibitor dasatinib (Item No. 11498).{45424} It is also a potential impurity in commercial preparations of dasatinib.{45425}
Brand:CaymanSKU:27845 - 5 mgAvailable on backorder
Dasatinib-d8 is intended for use as an internal standard for the quantification of dasatinib (Item No. 11498) by GC- or LC-MS. Dasatinib is a potent inhibitor of the non-receptor tyrosine kinases Abl and Src as well as other members of the Src family.{24166,24167} It is effective at sub-nanomolar concentrations, inhibiting Src, Abl, and Lck with IC50 values of 0.05, 0.5, and 0.4 nM, respectively.{24166,24156,24168} At nanomolar concentrations, dasatinib also blocks the activity of several other receptor and non-receptor tyrosine kinases, plus drug-resistant mutants.{24156,24168} Because of these activities, dasatinib has potential therapeutic value in diseases characterized by elevated levels of these kinases, including some forms of cancer and fibrotic disease.{24166,24164,17350,17482}
Brand:CaymanSKU:22368 -Out of stock
Dasatinib-d8 is intended for use as an internal standard for the quantification of dasatinib (Item No. 11498) by GC- or LC-MS. Dasatinib is a potent inhibitor of the non-receptor tyrosine kinases Abl and Src as well as other members of the Src family.{24166,24167} It is effective at sub-nanomolar concentrations, inhibiting Src, Abl, and Lck with IC50 values of 0.05, 0.5, and 0.4 nM, respectively.{24166,24156,24168} At nanomolar concentrations, dasatinib also blocks the activity of several other receptor and non-receptor tyrosine kinases, plus drug-resistant mutants.{24156,24168} Because of these activities, dasatinib has potential therapeutic value in diseases characterized by elevated levels of these kinases, including some forms of cancer and fibrotic disease.{24166,24164,17350,17482}
Brand:CaymanSKU:22368 -Out of stock
DAUDA is an environment-sensitive fluorescent fatty acid analogue that alters its fluorescent emission spectra and intensities on entry into binding proteins. DAUDA has been used to determine the relative affinity of natural fatty acids for polymorphs of the Schistosoma mansoni Sm14 fatty acid-binding protein by monitoring excitation and emission at 345 and 543 nM, respectively.{14648}
Brand:CaymanSKU:10005188 - 100 mgAvailable on backorder
DAUDA is an environment-sensitive fluorescent fatty acid analogue that alters its fluorescent emission spectra and intensities on entry into binding proteins. DAUDA has been used to determine the relative affinity of natural fatty acids for polymorphs of the Schistosoma mansoni Sm14 fatty acid-binding protein by monitoring excitation and emission at 345 and 543 nM, respectively.{14648}
Brand:CaymanSKU:10005188 - 25 mgAvailable on backorder
DAUDA is an environment-sensitive fluorescent fatty acid analogue that alters its fluorescent emission spectra and intensities on entry into binding proteins. DAUDA has been used to determine the relative affinity of natural fatty acids for polymorphs of the Schistosoma mansoni Sm14 fatty acid-binding protein by monitoring excitation and emission at 345 and 543 nM, respectively.{14648}
Brand:CaymanSKU:10005188 - 50 mgAvailable on backorder
Daunorubicin is an antitumor antibiotic.{22542} At 0.2-1μM, daunorubicin induces apoptosis in mature monocytic U937 and myelocytic HL-60 acute myeloid leukemia (AML) cells. However, immature AML cells (CD 34+-KG1a, -KG1, or -HEL cells) appear resistant to apoptosis at similar concentrations.{22542} In mature AML cells, daunorubicin has been shown to trigger a reactive oxygen species-dependent sphingomyelin-ceramide pathway that activates the MEKK1-SEK1-JNK cascade leading to enhanced DNA binding activity of the transcription factor AP-1.{22542,5396}
Brand:CaymanSKU:- Daunorubicin is an antitumor antibiotic.{22542} At 0.2-1μM, daunorubicin induces apoptosis in mature monocytic U937 and myelocytic HL-60 acute myeloid leukemia (AML) cells. However, immature AML cells (CD 34+-KG1a, -KG1, or -HEL cells) appear resistant to apoptosis at similar concentrations.{22542} In mature AML cells, daunorubicin has been shown to trigger a reactive oxygen species-dependent sphingomyelin-ceramide pathway that activates the MEKK1-SEK1-JNK cascade leading to enhanced DNA binding activity of the transcription factor AP-1.{22542,5396}
Brand:CaymanSKU:- Daunorubicin is an antitumor antibiotic.{22542} At 0.2-1μM, daunorubicin induces apoptosis in mature monocytic U937 and myelocytic HL-60 acute myeloid leukemia (AML) cells. However, immature AML cells (CD 34+-KG1a, -KG1, or -HEL cells) appear resistant to apoptosis at similar concentrations.{22542} In mature AML cells, daunorubicin has been shown to trigger a reactive oxygen species-dependent sphingomyelin-ceramide pathway that activates the MEKK1-SEK1-JNK cascade leading to enhanced DNA binding activity of the transcription factor AP-1.{22542,5396}
Brand:CaymanSKU:- Daunorubicin is an antitumor antibiotic.{22542} At 0.2-1μM, daunorubicin induces apoptosis in mature monocytic U937 and myelocytic HL-60 acute myeloid leukemia (AML) cells. However, immature AML cells (CD 34+-KG1a, -KG1, or -HEL cells) appear resistant to apoptosis at similar concentrations.{22542} In mature AML cells, daunorubicin has been shown to trigger a reactive oxygen species-dependent sphingomyelin-ceramide pathway that activates the MEKK1-SEK1-JNK cascade leading to enhanced DNA binding activity of the transcription factor AP-1.{22542,5396}
Brand:CaymanSKU:-
Daurisoline is an alkaloid that has been found in M. dauricum and has diverse biological activities.{46756,46758,46759} It enhances cytotoxicity induced by camptothecin (Item No. 11694) in HeLa cells when used at a concentration of 10 µM.{46756} Daurisoline inhibits camptothecin-induced autophagy in HeLa, A549, and HCT116 cells (IC50s = 74.75, 50.54, and 80.81 μM, respectively). It inhibits ADP-induced aggregation of platelets in isolated rabbit whole blood (IC50 = 100 µM).{46758} Daurisoline prolongs action potential duration (APD) and reduces early afterdepolarizations (EADs) in papillary muscle preparations isolated from hypertrophied rabbit hearts when used at a concentration of 15 µM.{46759}
Brand:CaymanSKU:29628 - 10 mgAvailable on backorder
Daurisoline is an alkaloid that has been found in M. dauricum and has diverse biological activities.{46756,46758,46759} It enhances cytotoxicity induced by camptothecin (Item No. 11694) in HeLa cells when used at a concentration of 10 µM.{46756} Daurisoline inhibits camptothecin-induced autophagy in HeLa, A549, and HCT116 cells (IC50s = 74.75, 50.54, and 80.81 μM, respectively). It inhibits ADP-induced aggregation of platelets in isolated rabbit whole blood (IC50 = 100 µM).{46758} Daurisoline prolongs action potential duration (APD) and reduces early afterdepolarizations (EADs) in papillary muscle preparations isolated from hypertrophied rabbit hearts when used at a concentration of 15 µM.{46759}
Brand:CaymanSKU:29628 - 25 mgAvailable on backorder
Daurisoline is an alkaloid that has been found in M. dauricum and has diverse biological activities.{46756,46758,46759} It enhances cytotoxicity induced by camptothecin (Item No. 11694) in HeLa cells when used at a concentration of 10 µM.{46756} Daurisoline inhibits camptothecin-induced autophagy in HeLa, A549, and HCT116 cells (IC50s = 74.75, 50.54, and 80.81 μM, respectively). It inhibits ADP-induced aggregation of platelets in isolated rabbit whole blood (IC50 = 100 µM).{46758} Daurisoline prolongs action potential duration (APD) and reduces early afterdepolarizations (EADs) in papillary muscle preparations isolated from hypertrophied rabbit hearts when used at a concentration of 15 µM.{46759}
Brand:CaymanSKU:29628 - 5 mgAvailable on backorder
Daurisoline is an alkaloid that has been found in M. dauricum and has diverse biological activities.{46756,46758,46759} It enhances cytotoxicity induced by camptothecin (Item No. 11694) in HeLa cells when used at a concentration of 10 µM.{46756} Daurisoline inhibits camptothecin-induced autophagy in HeLa, A549, and HCT116 cells (IC50s = 74.75, 50.54, and 80.81 μM, respectively). It inhibits ADP-induced aggregation of platelets in isolated rabbit whole blood (IC50 = 100 µM).{46758} Daurisoline prolongs action potential duration (APD) and reduces early afterdepolarizations (EADs) in papillary muscle preparations isolated from hypertrophied rabbit hearts when used at a concentration of 15 µM.{46759}
Brand:CaymanSKU:29628 - 50 mgAvailable on backorder
Davercin is a macrolide antibiotic that inhibits bacterial protein synthesis by targeting the 50S ribosomal subunit, blocking the progression of nascent polypeptide chains.{42015} It has broad-spectrum activity against various Gram-positive and Gram-negative bacteria (MICs = 0.02-50 μg/ml). Davercin is non-toxic to mice and rats (LD50s = 4.05 and 5.9 g/kg, respectively). Formulations containing davercin have been used to treat a variety of urogenital bacterial infections.
Brand:CaymanSKU:21348 -Out of stock
Davercin is a macrolide antibiotic that inhibits bacterial protein synthesis by targeting the 50S ribosomal subunit, blocking the progression of nascent polypeptide chains.{42015} It has broad-spectrum activity against various Gram-positive and Gram-negative bacteria (MICs = 0.02-50 μg/ml). Davercin is non-toxic to mice and rats (LD50s = 4.05 and 5.9 g/kg, respectively). Formulations containing davercin have been used to treat a variety of urogenital bacterial infections.
Brand:CaymanSKU:21348 -Out of stock
Davercin is a macrolide antibiotic that inhibits bacterial protein synthesis by targeting the 50S ribosomal subunit, blocking the progression of nascent polypeptide chains.{42015} It has broad-spectrum activity against various Gram-positive and Gram-negative bacteria (MICs = 0.02-50 μg/ml). Davercin is non-toxic to mice and rats (LD50s = 4.05 and 5.9 g/kg, respectively). Formulations containing davercin have been used to treat a variety of urogenital bacterial infections.
Brand:CaymanSKU:21348 -Out of stock
Davercin is a macrolide antibiotic that inhibits bacterial protein synthesis by targeting the 50S ribosomal subunit, blocking the progression of nascent polypeptide chains.{42015} It has broad-spectrum activity against various Gram-positive and Gram-negative bacteria (MICs = 0.02-50 μg/ml). Davercin is non-toxic to mice and rats (LD50s = 4.05 and 5.9 g/kg, respectively). Formulations containing davercin have been used to treat a variety of urogenital bacterial infections.
Brand:CaymanSKU:21348 -Out of stock
Redox-sensitive cysteine residues in proteins may function as sensors of reactive oxygen species (ROS) and also serve as molecular switches, activating or deactivating proteins, following a change in oxidation state. Modification of protein function through the reversible oxidation of cysteine is emerging as a biologically relevant signal transduction mechanism. Sulfenic acid is the initial oxidation product of cysteine by relatively mild oxidizing agents such as hydrogen peroxide. Sulfenic acid can be reduced back to the free thiol or be further oxidized to sulfinic and sulfonic acids.{16654} DAz-1 is a cell-permeable chemical probe that reacts specifically with sulfenic acid-modified proteins.{16660,16658} The azido group of DAz-1 provides a method for selective conjugation to phosphine- or alkynyl- derivatized reagents, such as biotin or various fluorophores, for subsequent analysis of the labeled proteins. DAz-1 is a less sensitive probe for sulfenic acid detection compared to its analog DAz-2 (Item No. 13382).{17444}
Brand:CaymanSKU:- Redox-sensitive cysteine residues in proteins may function as sensors of reactive oxygen species (ROS) and also serve as molecular switches, activating or deactivating proteins, following a change in oxidation state. Modification of protein function through the reversible oxidation of cysteine is emerging as a biologically relevant signal transduction mechanism. Sulfenic acid is the initial oxidation product of cysteine by relatively mild oxidizing agents such as hydrogen peroxide. Sulfenic acid can be reduced back to the free thiol or be further oxidized to sulfinic and sulfonic acids.{16654} DAz-1 is a cell-permeable chemical probe that reacts specifically with sulfenic acid-modified proteins.{16660,16658} The azido group of DAz-1 provides a method for selective conjugation to phosphine- or alkynyl- derivatized reagents, such as biotin or various fluorophores, for subsequent analysis of the labeled proteins. DAz-1 is a less sensitive probe for sulfenic acid detection compared to its analog DAz-2 (Item No. 13382).{17444}
Brand:CaymanSKU:- Redox-sensitive cysteine residues in proteins may function as sensors of reactive oxygen species (ROS) and also serve as molecular switches, activating or deactivating proteins, following a change in oxidation state. Modification of protein function through the reversible oxidation of cysteine is emerging as a biologically relevant signal transduction mechanism. Sulfenic acid is the initial oxidation product of cysteine by relatively mild oxidizing agents such as hydrogen peroxide. Sulfenic acid can be reduced back to the free thiol or be further oxidized to sulfinic and sulfonic acids.{16654} DAz-1 is a cell-permeable chemical probe that reacts specifically with sulfenic acid-modified proteins.{16660,16658} The azido group of DAz-1 provides a method for selective conjugation to phosphine- or alkynyl- derivatized reagents, such as biotin or various fluorophores, for subsequent analysis of the labeled proteins. DAz-1 is a less sensitive probe for sulfenic acid detection compared to its analog DAz-2 (Item No. 13382).{17444}
Brand:CaymanSKU:-
DAz-2 is a cell-permeable chemical probe used to detect cysteine oxidation in proteins. Redox-sensitive cysteine residues in proteins may function as sensors of reactive oxygen species (ROS) and also serve as molecular switches, activating or deactivating proteins, following a change in oxidation state. Modification of protein function through the reversible oxidation of cysteine is emerging as a biologically relevant signal transduction mechanism. Sulfenic acid is the initial oxidation product of cysteine by relatively mild oxidizing agents such as hydrogen peroxide. Sulfenic acid can be reduced back to the free thiol or be further oxidized to sulfinic and sulfonic acids.{16654} DAz-2 is a cell-permeable chemical probe that reacts specifically with sulfenic acid-modified proteins.{17444} The azido group of DAz-2 provides a method for selective conjugation to phosphine- or alkynyl- derivatized reagents, such as biotin or various fluorophores, for subsequent analysis of the labeled proteins. Use of DAz-2 in HeLa cells followed by Staudinger ligation to biotin and subsequent LC-MS/MS analysis, led to the identification of 193 sulfenic acid-modified proteins having a diverse range of functions.{17444}
Brand:CaymanSKU:- DAz-2 is a cell-permeable chemical probe used to detect cysteine oxidation in proteins. Redox-sensitive cysteine residues in proteins may function as sensors of reactive oxygen species (ROS) and also serve as molecular switches, activating or deactivating proteins, following a change in oxidation state. Modification of protein function through the reversible oxidation of cysteine is emerging as a biologically relevant signal transduction mechanism. Sulfenic acid is the initial oxidation product of cysteine by relatively mild oxidizing agents such as hydrogen peroxide. Sulfenic acid can be reduced back to the free thiol or be further oxidized to sulfinic and sulfonic acids.{16654} DAz-2 is a cell-permeable chemical probe that reacts specifically with sulfenic acid-modified proteins.{17444} The azido group of DAz-2 provides a method for selective conjugation to phosphine- or alkynyl- derivatized reagents, such as biotin or various fluorophores, for subsequent analysis of the labeled proteins. Use of DAz-2 in HeLa cells followed by Staudinger ligation to biotin and subsequent LC-MS/MS analysis, led to the identification of 193 sulfenic acid-modified proteins having a diverse range of functions.{17444}
Brand:CaymanSKU:- DAz-2 is a cell-permeable chemical probe used to detect cysteine oxidation in proteins. Redox-sensitive cysteine residues in proteins may function as sensors of reactive oxygen species (ROS) and also serve as molecular switches, activating or deactivating proteins, following a change in oxidation state. Modification of protein function through the reversible oxidation of cysteine is emerging as a biologically relevant signal transduction mechanism. Sulfenic acid is the initial oxidation product of cysteine by relatively mild oxidizing agents such as hydrogen peroxide. Sulfenic acid can be reduced back to the free thiol or be further oxidized to sulfinic and sulfonic acids.{16654} DAz-2 is a cell-permeable chemical probe that reacts specifically with sulfenic acid-modified proteins.{17444} The azido group of DAz-2 provides a method for selective conjugation to phosphine- or alkynyl- derivatized reagents, such as biotin or various fluorophores, for subsequent analysis of the labeled proteins. Use of DAz-2 in HeLa cells followed by Staudinger ligation to biotin and subsequent LC-MS/MS analysis, led to the identification of 193 sulfenic acid-modified proteins having a diverse range of functions.{17444}
Brand:CaymanSKU:-
DB07268 is a potent inhibitor of JNK1 (IC50 = 9 nM) that binds to the ATP site of JNK1.{40395} It is selective for JNK1 over P38, ERK2, AKT1, CHK1, and PAK4 among others. DB07268 did not reduce phosphorylation of insulin resistance substrate 1 (IRS-1) in HEK293 cells.{40396}
Brand:CaymanSKU:22257 -Out of stock
DB07268 is a potent inhibitor of JNK1 (IC50 = 9 nM) that binds to the ATP site of JNK1.{40395} It is selective for JNK1 over P38, ERK2, AKT1, CHK1, and PAK4 among others. DB07268 did not reduce phosphorylation of insulin resistance substrate 1 (IRS-1) in HEK293 cells.{40396}
Brand:CaymanSKU:22257 -Out of stock
DB07268 is a potent inhibitor of JNK1 (IC50 = 9 nM) that binds to the ATP site of JNK1.{40395} It is selective for JNK1 over P38, ERK2, AKT1, CHK1, and PAK4 among others. DB07268 did not reduce phosphorylation of insulin resistance substrate 1 (IRS-1) in HEK293 cells.{40396}
Brand:CaymanSKU:22257 -Out of stock
DB07268 is a potent inhibitor of JNK1 (IC50 = 9 nM) that binds to the ATP site of JNK1.{40395} It is selective for JNK1 over P38, ERK2, AKT1, CHK1, and PAK4 among others. DB07268 did not reduce phosphorylation of insulin resistance substrate 1 (IRS-1) in HEK293 cells.{40396}
Brand:CaymanSKU:22257 -Out of stock
The ATPase p97 is an ubiquitin-selective chaperone known to play a critical role in the degradation of misfolded membrane and secretory proteins and has been linked to various cellular processes that require unfolding and disassembly of protein complexes.{24975} DBeQ is a selective, reversible, and ATP-competitive inhibitor of the ATPase p97 (Ki = 3.2 μM; IC50 = 1.5 μM).{24976} It does not exhibit activity when tested against a panel 170 protein kinases at concentrations as high as 15 μM.{24976} At 10 μM it blocks endoplasmic reticulum-associated degradation, impairing the autophagy pathway and promoting the activation of caspase-3 and -7 in cancer cells.{24976}
Brand:CaymanSKU:- The ATPase p97 is an ubiquitin-selective chaperone known to play a critical role in the degradation of misfolded membrane and secretory proteins and has been linked to various cellular processes that require unfolding and disassembly of protein complexes.{24975} DBeQ is a selective, reversible, and ATP-competitive inhibitor of the ATPase p97 (Ki = 3.2 μM; IC50 = 1.5 μM).{24976} It does not exhibit activity when tested against a panel 170 protein kinases at concentrations as high as 15 μM.{24976} At 10 μM it blocks endoplasmic reticulum-associated degradation, impairing the autophagy pathway and promoting the activation of caspase-3 and -7 in cancer cells.{24976}
Brand:CaymanSKU:- The ATPase p97 is an ubiquitin-selective chaperone known to play a critical role in the degradation of misfolded membrane and secretory proteins and has been linked to various cellular processes that require unfolding and disassembly of protein complexes.{24975} DBeQ is a selective, reversible, and ATP-competitive inhibitor of the ATPase p97 (Ki = 3.2 μM; IC50 = 1.5 μM).{24976} It does not exhibit activity when tested against a panel 170 protein kinases at concentrations as high as 15 μM.{24976} At 10 μM it blocks endoplasmic reticulum-associated degradation, impairing the autophagy pathway and promoting the activation of caspase-3 and -7 in cancer cells.{24976}
Brand:CaymanSKU:- The ATPase p97 is an ubiquitin-selective chaperone known to play a critical role in the degradation of misfolded membrane and secretory proteins and has been linked to various cellular processes that require unfolding and disassembly of protein complexes.{24975} DBeQ is a selective, reversible, and ATP-competitive inhibitor of the ATPase p97 (Ki = 3.2 μM; IC50 = 1.5 μM).{24976} It does not exhibit activity when tested against a panel 170 protein kinases at concentrations as high as 15 μM.{24976} At 10 μM it blocks endoplasmic reticulum-associated degradation, impairing the autophagy pathway and promoting the activation of caspase-3 and -7 in cancer cells.{24976}
Brand:CaymanSKU:-
dBET1 is a hybrid molecule that combines (+)-JQ1 (Item No. 11187) and thalidomide (Item No. 14610).{29054} The JQ1 portion facilitates binding of dBET1 to the bromodomains of BET family transcriptional activators. The thalidomide moiety drives proteasomal degradation, as phthalimides bind cereblon to create a substrate recognition site for E3 protein ligase complex-mediated ubiquitination. dBET1 induces cereblon-dependent BET protein degradation in vitro (EC50 = 430 nM) and in vivo and delays leukemia progression in mice.
Brand:CaymanSKU:-Available on backorder
dBET1 is a hybrid molecule that combines (+)-JQ1 (Item No. 11187) and thalidomide (Item No. 14610).{29054} The JQ1 portion facilitates binding of dBET1 to the bromodomains of BET family transcriptional activators. The thalidomide moiety drives proteasomal degradation, as phthalimides bind cereblon to create a substrate recognition site for E3 protein ligase complex-mediated ubiquitination. dBET1 induces cereblon-dependent BET protein degradation in vitro (EC50 = 430 nM) and in vivo and delays leukemia progression in mice.
Brand:CaymanSKU:-Available on backorder
dBET1 is a hybrid molecule that combines (+)-JQ1 (Item No. 11187) and thalidomide (Item No. 14610).{29054} The JQ1 portion facilitates binding of dBET1 to the bromodomains of BET family transcriptional activators. The thalidomide moiety drives proteasomal degradation, as phthalimides bind cereblon to create a substrate recognition site for E3 protein ligase complex-mediated ubiquitination. dBET1 induces cereblon-dependent BET protein degradation in vitro (EC50 = 430 nM) and in vivo and delays leukemia progression in mice.
Brand:CaymanSKU:-Available on backorder
The lysophosphatidic acid (LPA) receptor LPA2 is a G protein-coupled receptor that has roles in protecting against radiation-induced cell death.{29230} DBIBB is a non-lipid agonist of LPA2 (EC50 = 0.10 µM) that is without effect at other LPA receptor subtypes.{28449} It protects rat intestinal crypt epithelium-like IEC-6 cells against caspase 3/7 activation and apoptosis following irradiation.{28449} DBIBB dose-dependently attenuates radiation-induced DNA damage in mouse embryo fibroblasts (MEFs) expressing LPA2 but not in MEFs lacking this receptor.{28449} It also increases the survival of mice suffering from hematopoietic acute radiation syndrome after total-body irradiation.{28449}
Brand:CaymanSKU:-Available on backorder
The lysophosphatidic acid (LPA) receptor LPA2 is a G protein-coupled receptor that has roles in protecting against radiation-induced cell death.{29230} DBIBB is a non-lipid agonist of LPA2 (EC50 = 0.10 µM) that is without effect at other LPA receptor subtypes.{28449} It protects rat intestinal crypt epithelium-like IEC-6 cells against caspase 3/7 activation and apoptosis following irradiation.{28449} DBIBB dose-dependently attenuates radiation-induced DNA damage in mouse embryo fibroblasts (MEFs) expressing LPA2 but not in MEFs lacking this receptor.{28449} It also increases the survival of mice suffering from hematopoietic acute radiation syndrome after total-body irradiation.{28449}
Brand:CaymanSKU:-Available on backorder