Chemicals
Showing 18751–18900 of 41137 results
-
Epinastine is a histamine H1 receptor antagonist (Kiapps = 1.41 and 1.62 nM using guinea pig cerebellar and lung membranes, respectively) and mast cell stabilizer.{48871,48872} It inhibits IgE-induced histamine, TNF-α, and IL-10 secretion in human cord blood stem cell-derived mast cells (CBMCs) when used at a concentration of 0.1 μg/ml.{48872} Epinastine inhibits histamine-induced cutaneous vascular permeability in rats and bronchoconstriction in anesthetized guinea pigs (ID50s = 5 and 0.1 mg/kg, respectively).{11338} It inhibits dye leakage into the conjunctiva in a rat model of passive anaphylaxis reaction-induced vascular hyperpermeability of the conjunctiva (ID50 = 9.7 mg/kg, p.o.).{48873} Topical administration of formulations containing epinastine (0.05% three times per day) reduces lid edema, tearing, and redness, as well as the number of neutrophils and eosinophils in the lid fornix, in a mouse model of atopic conjunctivitis.{48872} Formulations containing epinastine have been used in the prevention of itching associated with allergic conjunctivitis.
Brand:CaymanSKU:-Available on backorder
Epinastine is a histamine H1 receptor antagonist (Kiapps = 1.41 and 1.62 nM using guinea pig cerebellar and lung membranes, respectively) and mast cell stabilizer.{48871,48872} It inhibits IgE-induced histamine, TNF-α, and IL-10 secretion in human cord blood stem cell-derived mast cells (CBMCs) when used at a concentration of 0.1 μg/ml.{48872} Epinastine inhibits histamine-induced cutaneous vascular permeability in rats and bronchoconstriction in anesthetized guinea pigs (ID50s = 5 and 0.1 mg/kg, respectively).{11338} It inhibits dye leakage into the conjunctiva in a rat model of passive anaphylaxis reaction-induced vascular hyperpermeability of the conjunctiva (ID50 = 9.7 mg/kg, p.o.).{48873} Topical administration of formulations containing epinastine (0.05% three times per day) reduces lid edema, tearing, and redness, as well as the number of neutrophils and eosinophils in the lid fornix, in a mouse model of atopic conjunctivitis.{48872} Formulations containing epinastine have been used in the prevention of itching associated with allergic conjunctivitis.
Brand:CaymanSKU:-Available on backorder
Epinastine is a histamine H1 receptor antagonist (Kiapps = 1.41 and 1.62 nM using guinea pig cerebellar and lung membranes, respectively) and mast cell stabilizer.{48871,48872} It inhibits IgE-induced histamine, TNF-α, and IL-10 secretion in human cord blood stem cell-derived mast cells (CBMCs) when used at a concentration of 0.1 μg/ml.{48872} Epinastine inhibits histamine-induced cutaneous vascular permeability in rats and bronchoconstriction in anesthetized guinea pigs (ID50s = 5 and 0.1 mg/kg, respectively).{11338} It inhibits dye leakage into the conjunctiva in a rat model of passive anaphylaxis reaction-induced vascular hyperpermeability of the conjunctiva (ID50 = 9.7 mg/kg, p.o.).{48873} Topical administration of formulations containing epinastine (0.05% three times per day) reduces lid edema, tearing, and redness, as well as the number of neutrophils and eosinophils in the lid fornix, in a mouse model of atopic conjunctivitis.{48872} Formulations containing epinastine have been used in the prevention of itching associated with allergic conjunctivitis.
Brand:CaymanSKU:-Available on backorder
Epioxytetracycline is a degradation product of the antibiotic oxytetracycline (Item No. 18076).{48330,48331} It has been found in swine manure compost and wastewater and is considered a pollutant.
Brand:CaymanSKU:27987 - 1 mgAvailable on backorder
Epioxytetracycline is a degradation product of the antibiotic oxytetracycline (Item No. 18076).{48330,48331} It has been found in swine manure compost and wastewater and is considered a pollutant.
Brand:CaymanSKU:27987 - 10 mgAvailable on backorder
Epioxytetracycline is a degradation product of the antibiotic oxytetracycline (Item No. 18076).{48330,48331} It has been found in swine manure compost and wastewater and is considered a pollutant.
Brand:CaymanSKU:27987 - 5 mgAvailable on backorder
Epirubicin is a stereoisomer of the antitumor anthracycline doxorubicin (Item No. 15007) that undergoes β-glucuronidation, which partially detoxifies the dose-limiting side effects that are present with doxorubicin.{22870} Compared to doxorubicin, epirubicin is equally cytotoxic to HeLa cells (ID50s = 9 μM).{22870} When used either alone or in combination therapies, epirubicin has been shown to demonstrate high rates of complete or partial remission in various cancers including advanced ovary, lymphomas, breast, pancreas, gastric, hepatocellular carcinoma, head and neck tumors, and colorectal.{22870,20978}
Brand:CaymanSKU:12091 - 10 mgAvailable on backorder
Epirubicin is a stereoisomer of the antitumor anthracycline doxorubicin (Item No. 15007) that undergoes β-glucuronidation, which partially detoxifies the dose-limiting side effects that are present with doxorubicin.{22870} Compared to doxorubicin, epirubicin is equally cytotoxic to HeLa cells (ID50s = 9 μM).{22870} When used either alone or in combination therapies, epirubicin has been shown to demonstrate high rates of complete or partial remission in various cancers including advanced ovary, lymphomas, breast, pancreas, gastric, hepatocellular carcinoma, head and neck tumors, and colorectal.{22870,20978}
Brand:CaymanSKU:12091 - 100 mgAvailable on backorder
Epirubicin is a stereoisomer of the antitumor anthracycline doxorubicin (Item No. 15007) that undergoes β-glucuronidation, which partially detoxifies the dose-limiting side effects that are present with doxorubicin.{22870} Compared to doxorubicin, epirubicin is equally cytotoxic to HeLa cells (ID50s = 9 μM).{22870} When used either alone or in combination therapies, epirubicin has been shown to demonstrate high rates of complete or partial remission in various cancers including advanced ovary, lymphomas, breast, pancreas, gastric, hepatocellular carcinoma, head and neck tumors, and colorectal.{22870,20978}
Brand:CaymanSKU:12091 - 25 mgAvailable on backorder
Epirubicin is a stereoisomer of the antitumor anthracycline doxorubicin (Item No. 15007) that undergoes β-glucuronidation, which partially detoxifies the dose-limiting side effects that are present with doxorubicin.{22870} Compared to doxorubicin, epirubicin is equally cytotoxic to HeLa cells (ID50s = 9 μM).{22870} When used either alone or in combination therapies, epirubicin has been shown to demonstrate high rates of complete or partial remission in various cancers including advanced ovary, lymphomas, breast, pancreas, gastric, hepatocellular carcinoma, head and neck tumors, and colorectal.{22870,20978}
Brand:CaymanSKU:12091 - 5 mgAvailable on backorder
Epitalon is a synthetic tetrapeptide with anti-aging properties.{46381,46382,46383,46384} Dietary administration of epitalon (0.00001% w/w) reduces levels of lipid peroxidation products in aged D. melanogaster tissue homogenates.{46381} Epitalon (1 μg/animal) delays age-related estrous shutdown and decreases the frequency of bone marrow cell chromosomal aberrations in female mice.{46382} It decreases spontaneous mammary gland and ovarian tumor development and metastasis in aged female mice.{46383} Epitalon also stimulates melatonin synthesis and normalizes the circadian rhythm of cortisol secretion in senescent female M. mulatta monkeys.{46384}
Brand:CaymanSKU:27463 - 10 mgAvailable on backorder
Epitalon is a synthetic tetrapeptide with anti-aging properties.{46381,46382,46383,46384} Dietary administration of epitalon (0.00001% w/w) reduces levels of lipid peroxidation products in aged D. melanogaster tissue homogenates.{46381} Epitalon (1 μg/animal) delays age-related estrous shutdown and decreases the frequency of bone marrow cell chromosomal aberrations in female mice.{46382} It decreases spontaneous mammary gland and ovarian tumor development and metastasis in aged female mice.{46383} Epitalon also stimulates melatonin synthesis and normalizes the circadian rhythm of cortisol secretion in senescent female M. mulatta monkeys.{46384}
Brand:CaymanSKU:27463 - 100 mgAvailable on backorder
Epitalon is a synthetic tetrapeptide with anti-aging properties.{46381,46382,46383,46384} Dietary administration of epitalon (0.00001% w/w) reduces levels of lipid peroxidation products in aged D. melanogaster tissue homogenates.{46381} Epitalon (1 μg/animal) delays age-related estrous shutdown and decreases the frequency of bone marrow cell chromosomal aberrations in female mice.{46382} It decreases spontaneous mammary gland and ovarian tumor development and metastasis in aged female mice.{46383} Epitalon also stimulates melatonin synthesis and normalizes the circadian rhythm of cortisol secretion in senescent female M. mulatta monkeys.{46384}
Brand:CaymanSKU:27463 - 250 mgAvailable on backorder
Epitalon is a synthetic tetrapeptide with anti-aging properties.{46381,46382,46383,46384} Dietary administration of epitalon (0.00001% w/w) reduces levels of lipid peroxidation products in aged D. melanogaster tissue homogenates.{46381} Epitalon (1 μg/animal) delays age-related estrous shutdown and decreases the frequency of bone marrow cell chromosomal aberrations in female mice.{46382} It decreases spontaneous mammary gland and ovarian tumor development and metastasis in aged female mice.{46383} Epitalon also stimulates melatonin synthesis and normalizes the circadian rhythm of cortisol secretion in senescent female M. mulatta monkeys.{46384}
Brand:CaymanSKU:27463 - 50 mgAvailable on backorder
Epitetracycline is an epimer of the antibiotic tetracycline (Item No. 14328). Epimers of tetracycline form without catalysis and are considered degradation products.{17511,33081} Epitetracycline has decreased activity as an antibiotic or a Tet repressor effector but may have stronger toxic effects in animals.{17511,33081}
Brand:CaymanSKU:-Available on backorder
Epitetracycline is an epimer of the antibiotic tetracycline (Item No. 14328). Epimers of tetracycline form without catalysis and are considered degradation products.{17511,33081} Epitetracycline has decreased activity as an antibiotic or a Tet repressor effector but may have stronger toxic effects in animals.{17511,33081}
Brand:CaymanSKU:-Available on backorder
Epitetracycline is an epimer of the antibiotic tetracycline (Item No. 14328). Epimers of tetracycline form without catalysis and are considered degradation products.{17511,33081} Epitetracycline has decreased activity as an antibiotic or a Tet repressor effector but may have stronger toxic effects in animals.{17511,33081}
Brand:CaymanSKU:-Available on backorder
Epitetracycline is an epimer of the antibiotic tetracycline (Item No. 14328). Epimers of tetracycline form without catalysis and are considered degradation products.{17511,33081} Epitetracycline has decreased activity as an antibiotic or a Tet repressor effector but may have stronger toxic effects in animals.{17511,33081}
Brand:CaymanSKU:-Available on backorder
Eplerenone (Item No. 26302) is an analytical reference standard categorized as a diuretic.{33139,48162} It has been detected as an adverse analytical finding (AAF) during anti-doping testing.{48164} This product is intended for use in analytical forensic applications. This product is also available as a general research tool (Item No. 15616).
Brand:CaymanSKU:26302 - 1 mgAvailable on backorder
Eplerenone is a mineralocorticoid receptor antagonist.{18724} It is selective for the mineralocorticoid receptor over glucocorticoid, androgen, progesterone, and estrogen receptors in radioligand binding assays (IC50s = 138, 6,920, 523, >10,000, and 5,702 nM, respectively). Eplerenone inhibits aldosterone-induced mineralocorticoid activity in a luciferase assay (IC50 = 122 nM). In vivo, eplerenone (100 mg/kg per day) reduces urinary albumin secretion and glomerulosclerosis in the Dahl salt-sensitive rat model of hypertension and nephropathy. It reduces myocardial IL-1β levels and collagen deposition, as well as improves left ventricular systolic dysfunction in a mouse model of acute myocardial infarction.{59183} Formulations containing eplerenone have been used in the treatment of hypertension and heart failure after myocardial infarction.
Brand:CaymanSKU:- Eplerenone is a mineralocorticoid receptor antagonist.{18724} It is selective for the mineralocorticoid receptor over glucocorticoid, androgen, progesterone, and estrogen receptors in radioligand binding assays (IC50s = 138, 6,920, 523, >10,000, and 5,702 nM, respectively). Eplerenone inhibits aldosterone-induced mineralocorticoid activity in a luciferase assay (IC50 = 122 nM). In vivo, eplerenone (100 mg/kg per day) reduces urinary albumin secretion and glomerulosclerosis in the Dahl salt-sensitive rat model of hypertension and nephropathy. It reduces myocardial IL-1β levels and collagen deposition, as well as improves left ventricular systolic dysfunction in a mouse model of acute myocardial infarction.{59183} Formulations containing eplerenone have been used in the treatment of hypertension and heart failure after myocardial infarction.
Brand:CaymanSKU:- Eplerenone is a mineralocorticoid receptor antagonist.{18724} It is selective for the mineralocorticoid receptor over glucocorticoid, androgen, progesterone, and estrogen receptors in radioligand binding assays (IC50s = 138, 6,920, 523, >10,000, and 5,702 nM, respectively). Eplerenone inhibits aldosterone-induced mineralocorticoid activity in a luciferase assay (IC50 = 122 nM). In vivo, eplerenone (100 mg/kg per day) reduces urinary albumin secretion and glomerulosclerosis in the Dahl salt-sensitive rat model of hypertension and nephropathy. It reduces myocardial IL-1β levels and collagen deposition, as well as improves left ventricular systolic dysfunction in a mouse model of acute myocardial infarction.{59183} Formulations containing eplerenone have been used in the treatment of hypertension and heart failure after myocardial infarction.
Brand:CaymanSKU:- Eplerenone (Item No. 26302) is an analytical reference standard categorized as a diuretic.{33139,48162} It has been detected as an adverse analytical finding (AAF) during anti-doping testing.{48164} This product is intended for use in analytical forensic applications. This product is also available as a general research tool (Item No. 15616).
Brand:CaymanSKU:26302 - 5 mgAvailable on backorder
Eplerenone is a mineralocorticoid receptor antagonist.{18724} It is selective for the mineralocorticoid receptor over glucocorticoid, androgen, progesterone, and estrogen receptors in radioligand binding assays (IC50s = 138, 6,920, 523, >10,000, and 5,702 nM, respectively). Eplerenone inhibits aldosterone-induced mineralocorticoid activity in a luciferase assay (IC50 = 122 nM). In vivo, eplerenone (100 mg/kg per day) reduces urinary albumin secretion and glomerulosclerosis in the Dahl salt-sensitive rat model of hypertension and nephropathy. It reduces myocardial IL-1β levels and collagen deposition, as well as improves left ventricular systolic dysfunction in a mouse model of acute myocardial infarction.{59183} Formulations containing eplerenone have been used in the treatment of hypertension and heart failure after myocardial infarction.
Brand:CaymanSKU:-
Epothilone A (Epo A) is a biologically active macrolide produced from the fermentation of the soil bacteria S. cellulosum that was discovered as a potent antimicrotubule agent.{26908,19711,19714} In competition assays, epo A binds to β-tubulin with a similar order of magnitude as the binding of paclitaxel (Item No. 10461) to β-tubulin (IC50s = 2.3 and 3.6 µM, respectively).{26908,19711,19714,19713} Epo A is cytotoxic to human T-24 bladder carcinoma cells (IC50 = 0.05 µM in vitro) but has poor pharmacological properties and is 2-fold less potent in stabilizing microtubules compared to epothilone B (Item No. 10924).{26908}
Brand:CaymanSKU:-Out of stock
Epothilone A (Epo A) is a biologically active macrolide produced from the fermentation of the soil bacteria S. cellulosum that was discovered as a potent antimicrotubule agent.{26908,19711,19714} In competition assays, epo A binds to β-tubulin with a similar order of magnitude as the binding of paclitaxel (Item No. 10461) to β-tubulin (IC50s = 2.3 and 3.6 µM, respectively).{26908,19711,19714,19713} Epo A is cytotoxic to human T-24 bladder carcinoma cells (IC50 = 0.05 µM in vitro) but has poor pharmacological properties and is 2-fold less potent in stabilizing microtubules compared to epothilone B (Item No. 10924).{26908}
Brand:CaymanSKU:-Out of stock
Epothilone A (Epo A) is a biologically active macrolide produced from the fermentation of the soil bacteria S. cellulosum that was discovered as a potent antimicrotubule agent.{26908,19711,19714} In competition assays, epo A binds to β-tubulin with a similar order of magnitude as the binding of paclitaxel (Item No. 10461) to β-tubulin (IC50s = 2.3 and 3.6 µM, respectively).{26908,19711,19714,19713} Epo A is cytotoxic to human T-24 bladder carcinoma cells (IC50 = 0.05 µM in vitro) but has poor pharmacological properties and is 2-fold less potent in stabilizing microtubules compared to epothilone B (Item No. 10924).{26908}
Brand:CaymanSKU:-Out of stock
Epothilone B (Epo B) is a macrolide that causes the formation of bundles of intracellular microtubules in non-mitotic cells, induces the formation of hyperstable tubulin polymers, and arrests cell cycling in mitosis.{19711,19713} It induces mitotic arrest at the G2-M transition in Hs578T and HeLa cells (IC50 = 3 and 32 nM, respectively) as well as in multidrug resistant KB3-1 and KBV-1 cells (IC50 = 16 and 92 nM, respectively).{19711} Epo B causes cell cycle arrest at nanomolar IC50 values in cell lines from ovarian, breast, lung, colon, prostate, and squamous cancer.{19714}
Brand:CaymanSKU:10924 - 1 mgAvailable on backorder
Epothilone B (Epo B) is a macrolide that causes the formation of bundles of intracellular microtubules in non-mitotic cells, induces the formation of hyperstable tubulin polymers, and arrests cell cycling in mitosis.{19711,19713} It induces mitotic arrest at the G2-M transition in Hs578T and HeLa cells (IC50 = 3 and 32 nM, respectively) as well as in multidrug resistant KB3-1 and KBV-1 cells (IC50 = 16 and 92 nM, respectively).{19711} Epo B causes cell cycle arrest at nanomolar IC50 values in cell lines from ovarian, breast, lung, colon, prostate, and squamous cancer.{19714}
Brand:CaymanSKU:10924 - 10 mgAvailable on backorder
Epothilone B (Epo B) is a macrolide that causes the formation of bundles of intracellular microtubules in non-mitotic cells, induces the formation of hyperstable tubulin polymers, and arrests cell cycling in mitosis.{19711,19713} It induces mitotic arrest at the G2-M transition in Hs578T and HeLa cells (IC50 = 3 and 32 nM, respectively) as well as in multidrug resistant KB3-1 and KBV-1 cells (IC50 = 16 and 92 nM, respectively).{19711} Epo B causes cell cycle arrest at nanomolar IC50 values in cell lines from ovarian, breast, lung, colon, prostate, and squamous cancer.{19714}
Brand:CaymanSKU:10924 - 5 mgAvailable on backorder
Epothilones are microtubule-stabilizing agents with potential anti-neoplastic actions.{19711,19714,26908} They are natural macrolides that have high potency in both taxane-sensitive and taxane-resistant models.{19714,26908} Epothilone D is a desoxy form of epothilone B (Item No. 10924) that inhibits the growth of a variety of cancer cells both in vitro (IC50 values range from 0.97 to 21 nM) and in mice.{26908,30210} Epothilone D is brain penetrant and reduces neurodegeneration in aged tau transgenic mice.{30209,30212} Effects include improved axonal transport, decreased tau neuropathology, and reduced hippocampal neuron loss.{30209,30212} Epothilone D also rescues microtubule defects and attenuates nigrostriatal degeneration in a mouse model of Parkinson’s disease.{30210}
Brand:CaymanSKU:-Available on backorder
Epothilones are microtubule-stabilizing agents with potential anti-neoplastic actions.{19711,19714,26908} They are natural macrolides that have high potency in both taxane-sensitive and taxane-resistant models.{19714,26908} Epothilone D is a desoxy form of epothilone B (Item No. 10924) that inhibits the growth of a variety of cancer cells both in vitro (IC50 values range from 0.97 to 21 nM) and in mice.{26908,30210} Epothilone D is brain penetrant and reduces neurodegeneration in aged tau transgenic mice.{30209,30212} Effects include improved axonal transport, decreased tau neuropathology, and reduced hippocampal neuron loss.{30209,30212} Epothilone D also rescues microtubule defects and attenuates nigrostriatal degeneration in a mouse model of Parkinson’s disease.{30210}
Brand:CaymanSKU:-Available on backorder
Epothilones are microtubule-stabilizing agents with potential anti-neoplastic actions.{19711,19714,26908} They are natural macrolides that have high potency in both taxane-sensitive and taxane-resistant models.{19714,26908} Epothilone D is a desoxy form of epothilone B (Item No. 10924) that inhibits the growth of a variety of cancer cells both in vitro (IC50 values range from 0.97 to 21 nM) and in mice.{26908,30210} Epothilone D is brain penetrant and reduces neurodegeneration in aged tau transgenic mice.{30209,30212} Effects include improved axonal transport, decreased tau neuropathology, and reduced hippocampal neuron loss.{30209,30212} Epothilone D also rescues microtubule defects and attenuates nigrostriatal degeneration in a mouse model of Parkinson’s disease.{30210}
Brand:CaymanSKU:-Available on backorder
Epothilones are microtubule-stabilizing agents with potential anti-neoplastic actions.{19711,19714,26908} They are natural macrolides that have high potency in both taxane-sensitive and taxane-resistant models.{19714,26908} Epothilone D is a desoxy form of epothilone B (Item No. 10924) that inhibits the growth of a variety of cancer cells both in vitro (IC50 values range from 0.97 to 21 nM) and in mice.{26908,30210} Epothilone D is brain penetrant and reduces neurodegeneration in aged tau transgenic mice.{30209,30212} Effects include improved axonal transport, decreased tau neuropathology, and reduced hippocampal neuron loss.{30209,30212} Epothilone D also rescues microtubule defects and attenuates nigrostriatal degeneration in a mouse model of Parkinson’s disease.{30210}
Brand:CaymanSKU:-Available on backorder
Epoxomicin is a potent anti-tumor agent isolated from Actinomycetes that is used as a selective and irreversible inhibitor of the 20S proteasome. It inhibits proteasome activity in cell growth assays with an IC50 value of 4 nM and demonstrates potent cytotoxicity against B16-F10, HCT116, and Moser solid tumor cells, as well as P388 and K562 leukemia cells with IC50 values ranging from 2-44 nM.{13359,13358} By inhibiting osteoblast proteasome activity, epoxomicin stimulates bone formation at concentrations as low as 10 nM.{13351} Intraperitoneal injection of 1.5 mg/kg epoxomicin given daily for two weeks induces Parkinson’s-like symptoms in rats and addition of 100 nM epoxomicin to rat ventral midbrain cultures results in apoptosis specific to dopaminergic neurons.{13355,16504} Epoxomicin-induced parkinsonism can be a useful model to examine mechanisms and therapies for the disease.
Brand:CaymanSKU:10007806 - 100 µgAvailable on backorder
Epoxomicin is a potent anti-tumor agent isolated from Actinomycetes that is used as a selective and irreversible inhibitor of the 20S proteasome. It inhibits proteasome activity in cell growth assays with an IC50 value of 4 nM and demonstrates potent cytotoxicity against B16-F10, HCT116, and Moser solid tumor cells, as well as P388 and K562 leukemia cells with IC50 values ranging from 2-44 nM.{13359,13358} By inhibiting osteoblast proteasome activity, epoxomicin stimulates bone formation at concentrations as low as 10 nM.{13351} Intraperitoneal injection of 1.5 mg/kg epoxomicin given daily for two weeks induces Parkinson’s-like symptoms in rats and addition of 100 nM epoxomicin to rat ventral midbrain cultures results in apoptosis specific to dopaminergic neurons.{13355,16504} Epoxomicin-induced parkinsonism can be a useful model to examine mechanisms and therapies for the disease.
Brand:CaymanSKU:10007806 - 25 µgAvailable on backorder
Epoxomicin is a potent anti-tumor agent isolated from Actinomycetes that is used as a selective and irreversible inhibitor of the 20S proteasome. It inhibits proteasome activity in cell growth assays with an IC50 value of 4 nM and demonstrates potent cytotoxicity against B16-F10, HCT116, and Moser solid tumor cells, as well as P388 and K562 leukemia cells with IC50 values ranging from 2-44 nM.{13359,13358} By inhibiting osteoblast proteasome activity, epoxomicin stimulates bone formation at concentrations as low as 10 nM.{13351} Intraperitoneal injection of 1.5 mg/kg epoxomicin given daily for two weeks induces Parkinson’s-like symptoms in rats and addition of 100 nM epoxomicin to rat ventral midbrain cultures results in apoptosis specific to dopaminergic neurons.{13355,16504} Epoxomicin-induced parkinsonism can be a useful model to examine mechanisms and therapies for the disease.
Brand:CaymanSKU:10007806 - 250 µgAvailable on backorder
Epoxomicin is a potent anti-tumor agent isolated from Actinomycetes that is used as a selective and irreversible inhibitor of the 20S proteasome. It inhibits proteasome activity in cell growth assays with an IC50 value of 4 nM and demonstrates potent cytotoxicity against B16-F10, HCT116, and Moser solid tumor cells, as well as P388 and K562 leukemia cells with IC50 values ranging from 2-44 nM.{13359,13358} By inhibiting osteoblast proteasome activity, epoxomicin stimulates bone formation at concentrations as low as 10 nM.{13351} Intraperitoneal injection of 1.5 mg/kg epoxomicin given daily for two weeks induces Parkinson’s-like symptoms in rats and addition of 100 nM epoxomicin to rat ventral midbrain cultures results in apoptosis specific to dopaminergic neurons.{13355,16504} Epoxomicin-induced parkinsonism can be a useful model to examine mechanisms and therapies for the disease.
Brand:CaymanSKU:10007806 - 50 µgAvailable on backorder
Soluble epoxide hydrolase (sEH) catalyzes the conversion of epoxyeicosatrienoic acids (EpETrEs) to the corresponding DiHETrEs thereby diminishing their vasodilator activity.{12607} Inhibitors of sEH may therefore have clinical utility for treating hypertension and systemic inflammation.{14065,14072} Epoxy fluor 7 is a sensitive fluorescent substrate for soluble epoxide hydrolase (sEH) that can be used to monitor the activity of both human and mouse enzymes.{14078} Hydrolysis of the substrate epoxide yields a highly fluorescent product that can be monitored at excitation and emission wavelengths of 330 and 465 nm, respectively. Epoxy fluor 7 is more stable in aqueous solution and offers about 2-fold better sensitivity than previously used colorimetric substrates such as NEPC.{14078}
Brand:CaymanSKU:10008610 - 1 mgAvailable on backorder
Soluble epoxide hydrolase (sEH) catalyzes the conversion of epoxyeicosatrienoic acids (EpETrEs) to the corresponding DiHETrEs thereby diminishing their vasodilator activity.{12607} Inhibitors of sEH may therefore have clinical utility for treating hypertension and systemic inflammation.{14065,14072} Epoxy fluor 7 is a sensitive fluorescent substrate for soluble epoxide hydrolase (sEH) that can be used to monitor the activity of both human and mouse enzymes.{14078} Hydrolysis of the substrate epoxide yields a highly fluorescent product that can be monitored at excitation and emission wavelengths of 330 and 465 nm, respectively. Epoxy fluor 7 is more stable in aqueous solution and offers about 2-fold better sensitivity than previously used colorimetric substrates such as NEPC.{14078}
Brand:CaymanSKU:10008610 - 10 mgAvailable on backorder
Soluble epoxide hydrolase (sEH) catalyzes the conversion of epoxyeicosatrienoic acids (EpETrEs) to the corresponding DiHETrEs thereby diminishing their vasodilator activity.{12607} Inhibitors of sEH may therefore have clinical utility for treating hypertension and systemic inflammation.{14065,14072} Epoxy fluor 7 is a sensitive fluorescent substrate for soluble epoxide hydrolase (sEH) that can be used to monitor the activity of both human and mouse enzymes.{14078} Hydrolysis of the substrate epoxide yields a highly fluorescent product that can be monitored at excitation and emission wavelengths of 330 and 465 nm, respectively. Epoxy fluor 7 is more stable in aqueous solution and offers about 2-fold better sensitivity than previously used colorimetric substrates such as NEPC.{14078}
Brand:CaymanSKU:10008610 - 5 mgAvailable on backorder
Soluble epoxide hydrolase (sEH) catalyzes the conversion of epoxyeicosatrienoic acids (EpETrEs) to the corresponding DiHETrEs thereby diminishing their vasodilator activity.{12607} Inhibitors of sEH may therefore have clinical utility for treating hypertension and systemic inflammation.{14065,14072} Epoxy fluor 7 is a sensitive fluorescent substrate for soluble epoxide hydrolase (sEH) that can be used to monitor the activity of both human and mouse enzymes.{14078} Hydrolysis of the substrate epoxide yields a highly fluorescent product that can be monitored at excitation and emission wavelengths of 330 and 465 nm, respectively. Epoxy fluor 7 is more stable in aqueous solution and offers about 2-fold better sensitivity than previously used colorimetric substrates such as NEPC.{14078}
Brand:CaymanSKU:10008610 - 50 mgAvailable on backorder
Eprinomectin is an avermectin with anthelmintic and insecticidal activities.{42898} It is comprised of eprinomectin B1a (Item No. 28130) and eprinomectin B1b (Item No. 27994).{27367} Eprinomectin (≥0.08 mg/kg, applied topically) reduces worm burden by 99% or more in bovine models of adult H. placei, O. ostertagi, T. axei, Cooperia punctata, N. helvetianus, O. radiatum, or D. viviparus infection.{42898} It also reduces parasite burden in bovine models of horn fly (H. irritans) or mange mite (C. bovis) infestation, as well as in cows naturally infested with lice (L. vituli), when applied topically at doses ranging from 0.16 to 0.5 mg/kg. Formulations containing eprinomectin have been used in the treatment and control of a variety of endo- and ectoparasites in cattle.
Brand:CaymanSKU:28182 - 100 mgAvailable on backorder
Eprinomectin is an avermectin with anthelmintic and insecticidal activities.{42898} It is comprised of eprinomectin B1a (Item No. 28130) and eprinomectin B1b (Item No. 27994).{27367} Eprinomectin (≥0.08 mg/kg, applied topically) reduces worm burden by 99% or more in bovine models of adult H. placei, O. ostertagi, T. axei, Cooperia punctata, N. helvetianus, O. radiatum, or D. viviparus infection.{42898} It also reduces parasite burden in bovine models of horn fly (H. irritans) or mange mite (C. bovis) infestation, as well as in cows naturally infested with lice (L. vituli), when applied topically at doses ranging from 0.16 to 0.5 mg/kg. Formulations containing eprinomectin have been used in the treatment and control of a variety of endo- and ectoparasites in cattle.
Brand:CaymanSKU:28182 - 50 mgAvailable on backorder
Eprinomectin B1a is a major component (>90%) of the antiparasitic compound eprinomectin, which also contains eprinomectin B1b (27994) and belongs to the avermectin family of insecticides and anthelmintics.{47367}
Brand:CaymanSKU:28130 - 1 mgAvailable on backorder
Eprinomectin B1a is a major component (>90%) of the antiparasitic compound eprinomectin, which also contains eprinomectin B1b (27994) and belongs to the avermectin family of insecticides and anthelmintics.{47367}
Brand:CaymanSKU:28130 - 5 mgAvailable on backorder
Eprinomectin B1b is a minor component (1a (>90%; Item No. 28130) and belongs to the avermectin family of insecticides and anthelmintics.{47367}
Brand:CaymanSKU:27994 - 2.5 mgAvailable on backorder
Eprinomectin B1b is a minor component (1a (>90%; Item No. 28130) and belongs to the avermectin family of insecticides and anthelmintics.{47367}
Brand:CaymanSKU:27994 - 500 µgAvailable on backorder
Angiotensin II, as part of the renin-angiotensin-aldosterone system, facilitates a sympathetic nervous system response mediated by the angiotensin II type 1 (AT1) receptor, causing vasoconstriction and subsequent increase in blood pressure. It potentiates noradrenaline release from sympathetic nerve terminals at the presynaptic level as well as amplifies the α-adrenoceptor-mediated vasoconstrictor response to endogenous noradrenaline. Angiotensin II receptor blockers (ARBs) are a major class of therapeutics designed to lower blood pressure and to provide cardiovascular protection.{20999,21000} Eprosartan (mesylate) is a competitive AT1 receptor antagonist with IC50 values ranging from 1.4 – 3.9 nM and an elimination half-life of five to seven hours.{21001} Eprosartan is structurally distinct from other noncompetitive ARBs in that it does not contain a biphenyl, tetrazole moiety and blocks angiotensin II receptors on both sympathetic nerve terminals and blood vessels.{21000}
Brand:CaymanSKU:11578 - 10 mgAvailable on backorder
Angiotensin II, as part of the renin-angiotensin-aldosterone system, facilitates a sympathetic nervous system response mediated by the angiotensin II type 1 (AT1) receptor, causing vasoconstriction and subsequent increase in blood pressure. It potentiates noradrenaline release from sympathetic nerve terminals at the presynaptic level as well as amplifies the α-adrenoceptor-mediated vasoconstrictor response to endogenous noradrenaline. Angiotensin II receptor blockers (ARBs) are a major class of therapeutics designed to lower blood pressure and to provide cardiovascular protection.{20999,21000} Eprosartan (mesylate) is a competitive AT1 receptor antagonist with IC50 values ranging from 1.4 – 3.9 nM and an elimination half-life of five to seven hours.{21001} Eprosartan is structurally distinct from other noncompetitive ARBs in that it does not contain a biphenyl, tetrazole moiety and blocks angiotensin II receptors on both sympathetic nerve terminals and blood vessels.{21000}
Brand:CaymanSKU:11578 - 100 mgAvailable on backorder
Angiotensin II, as part of the renin-angiotensin-aldosterone system, facilitates a sympathetic nervous system response mediated by the angiotensin II type 1 (AT1) receptor, causing vasoconstriction and subsequent increase in blood pressure. It potentiates noradrenaline release from sympathetic nerve terminals at the presynaptic level as well as amplifies the α-adrenoceptor-mediated vasoconstrictor response to endogenous noradrenaline. Angiotensin II receptor blockers (ARBs) are a major class of therapeutics designed to lower blood pressure and to provide cardiovascular protection.{20999,21000} Eprosartan (mesylate) is a competitive AT1 receptor antagonist with IC50 values ranging from 1.4 – 3.9 nM and an elimination half-life of five to seven hours.{21001} Eprosartan is structurally distinct from other noncompetitive ARBs in that it does not contain a biphenyl, tetrazole moiety and blocks angiotensin II receptors on both sympathetic nerve terminals and blood vessels.{21000}
Brand:CaymanSKU:11578 - 50 mgAvailable on backorder
EPT (Item No. 27323) is an analytical reference standard categorized as a tryptamine. This product is intended for research and forensic applications.
Brand:CaymanSKU:27323 - 1 mgAvailable on backorder
EPT (Item No. 27323) is an analytical reference standard categorized as a tryptamine. This product is intended for research and forensic applications.
Brand:CaymanSKU:27323 - 5 mgAvailable on backorder
Eptapirone is a potent agonist of the serotonin (5-HT) receptor subtype 5-HT1A (Ki = 4.8 nM in a radioligand binding assay).{41165} It is selective for 5-HT1A over other 5-HT receptor subtypes, dopamine D2 receptors, α1-adrenergic receptors, and histamine H1 receptors (Kis = 11018) in HA7 cells transfected with human 5-HT1A receptors (EC50 = 158 nM). In vivo, eptapirone increases extracellular 5-HT (Item No. 14332) in the ventral hippocampus of rats (ED50 = 0.049 mg/kg) and serum corticosterone (Item No. 16063) levels when administered p.o. or i.p. (ED50s = 0.16 and 0.057 mg/kg, respectively). It decreases immobility in rats in a forced swim test and increases punished responding in a pigeon conflict procedure, demonstrating antidepressant-like and anxiolytic activity. Eptapirone (2.5 mg/kg, p.o.) also attenuates hypertension and tachycardia induced by sibutramine (Item No. 14476) in rats with no effect on sibutramine-induced hypophagia.{41166}
Brand:CaymanSKU:23449 - 1 mgAvailable on backorder
Eptapirone is a potent agonist of the serotonin (5-HT) receptor subtype 5-HT1A (Ki = 4.8 nM in a radioligand binding assay).{41165} It is selective for 5-HT1A over other 5-HT receptor subtypes, dopamine D2 receptors, α1-adrenergic receptors, and histamine H1 receptors (Kis = 11018) in HA7 cells transfected with human 5-HT1A receptors (EC50 = 158 nM). In vivo, eptapirone increases extracellular 5-HT (Item No. 14332) in the ventral hippocampus of rats (ED50 = 0.049 mg/kg) and serum corticosterone (Item No. 16063) levels when administered p.o. or i.p. (ED50s = 0.16 and 0.057 mg/kg, respectively). It decreases immobility in rats in a forced swim test and increases punished responding in a pigeon conflict procedure, demonstrating antidepressant-like and anxiolytic activity. Eptapirone (2.5 mg/kg, p.o.) also attenuates hypertension and tachycardia induced by sibutramine (Item No. 14476) in rats with no effect on sibutramine-induced hypophagia.{41166}
Brand:CaymanSKU:23449 - 10 mgAvailable on backorder
Eptapirone is a potent agonist of the serotonin (5-HT) receptor subtype 5-HT1A (Ki = 4.8 nM in a radioligand binding assay).{41165} It is selective for 5-HT1A over other 5-HT receptor subtypes, dopamine D2 receptors, α1-adrenergic receptors, and histamine H1 receptors (Kis = 11018) in HA7 cells transfected with human 5-HT1A receptors (EC50 = 158 nM). In vivo, eptapirone increases extracellular 5-HT (Item No. 14332) in the ventral hippocampus of rats (ED50 = 0.049 mg/kg) and serum corticosterone (Item No. 16063) levels when administered p.o. or i.p. (ED50s = 0.16 and 0.057 mg/kg, respectively). It decreases immobility in rats in a forced swim test and increases punished responding in a pigeon conflict procedure, demonstrating antidepressant-like and anxiolytic activity. Eptapirone (2.5 mg/kg, p.o.) also attenuates hypertension and tachycardia induced by sibutramine (Item No. 14476) in rats with no effect on sibutramine-induced hypophagia.{41166}
Brand:CaymanSKU:23449 - 25 mgAvailable on backorder
Eptapirone is a potent agonist of the serotonin (5-HT) receptor subtype 5-HT1A (Ki = 4.8 nM in a radioligand binding assay).{41165} It is selective for 5-HT1A over other 5-HT receptor subtypes, dopamine D2 receptors, α1-adrenergic receptors, and histamine H1 receptors (Kis = 11018) in HA7 cells transfected with human 5-HT1A receptors (EC50 = 158 nM). In vivo, eptapirone increases extracellular 5-HT (Item No. 14332) in the ventral hippocampus of rats (ED50 = 0.049 mg/kg) and serum corticosterone (Item No. 16063) levels when administered p.o. or i.p. (ED50s = 0.16 and 0.057 mg/kg, respectively). It decreases immobility in rats in a forced swim test and increases punished responding in a pigeon conflict procedure, demonstrating antidepressant-like and anxiolytic activity. Eptapirone (2.5 mg/kg, p.o.) also attenuates hypertension and tachycardia induced by sibutramine (Item No. 14476) in rats with no effect on sibutramine-induced hypophagia.{41166}
Brand:CaymanSKU:23449 - 5 mgAvailable on backorder
Eptifibatide is a potent glycoprotein IIb/IIIa antagonist (GPIIb/IIIa; Kd = 120 nM) that inhibits platelet aggregation.{38053,38054} Eptifibatide prevents binding of the adhesion proteins fibrinogen and von Willebrand factor to GPIIb/IIIa on the surface of activated platelets to prevent aggregation and thrombus formation.{38055} It inhibits ADP-induced citrated blood aggregation (IC50 = 0.11-0.22 μg/ml) in vitro and in vivo (IC50 = 52 μg/ml in porcine plasma).{38053,38056} Formulations containing eptifibatide have been used to reduce risk of thrombolysis in myocardial infarction in patients undergoing percutaneous coronary intervention.{38057}
Brand:CaymanSKU:21578 -Out of stock
Eptifibatide is a potent glycoprotein IIb/IIIa antagonist (GPIIb/IIIa; Kd = 120 nM) that inhibits platelet aggregation.{38053,38054} Eptifibatide prevents binding of the adhesion proteins fibrinogen and von Willebrand factor to GPIIb/IIIa on the surface of activated platelets to prevent aggregation and thrombus formation.{38055} It inhibits ADP-induced citrated blood aggregation (IC50 = 0.11-0.22 μg/ml) in vitro and in vivo (IC50 = 52 μg/ml in porcine plasma).{38053,38056} Formulations containing eptifibatide have been used to reduce risk of thrombolysis in myocardial infarction in patients undergoing percutaneous coronary intervention.{38057}
Brand:CaymanSKU:21578 -Out of stock
Eptifibatide is a potent glycoprotein IIb/IIIa antagonist (GPIIb/IIIa; Kd = 120 nM) that inhibits platelet aggregation.{38053,38054} Eptifibatide prevents binding of the adhesion proteins fibrinogen and von Willebrand factor to GPIIb/IIIa on the surface of activated platelets to prevent aggregation and thrombus formation.{38055} It inhibits ADP-induced citrated blood aggregation (IC50 = 0.11-0.22 μg/ml) in vitro and in vivo (IC50 = 52 μg/ml in porcine plasma).{38053,38056} Formulations containing eptifibatide have been used to reduce risk of thrombolysis in myocardial infarction in patients undergoing percutaneous coronary intervention.{38057}
Brand:CaymanSKU:21578 -Out of stock
Eptifibatide is a potent glycoprotein IIb/IIIa antagonist (GPIIb/IIIa; Kd = 120 nM) that inhibits platelet aggregation.{38053,38054} Eptifibatide prevents binding of the adhesion proteins fibrinogen and von Willebrand factor to GPIIb/IIIa on the surface of activated platelets to prevent aggregation and thrombus formation.{38055} It inhibits ADP-induced citrated blood aggregation (IC50 = 0.11-0.22 μg/ml) in vitro and in vivo (IC50 = 52 μg/ml in porcine plasma).{38053,38056} Formulations containing eptifibatide have been used to reduce risk of thrombolysis in myocardial infarction in patients undergoing percutaneous coronary intervention.{38057}
Brand:CaymanSKU:21578 -Out of stock
DOT1L is a protein methyltransferase. It is the only enzyme known to methylate histone 3 at lysine 79, where it catalyzes mono-, di-, and trimethylation.{21195} Proper DOT1L function is necessary for transcriptional activation of many genes, DNA damage repair, and cell cycle regulation.{21198} EPZ004777 is a potent inhibitor of DOT1L (IC50 = 400 pM) that selectively kills mixed lineage leukemia (MLL) cells in vitro and prolongs survival in an MLL xenograft mouse model.{30897,30896,30898,27033} It displays >1,000-fold selectivity for DOT1L relative to a panel of histone methyltransferases.{30897} DOT1L inhibition by EPZ004777 has also been shown to accelerate the reprogramming of somatic cells into induced pluripotent stem cells.{30334}
Brand:CaymanSKU:- DOT1L is a protein methyltransferase. It is the only enzyme known to methylate histone 3 at lysine 79, where it catalyzes mono-, di-, and trimethylation.{21195} Proper DOT1L function is necessary for transcriptional activation of many genes, DNA damage repair, and cell cycle regulation.{21198} EPZ004777 is a potent inhibitor of DOT1L (IC50 = 400 pM) that selectively kills mixed lineage leukemia (MLL) cells in vitro and prolongs survival in an MLL xenograft mouse model.{30897,30896,30898,27033} It displays >1,000-fold selectivity for DOT1L relative to a panel of histone methyltransferases.{30897} DOT1L inhibition by EPZ004777 has also been shown to accelerate the reprogramming of somatic cells into induced pluripotent stem cells.{30334}
Brand:CaymanSKU:- DOT1L is a protein methyltransferase. It is the only enzyme known to methylate histone 3 at lysine 79, where it catalyzes mono-, di-, and trimethylation.{21195} Proper DOT1L function is necessary for transcriptional activation of many genes, DNA damage repair, and cell cycle regulation.{21198} EPZ004777 is a potent inhibitor of DOT1L (IC50 = 400 pM) that selectively kills mixed lineage leukemia (MLL) cells in vitro and prolongs survival in an MLL xenograft mouse model.{30897,30896,30898,27033} It displays >1,000-fold selectivity for DOT1L relative to a panel of histone methyltransferases.{30897} DOT1L inhibition by EPZ004777 has also been shown to accelerate the reprogramming of somatic cells into induced pluripotent stem cells.{30334}
Brand:CaymanSKU:- DOT1L is a protein methyltransferase. It is the only enzyme known to methylate histone 3 at lysine 79, where it catalyzes mono-, di-, and trimethylation.{21195} Proper DOT1L function is necessary for transcriptional activation of many genes, DNA damage repair, and cell cycle regulation.{21198} EPZ004777 is a potent inhibitor of DOT1L (IC50 = 400 pM) that selectively kills mixed lineage leukemia (MLL) cells in vitro and prolongs survival in an MLL xenograft mouse model.{30897,30896,30898,27033} It displays >1,000-fold selectivity for DOT1L relative to a panel of histone methyltransferases.{30897} DOT1L inhibition by EPZ004777 has also been shown to accelerate the reprogramming of somatic cells into induced pluripotent stem cells.{30334}
Brand:CaymanSKU:-
EPZ005687 is a potent, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 24 nM), the enzymatic subunit of polycomb repressive complex 2 (PRC2).{26323} It acts competitively with the EZH2 substrate S-adenosylmethionine.{26323,24220,25004} EPZ005687 has greater than 500-fold selectivity against 15 other protein methyltransferases and has 50-fold selectivity against EZH1.{26323} It blocks trimethylation of the PRC2 target histone 3 lysine 27 (IC50 = 80 nM), decreasing the proliferation of lymphoma cells carrying mutant, but not wild-type, EZH2.{26323}
Brand:CaymanSKU:- EPZ005687 is a potent, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 24 nM), the enzymatic subunit of polycomb repressive complex 2 (PRC2).{26323} It acts competitively with the EZH2 substrate S-adenosylmethionine.{26323,24220,25004} EPZ005687 has greater than 500-fold selectivity against 15 other protein methyltransferases and has 50-fold selectivity against EZH1.{26323} It blocks trimethylation of the PRC2 target histone 3 lysine 27 (IC50 = 80 nM), decreasing the proliferation of lymphoma cells carrying mutant, but not wild-type, EZH2.{26323}
Brand:CaymanSKU:- EPZ005687 is a potent, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 24 nM), the enzymatic subunit of polycomb repressive complex 2 (PRC2).{26323} It acts competitively with the EZH2 substrate S-adenosylmethionine.{26323,24220,25004} EPZ005687 has greater than 500-fold selectivity against 15 other protein methyltransferases and has 50-fold selectivity against EZH1.{26323} It blocks trimethylation of the PRC2 target histone 3 lysine 27 (IC50 = 80 nM), decreasing the proliferation of lymphoma cells carrying mutant, but not wild-type, EZH2.{26323}
Brand:CaymanSKU:- EPZ005687 is a potent, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 24 nM), the enzymatic subunit of polycomb repressive complex 2 (PRC2).{26323} It acts competitively with the EZH2 substrate S-adenosylmethionine.{26323,24220,25004} EPZ005687 has greater than 500-fold selectivity against 15 other protein methyltransferases and has 50-fold selectivity against EZH1.{26323} It blocks trimethylation of the PRC2 target histone 3 lysine 27 (IC50 = 80 nM), decreasing the proliferation of lymphoma cells carrying mutant, but not wild-type, EZH2.{26323}
Brand:CaymanSKU:-
The lysine methyltransferase EZH2 (KMT6), part of polycomb repressive complex 2, catalyzes trimethylation of lysine 27 on histone H3 and is involved in proliferation and aggressive cell growth associated with neoplastic cells.{18930} EPZ011989 is an orally bioavailable EZH2 inhibitor with Ki values that are less than 3 nM for wild type and Tyr646 mutated EZH2.{30965} It displays 15-fold selectivity for EZH2 over EZH1 and is without effect against an array of other lysine methyltransferases.{30965} EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.{30965}
Brand:CaymanSKU:-Available on backorder
The lysine methyltransferase EZH2 (KMT6), part of polycomb repressive complex 2, catalyzes trimethylation of lysine 27 on histone H3 and is involved in proliferation and aggressive cell growth associated with neoplastic cells.{18930} EPZ011989 is an orally bioavailable EZH2 inhibitor with Ki values that are less than 3 nM for wild type and Tyr646 mutated EZH2.{30965} It displays 15-fold selectivity for EZH2 over EZH1 and is without effect against an array of other lysine methyltransferases.{30965} EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.{30965}
Brand:CaymanSKU:-Available on backorder
The lysine methyltransferase EZH2 (KMT6), part of polycomb repressive complex 2, catalyzes trimethylation of lysine 27 on histone H3 and is involved in proliferation and aggressive cell growth associated with neoplastic cells.{18930} EPZ011989 is an orally bioavailable EZH2 inhibitor with Ki values that are less than 3 nM for wild type and Tyr646 mutated EZH2.{30965} It displays 15-fold selectivity for EZH2 over EZH1 and is without effect against an array of other lysine methyltransferases.{30965} EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.{30965}
Brand:CaymanSKU:-Available on backorder
Protein arginine methyltransferases (PRMTs) target nuclear and cytoplasmic substrates and can alter protein actions and gene expression.{18398,18480} PRMT5, which can methylate histones H2A, H3, and H4, ribonucleoproteins, and other proteins, is upregulated in several human cancers, including lymphomas.{28582} Moreover, suppression of PRMT5 expression induces lymphoma cell death.{28581} EPZ015666 is a potent, orally bioavailable inhibitor of PRMT5 (Ki = 5 nM).{28891} It displays more than 20,000-fold selectivity for PRMT5 over other PMTs. EPZ015666 acts by blocking the association of PRMT5 with methylosome protein 50, which is necessary for the formation of an active methyltransferase complex. EPZ015666 (100 mg/kg twice daily) blocks the growth of mantle cell lymphoma Z-138 xenografts, without significant body weight loss, in mice.{28891}
Brand:CaymanSKU:-Available on backorder
Protein arginine methyltransferases (PRMTs) target nuclear and cytoplasmic substrates and can alter protein actions and gene expression.{18398,18480} PRMT5, which can methylate histones H2A, H3, and H4, ribonucleoproteins, and other proteins, is upregulated in several human cancers, including lymphomas.{28582} Moreover, suppression of PRMT5 expression induces lymphoma cell death.{28581} EPZ015666 is a potent, orally bioavailable inhibitor of PRMT5 (Ki = 5 nM).{28891} It displays more than 20,000-fold selectivity for PRMT5 over other PMTs. EPZ015666 acts by blocking the association of PRMT5 with methylosome protein 50, which is necessary for the formation of an active methyltransferase complex. EPZ015666 (100 mg/kg twice daily) blocks the growth of mantle cell lymphoma Z-138 xenografts, without significant body weight loss, in mice.{28891}
Brand:CaymanSKU:-Available on backorder
Protein arginine methyltransferases (PRMTs) target nuclear and cytoplasmic substrates and can alter protein actions and gene expression.{18398,18480} PRMT5, which can methylate histones H2A, H3, and H4, ribonucleoproteins, and other proteins, is upregulated in several human cancers, including lymphomas.{28582} Moreover, suppression of PRMT5 expression induces lymphoma cell death.{28581} EPZ015666 is a potent, orally bioavailable inhibitor of PRMT5 (Ki = 5 nM).{28891} It displays more than 20,000-fold selectivity for PRMT5 over other PMTs. EPZ015666 acts by blocking the association of PRMT5 with methylosome protein 50, which is necessary for the formation of an active methyltransferase complex. EPZ015666 (100 mg/kg twice daily) blocks the growth of mantle cell lymphoma Z-138 xenografts, without significant body weight loss, in mice.{28891}
Brand:CaymanSKU:-Available on backorder
Protein arginine methyltransferases (PRMTs) target nuclear and cytoplasmic substrates and can alter protein actions and gene expression.{18398,18480} PRMT5, which can methylate histones H2A, H3, and H4, ribonucleoproteins, and other proteins, is upregulated in several human cancers, including lymphomas.{28582} Moreover, suppression of PRMT5 expression induces lymphoma cell death.{28581} EPZ015666 is a potent, orally bioavailable inhibitor of PRMT5 (Ki = 5 nM).{28891} It displays more than 20,000-fold selectivity for PRMT5 over other PMTs. EPZ015666 acts by blocking the association of PRMT5 with methylosome protein 50, which is necessary for the formation of an active methyltransferase complex. EPZ015666 (100 mg/kg twice daily) blocks the growth of mantle cell lymphoma Z-138 xenografts, without significant body weight loss, in mice.{28891}
Brand:CaymanSKU:-Available on backorder
EPZ020411 is an inhibitor of protein arginine methyltranferase 6 (PRMT6; IC50 = 10 nM) that less potently targets PRMT1 and PRMT8 (IC50s = 119 and 223 nM, respectively).{32484} It dose-dependently decreases methylation of the PRMT6 substrate H3R2 in A375 cells transiently expressing PRMT6 (IC50 = 0.637 µM).{32484} EPZ020411 shows a moderate clearance rate in rats following intravenous bolus administration, and, following 5 mg/kg subcutaneous dosing, has an unbound blood concentration exceeding the PRMT6 biochemical IC50 value for more than 12 hours.{32484}
Brand:CaymanSKU:-Available on backorder
EPZ020411 is an inhibitor of protein arginine methyltranferase 6 (PRMT6; IC50 = 10 nM) that less potently targets PRMT1 and PRMT8 (IC50s = 119 and 223 nM, respectively).{32484} It dose-dependently decreases methylation of the PRMT6 substrate H3R2 in A375 cells transiently expressing PRMT6 (IC50 = 0.637 µM).{32484} EPZ020411 shows a moderate clearance rate in rats following intravenous bolus administration, and, following 5 mg/kg subcutaneous dosing, has an unbound blood concentration exceeding the PRMT6 biochemical IC50 value for more than 12 hours.{32484}
Brand:CaymanSKU:-Available on backorder
EPZ020411 is an inhibitor of protein arginine methyltranferase 6 (PRMT6; IC50 = 10 nM) that less potently targets PRMT1 and PRMT8 (IC50s = 119 and 223 nM, respectively).{32484} It dose-dependently decreases methylation of the PRMT6 substrate H3R2 in A375 cells transiently expressing PRMT6 (IC50 = 0.637 µM).{32484} EPZ020411 shows a moderate clearance rate in rats following intravenous bolus administration, and, following 5 mg/kg subcutaneous dosing, has an unbound blood concentration exceeding the PRMT6 biochemical IC50 value for more than 12 hours.{32484}
Brand:CaymanSKU:-Available on backorder
EPZ020411 is an inhibitor of protein arginine methyltranferase 6 (PRMT6; IC50 = 10 nM) that less potently targets PRMT1 and PRMT8 (IC50s = 119 and 223 nM, respectively).{32484} It dose-dependently decreases methylation of the PRMT6 substrate H3R2 in A375 cells transiently expressing PRMT6 (IC50 = 0.637 µM).{32484} EPZ020411 shows a moderate clearance rate in rats following intravenous bolus administration, and, following 5 mg/kg subcutaneous dosing, has an unbound blood concentration exceeding the PRMT6 biochemical IC50 value for more than 12 hours.{32484}
Brand:CaymanSKU:-Available on backorder
DOT1L is a non-SET domain containing methyltransferase whose function is important for the transcriptional activation of certain genes, DNA damage repair, and cell cycle regulation. DOT1L is known to play an essential role in MLL-rearranged leukemias, and thus has emerged as a drug target for these leukemias.{21198,21195} EPZ5676 is a highly potent aminonucleoside inhibitor of DOT1L histone methyltransferase activity (Ki = 80 pM) that demonstrates 37,000-fold selectivity over other methyltransferases.{26366,26367} In various human leukemia cell lines, EPZ5676 has been shown to inhibit the methylation of lysine 79 on histone 3 (IC50s = 3-5 nM), decreasing MLL-fusion target gene expression (IC50s = 53-67 nM).{26366} It can selectively inhibit the proliferation of acute leukemia cell lines bearing MLL translocations (IC50s range from 3.5 nM – 1.3 µM).{26366} Continuous intravenous infusion of EPZ5676 at a dose of 35 mg/kg has been reported to cause complete and sustained tumor regression in a rat xenograft model of MLL-rearranged leukemia.{26366}
Brand:CaymanSKU:-