Chemicals
Showing 26701–26850 of 41137 results
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Metronidazole is an antibiotic that has activity against anaerobic bacteria and protozoa including T. vaginalis, E. histolytica, G. lamblia, C. difficile, and H. pylori.{32541} It reduces the growth of E. coli in vitro (MIC = 128 mg/L under anaerobic conditions).{37625} In vivo, metronidazole reduces viable counts of B. fragilis in a rabbit model of infection. Formulations containing metronidazole have been used in the treatment of various infections including H. pylori and C. difficile.
Brand:CaymanSKU:9002409 - 10 gAvailable on backorder
Metronidazole is an antibiotic that has activity against anaerobic bacteria and protozoa including T. vaginalis, E. histolytica, G. lamblia, C. difficile, and H. pylori.{32541} It reduces the growth of E. coli in vitro (MIC = 128 mg/L under anaerobic conditions).{37625} In vivo, metronidazole reduces viable counts of B. fragilis in a rabbit model of infection. Formulations containing metronidazole have been used in the treatment of various infections including H. pylori and C. difficile.
Brand:CaymanSKU:9002409 - 100 gAvailable on backorder
Metronidazole is an antibiotic that has activity against anaerobic bacteria and protozoa including T. vaginalis, E. histolytica, G. lamblia, C. difficile, and H. pylori.{32541} It reduces the growth of E. coli in vitro (MIC = 128 mg/L under anaerobic conditions).{37625} In vivo, metronidazole reduces viable counts of B. fragilis in a rabbit model of infection. Formulations containing metronidazole have been used in the treatment of various infections including H. pylori and C. difficile.
Brand:CaymanSKU:9002409 - 25 gAvailable on backorder
Metronidazole is an antibiotic that has activity against anaerobic bacteria and protozoa including T. vaginalis, E. histolytica, G. lamblia, C. difficile, and H. pylori.{32541} It reduces the growth of E. coli in vitro (MIC = 128 mg/L under anaerobic conditions).{37625} In vivo, metronidazole reduces viable counts of B. fragilis in a rabbit model of infection. Formulations containing metronidazole have been used in the treatment of various infections including H. pylori and C. difficile.
Brand:CaymanSKU:9002409 - 5 gAvailable on backorder
Metronidazole-d4 is intended for use as an internal standard for the quantification of metronidazole (Item No. 9002409) by GC- or LC-MS. Metronidazole is an antibiotic that has activity against anaerobic bacteria and protozoa including T. vaginalis, E. histolytica, G. lamblia, C. difficile, and H. pylori.{32541} It reduces the growth of E. coli in vitro (MIC = 128 mg/L under anaerobic conditions).{37625} In vivo, metronidazole reduces viable counts of B. fragilis in a rabbit model of infection. Formulations containing metronidazole have been used in the treatment of various infections including H. pylori and C. difficile.
Brand:CaymanSKU:10010659 - 1 mgAvailable on backorder
Metyrapone blocks cortisol synthesis by inhibiting steroid 11β-hydroxylase in adrenal cortex (IC50 = 7.8 μM).{24101} Metyrapone binds with high affinity to cytochrome P(CYP)450 in hepatic microsomes and induces rat hepatic CYP1A1 and CYP3A gene expression.{24100,24099} It is used to assess adrenal insufficiency, to address hypercortisolism characteristic of Cushing’s syndrome, and may be of clinical value in the treatment of depression and in reducing brain damage resulting from hypoxia-ischemia.{24098,24096,24097}
Brand:CaymanSKU:- Metyrapone blocks cortisol synthesis by inhibiting steroid 11β-hydroxylase in adrenal cortex (IC50 = 7.8 μM).{24101} Metyrapone binds with high affinity to cytochrome P(CYP)450 in hepatic microsomes and induces rat hepatic CYP1A1 and CYP3A gene expression.{24100,24099} It is used to assess adrenal insufficiency, to address hypercortisolism characteristic of Cushing’s syndrome, and may be of clinical value in the treatment of depression and in reducing brain damage resulting from hypoxia-ischemia.{24098,24096,24097}
Brand:CaymanSKU:- Metyrapone blocks cortisol synthesis by inhibiting steroid 11β-hydroxylase in adrenal cortex (IC50 = 7.8 μM).{24101} Metyrapone binds with high affinity to cytochrome P(CYP)450 in hepatic microsomes and induces rat hepatic CYP1A1 and CYP3A gene expression.{24100,24099} It is used to assess adrenal insufficiency, to address hypercortisolism characteristic of Cushing’s syndrome, and may be of clinical value in the treatment of depression and in reducing brain damage resulting from hypoxia-ischemia.{24098,24096,24097}
Brand:CaymanSKU:-
Metyrosine is an inhibitor of tyrosine hydroxylase.{35206} In vivo, metyrosine (200 mg/kg) reduces norepinephrine and dopamine levels in rat brain and disrupts conditioned avoidance behavior in a dose-dependent manner. Metyrosine reduces dopamine transporter knockdown-induced hyperactivity and rearing behavior and increases exploratory behavior in a hole board assay in a mouse model of bipolar disorder mania.{35226} It reduces hypertension induced by dexamethasone (Item No. 11015) and cyclosporin in rats.{35214,35212} Metyrosine also inhibits norepinephrine production and increases plasma levels of leptin in fasted and fed mice.{35210}
Brand:CaymanSKU:24001 - 100 mgAvailable on backorder
Metyrosine is an inhibitor of tyrosine hydroxylase.{35206} In vivo, metyrosine (200 mg/kg) reduces norepinephrine and dopamine levels in rat brain and disrupts conditioned avoidance behavior in a dose-dependent manner. Metyrosine reduces dopamine transporter knockdown-induced hyperactivity and rearing behavior and increases exploratory behavior in a hole board assay in a mouse model of bipolar disorder mania.{35226} It reduces hypertension induced by dexamethasone (Item No. 11015) and cyclosporin in rats.{35214,35212} Metyrosine also inhibits norepinephrine production and increases plasma levels of leptin in fasted and fed mice.{35210}
Brand:CaymanSKU:24001 - 250 mgAvailable on backorder
Metyrosine is an inhibitor of tyrosine hydroxylase.{35206} In vivo, metyrosine (200 mg/kg) reduces norepinephrine and dopamine levels in rat brain and disrupts conditioned avoidance behavior in a dose-dependent manner. Metyrosine reduces dopamine transporter knockdown-induced hyperactivity and rearing behavior and increases exploratory behavior in a hole board assay in a mouse model of bipolar disorder mania.{35226} It reduces hypertension induced by dexamethasone (Item No. 11015) and cyclosporin in rats.{35214,35212} Metyrosine also inhibits norepinephrine production and increases plasma levels of leptin in fasted and fed mice.{35210}
Brand:CaymanSKU:24001 - 50 mgAvailable on backorder
Metyrosine is an inhibitor of tyrosine hydroxylase.{35206} In vivo, metyrosine (200 mg/kg) reduces norepinephrine and dopamine levels in rat brain and disrupts conditioned avoidance behavior in a dose-dependent manner. Metyrosine reduces dopamine transporter knockdown-induced hyperactivity and rearing behavior and increases exploratory behavior in a hole board assay in a mouse model of bipolar disorder mania.{35226} It reduces hypertension induced by dexamethasone (Item No. 11015) and cyclosporin in rats.{35214,35212} Metyrosine also inhibits norepinephrine production and increases plasma levels of leptin in fasted and fed mice.{35210}
Brand:CaymanSKU:24001 - 500 mgAvailable on backorder
Mevastatin is a potent, reversible, and competitive HMG-CoA reductase inhibitor with a Ki value of 1 nM for the open ring acid form of the molecule.{15081} In vivo, mevastatin (50 mg/kg) inhibits cholesterogenesis in the liver and ileum of normolipidemic rats, cholestyramine-treated rats, and cholesterol-fed rats.{39406} Mevastatin also suppresses TNF-induced NF-κB activation (IC50 = ~17 µM), which potentiates apoptosis in human myeloid leukemia cells.{15363} Formulations containing mevastatin have been used to reduce plasma LDL-cholesterol in patients with familial hypercholesterolemia.{15081}
Brand:CaymanSKU:10010340 - 10 mgAvailable on backorder
Mevastatin is a potent, reversible, and competitive HMG-CoA reductase inhibitor with a Ki value of 1 nM for the open ring acid form of the molecule.{15081} In vivo, mevastatin (50 mg/kg) inhibits cholesterogenesis in the liver and ileum of normolipidemic rats, cholestyramine-treated rats, and cholesterol-fed rats.{39406} Mevastatin also suppresses TNF-induced NF-κB activation (IC50 = ~17 µM), which potentiates apoptosis in human myeloid leukemia cells.{15363} Formulations containing mevastatin have been used to reduce plasma LDL-cholesterol in patients with familial hypercholesterolemia.{15081}
Brand:CaymanSKU:10010340 - 25 mgAvailable on backorder
Mevastatin is a potent, reversible, and competitive HMG-CoA reductase inhibitor with a Ki value of 1 nM for the open ring acid form of the molecule.{15081} In vivo, mevastatin (50 mg/kg) inhibits cholesterogenesis in the liver and ileum of normolipidemic rats, cholestyramine-treated rats, and cholesterol-fed rats.{39406} Mevastatin also suppresses TNF-induced NF-κB activation (IC50 = ~17 µM), which potentiates apoptosis in human myeloid leukemia cells.{15363} Formulations containing mevastatin have been used to reduce plasma LDL-cholesterol in patients with familial hypercholesterolemia.{15081}
Brand:CaymanSKU:10010340 - 5 mgAvailable on backorder
Mevastatin is a potent, reversible, and competitive HMG-CoA reductase inhibitor with a Ki value of 1 nM for the open ring acid form of the molecule.{15081} In vivo, mevastatin (50 mg/kg) inhibits cholesterogenesis in the liver and ileum of normolipidemic rats, cholestyramine-treated rats, and cholesterol-fed rats.{39406} Mevastatin also suppresses TNF-induced NF-κB activation (IC50 = ~17 µM), which potentiates apoptosis in human myeloid leukemia cells.{15363} Formulations containing mevastatin have been used to reduce plasma LDL-cholesterol in patients with familial hypercholesterolemia.{15081}
Brand:CaymanSKU:10010340 - 50 mgAvailable on backorder
Mezlocillin is a β-lactam antibiotic and derivative of ampicillin (Item No. 14417).{52600,52601} It is active against B. fragilis, E. lentum, P. morbillorum, and F. nucleatum (MICs = 8, 4, 2, and 4 µg/ml, respectively).{52601} Mezlocillin (32 µg/ml) is also active against 10 strains of S. faecalis.{52600} In vivo, mezlocillin (240 mg/kg) increases survival and reduces bacteremia in a rabbit model of S. faecalis endocarditis. It completely eliminates lung P. morbillorum, E. lentum, and F. nucelatum, but not B. fragilis, in a rabbit model of pulmonary P. morbillorum, E. lentum, F. nucelatum, and B. fragilis infection when administered at a dose of 300 mg/kg.{52601} Formulations containing mezlocillin have been used in the treatment of various bacterial infections.
Brand:CaymanSKU:30691 - 1 gAvailable on backorder
Mezlocillin is a β-lactam antibiotic and derivative of ampicillin (Item No. 14417).{52600,52601} It is active against B. fragilis, E. lentum, P. morbillorum, and F. nucleatum (MICs = 8, 4, 2, and 4 µg/ml, respectively).{52601} Mezlocillin (32 µg/ml) is also active against 10 strains of S. faecalis.{52600} In vivo, mezlocillin (240 mg/kg) increases survival and reduces bacteremia in a rabbit model of S. faecalis endocarditis. It completely eliminates lung P. morbillorum, E. lentum, and F. nucelatum, but not B. fragilis, in a rabbit model of pulmonary P. morbillorum, E. lentum, F. nucelatum, and B. fragilis infection when administered at a dose of 300 mg/kg.{52601} Formulations containing mezlocillin have been used in the treatment of various bacterial infections.
Brand:CaymanSKU:30691 - 250 mgAvailable on backorder
Mezlocillin is a β-lactam antibiotic and derivative of ampicillin (Item No. 14417).{52600,52601} It is active against B. fragilis, E. lentum, P. morbillorum, and F. nucleatum (MICs = 8, 4, 2, and 4 µg/ml, respectively).{52601} Mezlocillin (32 µg/ml) is also active against 10 strains of S. faecalis.{52600} In vivo, mezlocillin (240 mg/kg) increases survival and reduces bacteremia in a rabbit model of S. faecalis endocarditis. It completely eliminates lung P. morbillorum, E. lentum, and F. nucelatum, but not B. fragilis, in a rabbit model of pulmonary P. morbillorum, E. lentum, F. nucelatum, and B. fragilis infection when administered at a dose of 300 mg/kg.{52601} Formulations containing mezlocillin have been used in the treatment of various bacterial infections.
Brand:CaymanSKU:30691 - 5 gAvailable on backorder
Mezlocillin is a β-lactam antibiotic and derivative of ampicillin (Item No. 14417).{52600,52601} It is active against B. fragilis, E. lentum, P. morbillorum, and F. nucleatum (MICs = 8, 4, 2, and 4 µg/ml, respectively).{52601} Mezlocillin (32 µg/ml) is also active against 10 strains of S. faecalis.{52600} In vivo, mezlocillin (240 mg/kg) increases survival and reduces bacteremia in a rabbit model of S. faecalis endocarditis. It completely eliminates lung P. morbillorum, E. lentum, and F. nucelatum, but not B. fragilis, in a rabbit model of pulmonary P. morbillorum, E. lentum, F. nucelatum, and B. fragilis infection when administered at a dose of 300 mg/kg.{52601} Formulations containing mezlocillin have been used in the treatment of various bacterial infections.
Brand:CaymanSKU:30691 - 500 mgAvailable on backorder
Prostaglandin E2 (PGE2; Item No. 14010) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption, inflammation, cancer, and atherosclerosis.{16772,16773,16619} MF498 is a selective EP4 receptor antagonist (Ki = 0.7 nM versus a Ki > 1 µM for other EP receptors).{18105} In HEK293 cells expressing the human EP4 receptor, MF498 inhibits EP ligand induced activity with an IC50 value of 1.7 nM.{18105} In various animal models for arthritis, MF498 has been shown to inhibit inflammation without gastrointestinal toxicity (ED50 values as low as 0.02 mg/kg/day).{18105}
Brand:CaymanSKU:- Prostaglandin E2 (PGE2; Item No. 14010) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption, inflammation, cancer, and atherosclerosis.{16772,16773,16619} MF498 is a selective EP4 receptor antagonist (Ki = 0.7 nM versus a Ki > 1 µM for other EP receptors).{18105} In HEK293 cells expressing the human EP4 receptor, MF498 inhibits EP ligand induced activity with an IC50 value of 1.7 nM.{18105} In various animal models for arthritis, MF498 has been shown to inhibit inflammation without gastrointestinal toxicity (ED50 values as low as 0.02 mg/kg/day).{18105}
Brand:CaymanSKU:- Prostaglandin E2 (PGE2; Item No. 14010) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption, inflammation, cancer, and atherosclerosis.{16772,16773,16619} MF498 is a selective EP4 receptor antagonist (Ki = 0.7 nM versus a Ki > 1 µM for other EP receptors).{18105} In HEK293 cells expressing the human EP4 receptor, MF498 inhibits EP ligand induced activity with an IC50 value of 1.7 nM.{18105} In various animal models for arthritis, MF498 has been shown to inhibit inflammation without gastrointestinal toxicity (ED50 values as low as 0.02 mg/kg/day).{18105}
Brand:CaymanSKU:- Prostaglandin E2 (PGE2; Item No. 14010) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption, inflammation, cancer, and atherosclerosis.{16772,16773,16619} MF498 is a selective EP4 receptor antagonist (Ki = 0.7 nM versus a Ki > 1 µM for other EP receptors).{18105} In HEK293 cells expressing the human EP4 receptor, MF498 inhibits EP ligand induced activity with an IC50 value of 1.7 nM.{18105} In various animal models for arthritis, MF498 has been shown to inhibit inflammation without gastrointestinal toxicity (ED50 values as low as 0.02 mg/kg/day).{18105}
Brand:CaymanSKU:-
Microsomal prostaglandin E2 synthase-1 (mPGES-1) is the terminal enzyme in the biosynthesis of PGE2.{19887,16438,18830} MF63 is a potent, selective, and orally active inhibitor of human mPGES-1 (IC50 = 1.3 nM).{27593,27594} It displays greater than 1,000-fold selectivity over other prostanoid synthases.{27594} MF63 also potently inhibits guinea pig mPGES-1 (IC50 = 0.9 nM) but not mouse or rat mPGES-1.{27594} In guinea pigs or in mice expressing human mPGES-1, MF63 prevents LPS-induced pyresis, hyperalgesia, and iodoacetate-induced osteoarthritic pain.{27594} It does not produce the gastrointestinal toxicity that is caused by non-selective COX inhibitors, although it markedly suppresses PGE2 synthesis in the stomach.{27594}
Brand:CaymanSKU:- Microsomal prostaglandin E2 synthase-1 (mPGES-1) is the terminal enzyme in the biosynthesis of PGE2.{19887,16438,18830} MF63 is a potent, selective, and orally active inhibitor of human mPGES-1 (IC50 = 1.3 nM).{27593,27594} It displays greater than 1,000-fold selectivity over other prostanoid synthases.{27594} MF63 also potently inhibits guinea pig mPGES-1 (IC50 = 0.9 nM) but not mouse or rat mPGES-1.{27594} In guinea pigs or in mice expressing human mPGES-1, MF63 prevents LPS-induced pyresis, hyperalgesia, and iodoacetate-induced osteoarthritic pain.{27594} It does not produce the gastrointestinal toxicity that is caused by non-selective COX inhibitors, although it markedly suppresses PGE2 synthesis in the stomach.{27594}
Brand:CaymanSKU:- Microsomal prostaglandin E2 synthase-1 (mPGES-1) is the terminal enzyme in the biosynthesis of PGE2.{19887,16438,18830} MF63 is a potent, selective, and orally active inhibitor of human mPGES-1 (IC50 = 1.3 nM).{27593,27594} It displays greater than 1,000-fold selectivity over other prostanoid synthases.{27594} MF63 also potently inhibits guinea pig mPGES-1 (IC50 = 0.9 nM) but not mouse or rat mPGES-1.{27594} In guinea pigs or in mice expressing human mPGES-1, MF63 prevents LPS-induced pyresis, hyperalgesia, and iodoacetate-induced osteoarthritic pain.{27594} It does not produce the gastrointestinal toxicity that is caused by non-selective COX inhibitors, although it markedly suppresses PGE2 synthesis in the stomach.{27594}
Brand:CaymanSKU:- Microsomal prostaglandin E2 synthase-1 (mPGES-1) is the terminal enzyme in the biosynthesis of PGE2.{19887,16438,18830} MF63 is a potent, selective, and orally active inhibitor of human mPGES-1 (IC50 = 1.3 nM).{27593,27594} It displays greater than 1,000-fold selectivity over other prostanoid synthases.{27594} MF63 also potently inhibits guinea pig mPGES-1 (IC50 = 0.9 nM) but not mouse or rat mPGES-1.{27594} In guinea pigs or in mice expressing human mPGES-1, MF63 prevents LPS-induced pyresis, hyperalgesia, and iodoacetate-induced osteoarthritic pain.{27594} It does not produce the gastrointestinal toxicity that is caused by non-selective COX inhibitors, although it markedly suppresses PGE2 synthesis in the stomach.{27594}
Brand:CaymanSKU:-
MG149 is a histone acetyltransferase (HAT) inhibitor with IC50 values of 74 and 47 μM, for human recombinant Tip60 and males absent on the first (MOF) HATs, respectively.{41057,41058} MG149 targets the acetyl-CoA binding site and inhibits acetyltransferase activity in the nuclear extract from murine hippocampus, amygdala, and prefrontal cortex.{41059} MG149 also inhibits the p53 and NF-κB pathways.
Brand:CaymanSKU:22135 -Out of stock
MG149 is a histone acetyltransferase (HAT) inhibitor with IC50 values of 74 and 47 μM, for human recombinant Tip60 and males absent on the first (MOF) HATs, respectively.{41057,41058} MG149 targets the acetyl-CoA binding site and inhibits acetyltransferase activity in the nuclear extract from murine hippocampus, amygdala, and prefrontal cortex.{41059} MG149 also inhibits the p53 and NF-κB pathways.
Brand:CaymanSKU:22135 -Out of stock
MG149 is a histone acetyltransferase (HAT) inhibitor with IC50 values of 74 and 47 μM, for human recombinant Tip60 and males absent on the first (MOF) HATs, respectively.{41057,41058} MG149 targets the acetyl-CoA binding site and inhibits acetyltransferase activity in the nuclear extract from murine hippocampus, amygdala, and prefrontal cortex.{41059} MG149 also inhibits the p53 and NF-κB pathways.
Brand:CaymanSKU:22135 -Out of stock
MG149 is a histone acetyltransferase (HAT) inhibitor with IC50 values of 74 and 47 μM, for human recombinant Tip60 and males absent on the first (MOF) HATs, respectively.{41057,41058} MG149 targets the acetyl-CoA binding site and inhibits acetyltransferase activity in the nuclear extract from murine hippocampus, amygdala, and prefrontal cortex.{41059} MG149 also inhibits the p53 and NF-κB pathways.
Brand:CaymanSKU:22135 -Out of stock
MG624 is an antagonist of neuronal nicotinic acetylcholine receptors (nAChRs; Ki = 0.055 µM in neuronal chick optic lobe membranes).{42205} It is selective for neuronal nAChRs over muscle-type AChRs (Ki = 70 µM in TE671 cells that express muscle-type AChRs). MG624 inhibits currents evoked by acetylcholine in Xenopus oocytes expressing chick α7 subunit-containing nAChRs (IC50 = 94 nM). It is selective for α7 subunit-containing nAChRs over α6, β2, and β4 subunit-containing nAChRs (Kis = 4.52, 12, and 9.2 µM, respectively).{42206} It selectively decreases vagus nerve stimulation-induced contractions of isolated guinea pig vagus nerve-stomach preparations (EC50 = 49.4 µM) over isolated rat phrenic nerve-hemidiaphragm preparations (EC50 = 486 µM). MG624 decreases protein levels of early growth response gene 1 (Egr-1) induced by nicotine in human microvascular endothelial cells of the lung (HMEC-Ls).{42207} It also decreases proliferation of HMEC-Ls and inhibits angiogenesis in vitro and ex vivo as well as in an H69 small cell lung cancer (SCLC) mouse xenograft model concomitant with a reduction in tumor growth when administered in the diet at a dose of approximately 10 mg/kg per day.
Brand:CaymanSKU:24298 - 1 mgAvailable on backorder
MG624 is an antagonist of neuronal nicotinic acetylcholine receptors (nAChRs; Ki = 0.055 µM in neuronal chick optic lobe membranes).{42205} It is selective for neuronal nAChRs over muscle-type AChRs (Ki = 70 µM in TE671 cells that express muscle-type AChRs). MG624 inhibits currents evoked by acetylcholine in Xenopus oocytes expressing chick α7 subunit-containing nAChRs (IC50 = 94 nM). It is selective for α7 subunit-containing nAChRs over α6, β2, and β4 subunit-containing nAChRs (Kis = 4.52, 12, and 9.2 µM, respectively).{42206} It selectively decreases vagus nerve stimulation-induced contractions of isolated guinea pig vagus nerve-stomach preparations (EC50 = 49.4 µM) over isolated rat phrenic nerve-hemidiaphragm preparations (EC50 = 486 µM). MG624 decreases protein levels of early growth response gene 1 (Egr-1) induced by nicotine in human microvascular endothelial cells of the lung (HMEC-Ls).{42207} It also decreases proliferation of HMEC-Ls and inhibits angiogenesis in vitro and ex vivo as well as in an H69 small cell lung cancer (SCLC) mouse xenograft model concomitant with a reduction in tumor growth when administered in the diet at a dose of approximately 10 mg/kg per day.
Brand:CaymanSKU:24298 - 10 mgAvailable on backorder
MG624 is an antagonist of neuronal nicotinic acetylcholine receptors (nAChRs; Ki = 0.055 µM in neuronal chick optic lobe membranes).{42205} It is selective for neuronal nAChRs over muscle-type AChRs (Ki = 70 µM in TE671 cells that express muscle-type AChRs). MG624 inhibits currents evoked by acetylcholine in Xenopus oocytes expressing chick α7 subunit-containing nAChRs (IC50 = 94 nM). It is selective for α7 subunit-containing nAChRs over α6, β2, and β4 subunit-containing nAChRs (Kis = 4.52, 12, and 9.2 µM, respectively).{42206} It selectively decreases vagus nerve stimulation-induced contractions of isolated guinea pig vagus nerve-stomach preparations (EC50 = 49.4 µM) over isolated rat phrenic nerve-hemidiaphragm preparations (EC50 = 486 µM). MG624 decreases protein levels of early growth response gene 1 (Egr-1) induced by nicotine in human microvascular endothelial cells of the lung (HMEC-Ls).{42207} It also decreases proliferation of HMEC-Ls and inhibits angiogenesis in vitro and ex vivo as well as in an H69 small cell lung cancer (SCLC) mouse xenograft model concomitant with a reduction in tumor growth when administered in the diet at a dose of approximately 10 mg/kg per day.
Brand:CaymanSKU:24298 - 5 mgAvailable on backorder
MGCD-265 is an orally bioavailable, multi-targeted tyrosine kinase inhibitor, inhibiting MET, VGFR1-3, Tie, and Ron. Formulations containing MGCD-265, alone or in combination with other chemotherapeutic compounds, are being tested in animal models and clinical cancer trials, particularly for non-small cell lung cancer.{29344}
Brand:CaymanSKU:20097 -Available on backorder
MGCD-265 is an orally bioavailable, multi-targeted tyrosine kinase inhibitor, inhibiting MET, VGFR1-3, Tie, and Ron. Formulations containing MGCD-265, alone or in combination with other chemotherapeutic compounds, are being tested in animal models and clinical cancer trials, particularly for non-small cell lung cancer.{29344}
Brand:CaymanSKU:20097 -Available on backorder
MGCD-265 is an orally bioavailable, multi-targeted tyrosine kinase inhibitor, inhibiting MET, VGFR1-3, Tie, and Ron. Formulations containing MGCD-265, alone or in combination with other chemotherapeutic compounds, are being tested in animal models and clinical cancer trials, particularly for non-small cell lung cancer.{29344}
Brand:CaymanSKU:20097 -Available on backorder
MGCD-265 is an orally bioavailable, multi-targeted tyrosine kinase inhibitor, inhibiting MET, VGFR1-3, Tie, and Ron. Formulations containing MGCD-265, alone or in combination with other chemotherapeutic compounds, are being tested in animal models and clinical cancer trials, particularly for non-small cell lung cancer.{29344}
Brand:CaymanSKU:20097 -Available on backorder
MGK-264 is a dicarboxamide synergist used to enhance the effects of pesticides.{43335} It is not lethal to house flies when used at a concentration of 5,000 ppm and induces only 26.4% mortality of two-spotted spider mites when used at a concentration of 1,000 ppm. MGK-264 has synergistic effects on toxicity when used in combination with the insecticide Plictran in susceptible strains of S. littoralis (LD50s = 0.98 and 40 µg/larva with or without MGK-264) and in field strains (LD50s = 0.15 and 1.1 µg/larva with or without MGK-264).{43336} It also decreases the fecundity of adult L. acuminata and reduces survival of the offspring after hatching when used in combination with sublethal doses of a variety of plant-derived molluscicides.{43337}
Brand:CaymanSKU:25819 - 100 mgAvailable on backorder
MGK-264 is a dicarboxamide synergist used to enhance the effects of pesticides.{43335} It is not lethal to house flies when used at a concentration of 5,000 ppm and induces only 26.4% mortality of two-spotted spider mites when used at a concentration of 1,000 ppm. MGK-264 has synergistic effects on toxicity when used in combination with the insecticide Plictran in susceptible strains of S. littoralis (LD50s = 0.98 and 40 µg/larva with or without MGK-264) and in field strains (LD50s = 0.15 and 1.1 µg/larva with or without MGK-264).{43336} It also decreases the fecundity of adult L. acuminata and reduces survival of the offspring after hatching when used in combination with sublethal doses of a variety of plant-derived molluscicides.{43337}
Brand:CaymanSKU:25819 - 50 mgAvailable on backorder
MGL-3196 is an agonist of thyroid hormone receptor β (TRβ; EC50s = 0.21 and 3.74 µM for TRβ and TRα, respectively).{37297} It also inhibits ether-a-go-go-related gene (ERG) potassium channels (IC50 = 30 µM). MGL-3196 is a liver-directed compound, with a liver to plasma ratio of 8:1 in mice with diet-induced obesity (DIO), which reduces the likelihood of adverse effects from systemic exposure. It does not affect the expression of α-myosin heavy chain (α-MHC) in a rat model of hypothyroidism, an effect mediated by TRα, indicating low potential for cardiac adverse effects. MGL-3196 lowers non-HDL cholesterol and liver triglycerides without affecting thyroid stimulating hormone (Tsh) levels in rat and rabbit models of hypercholesterolemia. It also lowers plasma glucose levels and improves insulin sensitivity in DIO mice. Formulations containing MGL-3196 are in clinical trials for the treatment of non-alcoholic steatohepatitis (NASH) and familial hypercholesterolemia.
Brand:CaymanSKU:23845 - 1 mgAvailable on backorder
MGL-3196 is an agonist of thyroid hormone receptor β (TRβ; EC50s = 0.21 and 3.74 µM for TRβ and TRα, respectively).{37297} It also inhibits ether-a-go-go-related gene (ERG) potassium channels (IC50 = 30 µM). MGL-3196 is a liver-directed compound, with a liver to plasma ratio of 8:1 in mice with diet-induced obesity (DIO), which reduces the likelihood of adverse effects from systemic exposure. It does not affect the expression of α-myosin heavy chain (α-MHC) in a rat model of hypothyroidism, an effect mediated by TRα, indicating low potential for cardiac adverse effects. MGL-3196 lowers non-HDL cholesterol and liver triglycerides without affecting thyroid stimulating hormone (Tsh) levels in rat and rabbit models of hypercholesterolemia. It also lowers plasma glucose levels and improves insulin sensitivity in DIO mice. Formulations containing MGL-3196 are in clinical trials for the treatment of non-alcoholic steatohepatitis (NASH) and familial hypercholesterolemia.
Brand:CaymanSKU:23845 - 10 mgAvailable on backorder
MGL-3196 is an agonist of thyroid hormone receptor β (TRβ; EC50s = 0.21 and 3.74 µM for TRβ and TRα, respectively).{37297} It also inhibits ether-a-go-go-related gene (ERG) potassium channels (IC50 = 30 µM). MGL-3196 is a liver-directed compound, with a liver to plasma ratio of 8:1 in mice with diet-induced obesity (DIO), which reduces the likelihood of adverse effects from systemic exposure. It does not affect the expression of α-myosin heavy chain (α-MHC) in a rat model of hypothyroidism, an effect mediated by TRα, indicating low potential for cardiac adverse effects. MGL-3196 lowers non-HDL cholesterol and liver triglycerides without affecting thyroid stimulating hormone (Tsh) levels in rat and rabbit models of hypercholesterolemia. It also lowers plasma glucose levels and improves insulin sensitivity in DIO mice. Formulations containing MGL-3196 are in clinical trials for the treatment of non-alcoholic steatohepatitis (NASH) and familial hypercholesterolemia.
Brand:CaymanSKU:23845 - 5 mgAvailable on backorder
MGR1 is a probe that generates reactive oxygen species (ROS).{35560} Upon activation by esterases, MGR1 produces superoxide in vitro, an effect that is reversed by superoxide dismutase (SOD). MGR1 produces ROS and increases production of oxidized phosphatidylserine species in HEK293T cells. It reduces viability of HEK293T cells (IC50s = 5.1-6.3 μM).
Brand:CaymanSKU:27499 - 1 mgAvailable on backorder
MGR1 is a probe that generates reactive oxygen species (ROS).{35560} Upon activation by esterases, MGR1 produces superoxide in vitro, an effect that is reversed by superoxide dismutase (SOD). MGR1 produces ROS and increases production of oxidized phosphatidylserine species in HEK293T cells. It reduces viability of HEK293T cells (IC50s = 5.1-6.3 μM).
Brand:CaymanSKU:27499 - 500 µgAvailable on backorder
MGR2 is a negative control compound for the activity of the reactive oxygen species-generating probe MGR1 (Item No. 27499).{35560} Unlike MGR1, MGR2 does not induce superoxide production or cell death in HEK293T cells.
Brand:CaymanSKU:27575 - 10 mgAvailable on backorder
MGR2 is a negative control compound for the activity of the reactive oxygen species-generating probe MGR1 (Item No. 27499).{35560} Unlike MGR1, MGR2 does not induce superoxide production or cell death in HEK293T cells.
Brand:CaymanSKU:27575 - 25 mgAvailable on backorder
MGR2 is a negative control compound for the activity of the reactive oxygen species-generating probe MGR1 (Item No. 27499).{35560} Unlike MGR1, MGR2 does not induce superoxide production or cell death in HEK293T cells.
Brand:CaymanSKU:27575 - 5 mgAvailable on backorder
MHAPC-Chol is a cationic cholesterol.{45145} MHAPC-Chol, as part of a lipoplex with DOPE (Item No. 15091), has been used for siRNA delivery and gene silencing in MCF-7 cells in a luciferase assay without affecting cell viability. It has also been used to deliver siRNA into mice via intravenous injection, resulting in MHAPC-chol accumulation in the liver.
Brand:CaymanSKU:26585 - 1 mgAvailable on backorder
MHAPC-Chol is a cationic cholesterol.{45145} MHAPC-Chol, as part of a lipoplex with DOPE (Item No. 15091), has been used for siRNA delivery and gene silencing in MCF-7 cells in a luciferase assay without affecting cell viability. It has also been used to deliver siRNA into mice via intravenous injection, resulting in MHAPC-chol accumulation in the liver.
Brand:CaymanSKU:26585 - 10 mgAvailable on backorder
MHAPC-Chol is a cationic cholesterol.{45145} MHAPC-Chol, as part of a lipoplex with DOPE (Item No. 15091), has been used for siRNA delivery and gene silencing in MCF-7 cells in a luciferase assay without affecting cell viability. It has also been used to deliver siRNA into mice via intravenous injection, resulting in MHAPC-chol accumulation in the liver.
Brand:CaymanSKU:26585 - 5 mgAvailable on backorder
MHAPC-Chol is a cationic cholesterol.{45145} MHAPC-Chol, as part of a lipoplex with DOPE (Item No. 15091), has been used for siRNA delivery and gene silencing in MCF-7 cells in a luciferase assay without affecting cell viability. It has also been used to deliver siRNA into mice via intravenous injection, resulting in MHAPC-chol accumulation in the liver.
Brand:CaymanSKU:26585 - 500 µgAvailable on backorder
MHY1485 is a cell-permeable activator of mTOR that has been shown to increase levels of cellular mTOR Ser2448 and downstream substrate 4E-BP Thr37/46 phosphorylation in rat liver Ac2F cells.{32639} It can induce cellular LC3-II accumulation in Ac2F cells and has been shown to inhibit autophagy by suppressing the fusion between autophagosomes and lysosomes.{32639}
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MHY1485 is a cell-permeable activator of mTOR that has been shown to increase levels of cellular mTOR Ser2448 and downstream substrate 4E-BP Thr37/46 phosphorylation in rat liver Ac2F cells.{32639} It can induce cellular LC3-II accumulation in Ac2F cells and has been shown to inhibit autophagy by suppressing the fusion between autophagosomes and lysosomes.{32639}
Brand:CaymanSKU:-Available on backorder
MHY1485 is a cell-permeable activator of mTOR that has been shown to increase levels of cellular mTOR Ser2448 and downstream substrate 4E-BP Thr37/46 phosphorylation in rat liver Ac2F cells.{32639} It can induce cellular LC3-II accumulation in Ac2F cells and has been shown to inhibit autophagy by suppressing the fusion between autophagosomes and lysosomes.{32639}
Brand:CaymanSKU:-Available on backorder
MHY1485 is a cell-permeable activator of mTOR that has been shown to increase levels of cellular mTOR Ser2448 and downstream substrate 4E-BP Thr37/46 phosphorylation in rat liver Ac2F cells.{32639} It can induce cellular LC3-II accumulation in Ac2F cells and has been shown to inhibit autophagy by suppressing the fusion between autophagosomes and lysosomes.{32639}
Brand:CaymanSKU:-Available on backorder
MHY908 is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ that increases transcriptional activity of PPARα and PPARγ in a luciferase reporter assay in AC2F rat liver cells when used at a concentration of 5 µM.{29289} In vivo, MHY908 (3 mg/kg per day) reduces serum glucose, triglyceride, and insulin levels and improves hepatic steatosis by reducing hepatic triglyceride levels and lipid droplet accumulation in db/db mice and 20-month-old rats.{29289,37693} It reduces peroxynitrite and COX-2 levels, reactive oxygen species (ROS) production, and Akt phosphorylation in isolated kidney from 20-month-old rats when administered at a dose of 3 mg/kg.{37693} MHY908 inhibits mushroom tyrosinase (IC50 = 8.19 µM).{37692} It also inhibits increases in melanin content in α-melanocyte stimulating hormone-induced B16/F10 murine melanoma cells when used at a concentration of 10 µM.
Brand:CaymanSKU:-Available on backorder
MHY908 is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ that increases transcriptional activity of PPARα and PPARγ in a luciferase reporter assay in AC2F rat liver cells when used at a concentration of 5 µM.{29289} In vivo, MHY908 (3 mg/kg per day) reduces serum glucose, triglyceride, and insulin levels and improves hepatic steatosis by reducing hepatic triglyceride levels and lipid droplet accumulation in db/db mice and 20-month-old rats.{29289,37693} It reduces peroxynitrite and COX-2 levels, reactive oxygen species (ROS) production, and Akt phosphorylation in isolated kidney from 20-month-old rats when administered at a dose of 3 mg/kg.{37693} MHY908 inhibits mushroom tyrosinase (IC50 = 8.19 µM).{37692} It also inhibits increases in melanin content in α-melanocyte stimulating hormone-induced B16/F10 murine melanoma cells when used at a concentration of 10 µM.
Brand:CaymanSKU:-Available on backorder
MHY908 is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ that increases transcriptional activity of PPARα and PPARγ in a luciferase reporter assay in AC2F rat liver cells when used at a concentration of 5 µM.{29289} In vivo, MHY908 (3 mg/kg per day) reduces serum glucose, triglyceride, and insulin levels and improves hepatic steatosis by reducing hepatic triglyceride levels and lipid droplet accumulation in db/db mice and 20-month-old rats.{29289,37693} It reduces peroxynitrite and COX-2 levels, reactive oxygen species (ROS) production, and Akt phosphorylation in isolated kidney from 20-month-old rats when administered at a dose of 3 mg/kg.{37693} MHY908 inhibits mushroom tyrosinase (IC50 = 8.19 µM).{37692} It also inhibits increases in melanin content in α-melanocyte stimulating hormone-induced B16/F10 murine melanoma cells when used at a concentration of 10 µM.
Brand:CaymanSKU:-Available on backorder
MHY908 is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ that increases transcriptional activity of PPARα and PPARγ in a luciferase reporter assay in AC2F rat liver cells when used at a concentration of 5 µM.{29289} In vivo, MHY908 (3 mg/kg per day) reduces serum glucose, triglyceride, and insulin levels and improves hepatic steatosis by reducing hepatic triglyceride levels and lipid droplet accumulation in db/db mice and 20-month-old rats.{29289,37693} It reduces peroxynitrite and COX-2 levels, reactive oxygen species (ROS) production, and Akt phosphorylation in isolated kidney from 20-month-old rats when administered at a dose of 3 mg/kg.{37693} MHY908 inhibits mushroom tyrosinase (IC50 = 8.19 µM).{37692} It also inhibits increases in melanin content in α-melanocyte stimulating hormone-induced B16/F10 murine melanoma cells when used at a concentration of 10 µM.
Brand:CaymanSKU:-Available on backorder
MI 2 is an inhibitor of the paracaspase MALT1 with an IC50 value of 5.84 μM in a fluorescence assay.{36194} It inhibits the growth of MALT1-dependent activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL) cell lines (GI50s = 0.2, 0.5, 0.4, and 0.4 μM for HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells, respectively). MI 2 inhibits cleavage of the MALT1 target protein CYLD in a dose-dependent manner in HBL-1 cells but does not inhibit caspase-3, caspase-8, and caspase-9, which are structurally similar to MALT1. MI 2 (25 mg/kg, i.v.) reduces tumor size in TMD8 and HBL-1 mouse xenograft models.
Brand:CaymanSKU:23437 - 1 mgAvailable on backorder
MI 2 is an inhibitor of the paracaspase MALT1 with an IC50 value of 5.84 μM in a fluorescence assay.{36194} It inhibits the growth of MALT1-dependent activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL) cell lines (GI50s = 0.2, 0.5, 0.4, and 0.4 μM for HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells, respectively). MI 2 inhibits cleavage of the MALT1 target protein CYLD in a dose-dependent manner in HBL-1 cells but does not inhibit caspase-3, caspase-8, and caspase-9, which are structurally similar to MALT1. MI 2 (25 mg/kg, i.v.) reduces tumor size in TMD8 and HBL-1 mouse xenograft models.
Brand:CaymanSKU:23437 - 10 mgAvailable on backorder
MI 2 is an inhibitor of the paracaspase MALT1 with an IC50 value of 5.84 μM in a fluorescence assay.{36194} It inhibits the growth of MALT1-dependent activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL) cell lines (GI50s = 0.2, 0.5, 0.4, and 0.4 μM for HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells, respectively). MI 2 inhibits cleavage of the MALT1 target protein CYLD in a dose-dependent manner in HBL-1 cells but does not inhibit caspase-3, caspase-8, and caspase-9, which are structurally similar to MALT1. MI 2 (25 mg/kg, i.v.) reduces tumor size in TMD8 and HBL-1 mouse xenograft models.
Brand:CaymanSKU:23437 - 25 mgAvailable on backorder
MI 2 is an inhibitor of the paracaspase MALT1 with an IC50 value of 5.84 μM in a fluorescence assay.{36194} It inhibits the growth of MALT1-dependent activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL) cell lines (GI50s = 0.2, 0.5, 0.4, and 0.4 μM for HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells, respectively). MI 2 inhibits cleavage of the MALT1 target protein CYLD in a dose-dependent manner in HBL-1 cells but does not inhibit caspase-3, caspase-8, and caspase-9, which are structurally similar to MALT1. MI 2 (25 mg/kg, i.v.) reduces tumor size in TMD8 and HBL-1 mouse xenograft models.
Brand:CaymanSKU:23437 - 5 mgAvailable on backorder
MI-136 is an inhibitor of the menin-MLL interaction (IC50 = 31 nM; Kd = 23.6 nM).{30618,28761} By blocking MLL recruitment predominantly at the level of the menin-MLL interaction, it can inhibit androgen receptor (AR)-mediated transcription.{32723} At 40 mg/kg, MI-136 has been shown to block AR signaling, inhibiting the growth of castration-resistant tumors in mice.{32723}
Brand:CaymanSKU:-Available on backorder
MI-136 is an inhibitor of the menin-MLL interaction (IC50 = 31 nM; Kd = 23.6 nM).{30618,28761} By blocking MLL recruitment predominantly at the level of the menin-MLL interaction, it can inhibit androgen receptor (AR)-mediated transcription.{32723} At 40 mg/kg, MI-136 has been shown to block AR signaling, inhibiting the growth of castration-resistant tumors in mice.{32723}
Brand:CaymanSKU:-Available on backorder
MI-136 is an inhibitor of the menin-MLL interaction (IC50 = 31 nM; Kd = 23.6 nM).{30618,28761} By blocking MLL recruitment predominantly at the level of the menin-MLL interaction, it can inhibit androgen receptor (AR)-mediated transcription.{32723} At 40 mg/kg, MI-136 has been shown to block AR signaling, inhibiting the growth of castration-resistant tumors in mice.{32723}
Brand:CaymanSKU:-Available on backorder
MI-136 is an inhibitor of the menin-MLL interaction (IC50 = 31 nM; Kd = 23.6 nM).{30618,28761} By blocking MLL recruitment predominantly at the level of the menin-MLL interaction, it can inhibit androgen receptor (AR)-mediated transcription.{32723} At 40 mg/kg, MI-136 has been shown to block AR signaling, inhibiting the growth of castration-resistant tumors in mice.{32723}
Brand:CaymanSKU:-Available on backorder
MI-192 is an inhibitor of histone deacetylases (HDACs) that preferentially inhibits HDAC2 (IC50 = 30 nM) and HDAC3 (IC50 = 16 nM) over HDAC1, 4, 6, 7, and 8 (IC50s = 4.8, 5, >10, 4.1, and >10 μM, respectively).{29271} At 0.1-0.4 μM, it induces differentiation and promotes apoptosis of acute myeloid leukemic cell lines U937, HL60, and Kasumi-1.{29271}
Brand:CaymanSKU:-Available on backorder
MI-192 is an inhibitor of histone deacetylases (HDACs) that preferentially inhibits HDAC2 (IC50 = 30 nM) and HDAC3 (IC50 = 16 nM) over HDAC1, 4, 6, 7, and 8 (IC50s = 4.8, 5, >10, 4.1, and >10 μM, respectively).{29271} At 0.1-0.4 μM, it induces differentiation and promotes apoptosis of acute myeloid leukemic cell lines U937, HL60, and Kasumi-1.{29271}
Brand:CaymanSKU:-Available on backorder
MI-192 is an inhibitor of histone deacetylases (HDACs) that preferentially inhibits HDAC2 (IC50 = 30 nM) and HDAC3 (IC50 = 16 nM) over HDAC1, 4, 6, 7, and 8 (IC50s = 4.8, 5, >10, 4.1, and >10 μM, respectively).{29271} At 0.1-0.4 μM, it induces differentiation and promotes apoptosis of acute myeloid leukemic cell lines U937, HL60, and Kasumi-1.{29271}
Brand:CaymanSKU:-Available on backorder
MI-2 is an inhibitor of the protein-protein interaction between menin and mixed lineage leukemia (MLL) fusion proteins (IC50 = 446 nM).{20716} It binds to menin (Kd = 158 nM) and inhibits the menin interaction with the MLL fusion protein MLL-AF9 in HEK293 cells without affecting protein levels of menin or MLL-AF9. MI-2 inhibits the growth of mouse bone marrow cells (BMCs) expressing the Hoxa9 transformation-dependent MLL-AF9 (GI50 = 5 μM). It also inhibits the growth of MV4, KOPN-8, ML-2, and MonoMac6 MLL cells expressing MLL fusion proteins (GI50s = 9.5, 7.2, 8.7, and 18 μM, respectively), as well as induces hematopoietic differentiation.
Brand:CaymanSKU:29218 - 10 mgAvailable on backorder
MI-2 is an inhibitor of the protein-protein interaction between menin and mixed lineage leukemia (MLL) fusion proteins (IC50 = 446 nM).{20716} It binds to menin (Kd = 158 nM) and inhibits the menin interaction with the MLL fusion protein MLL-AF9 in HEK293 cells without affecting protein levels of menin or MLL-AF9. MI-2 inhibits the growth of mouse bone marrow cells (BMCs) expressing the Hoxa9 transformation-dependent MLL-AF9 (GI50 = 5 μM). It also inhibits the growth of MV4, KOPN-8, ML-2, and MonoMac6 MLL cells expressing MLL fusion proteins (GI50s = 9.5, 7.2, 8.7, and 18 μM, respectively), as well as induces hematopoietic differentiation.
Brand:CaymanSKU:29218 - 25 mgAvailable on backorder
MI-2 is an inhibitor of the protein-protein interaction between menin and mixed lineage leukemia (MLL) fusion proteins (IC50 = 446 nM).{20716} It binds to menin (Kd = 158 nM) and inhibits the menin interaction with the MLL fusion protein MLL-AF9 in HEK293 cells without affecting protein levels of menin or MLL-AF9. MI-2 inhibits the growth of mouse bone marrow cells (BMCs) expressing the Hoxa9 transformation-dependent MLL-AF9 (GI50 = 5 μM). It also inhibits the growth of MV4, KOPN-8, ML-2, and MonoMac6 MLL cells expressing MLL fusion proteins (GI50s = 9.5, 7.2, 8.7, and 18 μM, respectively), as well as induces hematopoietic differentiation.
Brand:CaymanSKU:29218 - 5 mgAvailable on backorder
MI-2 is an inhibitor of the protein-protein interaction between menin and mixed lineage leukemia (MLL) fusion proteins (IC50 = 446 nM).{20716} It binds to menin (Kd = 158 nM) and inhibits the menin interaction with the MLL fusion protein MLL-AF9 in HEK293 cells without affecting protein levels of menin or MLL-AF9. MI-2 inhibits the growth of mouse bone marrow cells (BMCs) expressing the Hoxa9 transformation-dependent MLL-AF9 (GI50 = 5 μM). It also inhibits the growth of MV4, KOPN-8, ML-2, and MonoMac6 MLL cells expressing MLL fusion proteins (GI50s = 9.5, 7.2, 8.7, and 18 μM, respectively), as well as induces hematopoietic differentiation.
Brand:CaymanSKU:29218 - 50 mgAvailable on backorder
MI-3 is an inhibitor of the interaction between menin and mixed lineage leukemia (MLL) fusion proteins (IC50 = 648 nM).{20716} MI-3 binds to menin (Kd = 201 nM) and inhibits the menin interaction with the MLL fusion protein MLL-AF9 in HEK293 cells without affecting protein levels of menin or MLL-AF9. It inhibits growth of mouse bone marrow cells (BMCs) expressing the Hoxa9 transformation-dependent MLL fusion proteins MLL-AF9 or MLL-ENL (IC50 = 5 µM for both), as well as reduces colony formation and induces differentiation of MLL-AF9-transformed BMCs. MI-3 inhibits growth of human leukemia cell lines containing MLL translocations and decreases the expression of the transcription factors HOXA9, HOXA10, and MEIS1 in THP-1 cells.
Brand:CaymanSKU:27214 - 1 mgAvailable on backorder
MI-3 is an inhibitor of the interaction between menin and mixed lineage leukemia (MLL) fusion proteins (IC50 = 648 nM).{20716} MI-3 binds to menin (Kd = 201 nM) and inhibits the menin interaction with the MLL fusion protein MLL-AF9 in HEK293 cells without affecting protein levels of menin or MLL-AF9. It inhibits growth of mouse bone marrow cells (BMCs) expressing the Hoxa9 transformation-dependent MLL fusion proteins MLL-AF9 or MLL-ENL (IC50 = 5 µM for both), as well as reduces colony formation and induces differentiation of MLL-AF9-transformed BMCs. MI-3 inhibits growth of human leukemia cell lines containing MLL translocations and decreases the expression of the transcription factors HOXA9, HOXA10, and MEIS1 in THP-1 cells.
Brand:CaymanSKU:27214 - 5 mgAvailable on backorder
MI-3 is an inhibitor of the interaction between menin and mixed lineage leukemia (MLL) fusion proteins (IC50 = 648 nM).{20716} MI-3 binds to menin (Kd = 201 nM) and inhibits the menin interaction with the MLL fusion protein MLL-AF9 in HEK293 cells without affecting protein levels of menin or MLL-AF9. It inhibits growth of mouse bone marrow cells (BMCs) expressing the Hoxa9 transformation-dependent MLL fusion proteins MLL-AF9 or MLL-ENL (IC50 = 5 µM for both), as well as reduces colony formation and induces differentiation of MLL-AF9-transformed BMCs. MI-3 inhibits growth of human leukemia cell lines containing MLL translocations and decreases the expression of the transcription factors HOXA9, HOXA10, and MEIS1 in THP-1 cells.
Brand:CaymanSKU:27214 - 500 µgAvailable on backorder
The protein p53, often called the ‘guardian of the genome,’ is a transcription factor that is activated in response to cellular stress (low oxygen levels, heat shock, DNA damage, etc.) and acts to prevent further proliferation of the stressed cell by promoting cell cycle arrest or apoptosis. Its role as a tumor suppressor is evident by the observation that approximately 50% of human tumors have mutated or non-functional p53. Mdm2, a key negative regulator of p53, which is over-expressed in many human tumors, functions by binding to and targeting p53 for proteasomal degradation. MI-77301 binds to MDM2 with a Ki value of 0.88 nM and blocks the MDM2-p53 interaction.{29885} It activates wild-type p53 in vitro and in xenograft tumor tissue of leukemia and solid tumors, leading to p53-dependent cell cycle arrest and/or apoptosis.{29885} In an SJSA-1 xenograft model of osteosarcoma, a single dose of 200 mg/kg MI-77301 induces complete tumor regression in mice by upregulating the pro-apoptotic protein PUMA.{29885}
Brand:CaymanSKU:-Available on backorder
The protein p53, often called the ‘guardian of the genome,’ is a transcription factor that is activated in response to cellular stress (low oxygen levels, heat shock, DNA damage, etc.) and acts to prevent further proliferation of the stressed cell by promoting cell cycle arrest or apoptosis. Its role as a tumor suppressor is evident by the observation that approximately 50% of human tumors have mutated or non-functional p53. Mdm2, a key negative regulator of p53, which is over-expressed in many human tumors, functions by binding to and targeting p53 for proteasomal degradation. MI-77301 binds to MDM2 with a Ki value of 0.88 nM and blocks the MDM2-p53 interaction.{29885} It activates wild-type p53 in vitro and in xenograft tumor tissue of leukemia and solid tumors, leading to p53-dependent cell cycle arrest and/or apoptosis.{29885} In an SJSA-1 xenograft model of osteosarcoma, a single dose of 200 mg/kg MI-77301 induces complete tumor regression in mice by upregulating the pro-apoptotic protein PUMA.{29885}
Brand:CaymanSKU:-Available on backorder