Chemicals
Showing 39751–39900 of 41137 results
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Voacamine is an alkaloid originally isolated from Voacanga that has diverse biological activities.{37654} It is a cannabinoid receptor 1 (CB1) antagonist (IC50 = 41 nM).{37655} Voacamine (1-10 µg/ml) time- and dose-dependently decreases survival of U2OS and multi-drug resistant U2OS (U2OS/DX) osteosarcoma cells and induces autophagy but not apoptosis.{37656} It also has antimalarial activity, inhibiting growth of P. falciparum in vitro at the trophozoite and schizont stages and reducing parasitemia in mice infected with P. yoelii when administered at doses of 2.5, 5, and 10 mg/kg.{37657}
Brand:CaymanSKU:25204 - 1 mgAvailable on backorder
Voacamine is an alkaloid originally isolated from Voacanga that has diverse biological activities.{37654} It is a cannabinoid receptor 1 (CB1) antagonist (IC50 = 41 nM).{37655} Voacamine (1-10 µg/ml) time- and dose-dependently decreases survival of U2OS and multi-drug resistant U2OS (U2OS/DX) osteosarcoma cells and induces autophagy but not apoptosis.{37656} It also has antimalarial activity, inhibiting growth of P. falciparum in vitro at the trophozoite and schizont stages and reducing parasitemia in mice infected with P. yoelii when administered at doses of 2.5, 5, and 10 mg/kg.{37657}
Brand:CaymanSKU:25204 - 5 mgAvailable on backorder
Voacamine is an alkaloid originally isolated from Voacanga that has diverse biological activities.{37654} It is a cannabinoid receptor 1 (CB1) antagonist (IC50 = 41 nM).{37655} Voacamine (1-10 µg/ml) time- and dose-dependently decreases survival of U2OS and multi-drug resistant U2OS (U2OS/DX) osteosarcoma cells and induces autophagy but not apoptosis.{37656} It also has antimalarial activity, inhibiting growth of P. falciparum in vitro at the trophozoite and schizont stages and reducing parasitemia in mice infected with P. yoelii when administered at doses of 2.5, 5, and 10 mg/kg.{37657}
Brand:CaymanSKU:25204 - 500 µgAvailable on backorder
Voacangine is an indole alkaloid that has been found in T. citrifolia, V. africana, V. obtusa, and T. iboga with diverse biological activities.{41758,41754} It inhibits the growth of M. tuberculosis, M. avium, and M. kansasii with MIC values of 50, >200, and 100 μg/mL, respectively.{41754} Voacangine (0.01-100 μM) dose-dependently reduces membrane currents in HEK293 cells expressing the hERG potassium channel and displaces the hERG ligand dofetilide (Item No. 15045) with a Ki value of 3.9 μM.{41755} Voacangine suppresses agonist-induced activation of transient receptor potential (TRP) channels with IC50 values of 50 and 9 μM for activation induced by the TRPV1 agonist capsaicin (Item No. 92350) and the TRPM8 agonist menthol, respectively.{41756} It also activates TRPA1 channels and stimulates calcium influx (IC50 = 8 μM in HEK293 cells expressing TRPA1), an effect that is blocked by the TRPA1 blocker HC-030031 (Item No. 11923). In vivo, voacangine (2 and 4 μg per egg) inhibits angiogenesis in chick embryo chorioallantoic membranes without apparent cytotoxicity.{41757}
Brand:CaymanSKU:24692 - 1 mgAvailable on backorder
Voacangine is an indole alkaloid that has been found in T. citrifolia, V. africana, V. obtusa, and T. iboga with diverse biological activities.{41758,41754} It inhibits the growth of M. tuberculosis, M. avium, and M. kansasii with MIC values of 50, >200, and 100 μg/mL, respectively.{41754} Voacangine (0.01-100 μM) dose-dependently reduces membrane currents in HEK293 cells expressing the hERG potassium channel and displaces the hERG ligand dofetilide (Item No. 15045) with a Ki value of 3.9 μM.{41755} Voacangine suppresses agonist-induced activation of transient receptor potential (TRP) channels with IC50 values of 50 and 9 μM for activation induced by the TRPV1 agonist capsaicin (Item No. 92350) and the TRPM8 agonist menthol, respectively.{41756} It also activates TRPA1 channels and stimulates calcium influx (IC50 = 8 μM in HEK293 cells expressing TRPA1), an effect that is blocked by the TRPA1 blocker HC-030031 (Item No. 11923). In vivo, voacangine (2 and 4 μg per egg) inhibits angiogenesis in chick embryo chorioallantoic membranes without apparent cytotoxicity.{41757}
Brand:CaymanSKU:24692 - 10 mgAvailable on backorder
Voacangine is an indole alkaloid that has been found in T. citrifolia, V. africana, V. obtusa, and T. iboga with diverse biological activities.{41758,41754} It inhibits the growth of M. tuberculosis, M. avium, and M. kansasii with MIC values of 50, >200, and 100 μg/mL, respectively.{41754} Voacangine (0.01-100 μM) dose-dependently reduces membrane currents in HEK293 cells expressing the hERG potassium channel and displaces the hERG ligand dofetilide (Item No. 15045) with a Ki value of 3.9 μM.{41755} Voacangine suppresses agonist-induced activation of transient receptor potential (TRP) channels with IC50 values of 50 and 9 μM for activation induced by the TRPV1 agonist capsaicin (Item No. 92350) and the TRPM8 agonist menthol, respectively.{41756} It also activates TRPA1 channels and stimulates calcium influx (IC50 = 8 μM in HEK293 cells expressing TRPA1), an effect that is blocked by the TRPA1 blocker HC-030031 (Item No. 11923). In vivo, voacangine (2 and 4 μg per egg) inhibits angiogenesis in chick embryo chorioallantoic membranes without apparent cytotoxicity.{41757}
Brand:CaymanSKU:24692 - 5 mgAvailable on backorder
Brand:CaymanSKU:30057 - 1 mgAvailable on backorder
Brand:CaymanSKU:30057 - 5 mgAvailable on backorder
Voglibose is a competitive α-glucosidase inhibitor (IC50 = 5.6 µM) that was first isolated from S. hygroscopicus.{31636,22626} It has been shown to delay the absorption and digestion of dietary polysaccharides by reversibly inhibiting digestive enzymes such as maltase, isomaltase, and sucrase with IC50 values of 0.18, 5.2, and 0.37 µM, respectively.{22626,22628} Voglibose is also reported to increase glucagon-like peptide 1 release.{31637,31638} In clinical trials, voglibose has been used to inhibit postprandial hyperglycemia associated with diabetes without cardiovascular complications.{31636,22629}
Brand:CaymanSKU:- Voglibose is a competitive α-glucosidase inhibitor (IC50 = 5.6 µM) that was first isolated from S. hygroscopicus.{31636,22626} It has been shown to delay the absorption and digestion of dietary polysaccharides by reversibly inhibiting digestive enzymes such as maltase, isomaltase, and sucrase with IC50 values of 0.18, 5.2, and 0.37 µM, respectively.{22626,22628} Voglibose is also reported to increase glucagon-like peptide 1 release.{31637,31638} In clinical trials, voglibose has been used to inhibit postprandial hyperglycemia associated with diabetes without cardiovascular complications.{31636,22629}
Brand:CaymanSKU:- Voglibose is a competitive α-glucosidase inhibitor (IC50 = 5.6 µM) that was first isolated from S. hygroscopicus.{31636,22626} It has been shown to delay the absorption and digestion of dietary polysaccharides by reversibly inhibiting digestive enzymes such as maltase, isomaltase, and sucrase with IC50 values of 0.18, 5.2, and 0.37 µM, respectively.{22626,22628} Voglibose is also reported to increase glucagon-like peptide 1 release.{31637,31638} In clinical trials, voglibose has been used to inhibit postprandial hyperglycemia associated with diabetes without cardiovascular complications.{31636,22629}
Brand:CaymanSKU:- Voglibose is a competitive α-glucosidase inhibitor (IC50 = 5.6 µM) that was first isolated from S. hygroscopicus.{31636,22626} It has been shown to delay the absorption and digestion of dietary polysaccharides by reversibly inhibiting digestive enzymes such as maltase, isomaltase, and sucrase with IC50 values of 0.18, 5.2, and 0.37 µM, respectively.{22626,22628} Voglibose is also reported to increase glucagon-like peptide 1 release.{31637,31638} In clinical trials, voglibose has been used to inhibit postprandial hyperglycemia associated with diabetes without cardiovascular complications.{31636,22629}
Brand:CaymanSKU:-
Volinanserin is a potent and selective antagonist of the serotonin receptor 5-HT2A (Ki = 0.36-0.85 nM).{25877,25875} It weakly binds 5-HT2C, α1-adrenergic, and sigma receptors (Ki = 88, 128, and 87 nM) and much less effectively associates with other serotonin, dopamine, adrenergic, muscarinic acetylcholine receptors and monoamine transporters.{25875,25876} Volinanserin displays antipsychotic activity, attenuates impulsivity, and augments antidepressant effects in vivo.{25877,25878,23022}
Brand:CaymanSKU:- Volinanserin is a potent and selective antagonist of the serotonin receptor 5-HT2A (Ki = 0.36-0.85 nM).{25877,25875} It weakly binds 5-HT2C, α1-adrenergic, and sigma receptors (Ki = 88, 128, and 87 nM) and much less effectively associates with other serotonin, dopamine, adrenergic, muscarinic acetylcholine receptors and monoamine transporters.{25875,25876} Volinanserin displays antipsychotic activity, attenuates impulsivity, and augments antidepressant effects in vivo.{25877,25878,23022}
Brand:CaymanSKU:- Volinanserin is a potent and selective antagonist of the serotonin receptor 5-HT2A (Ki = 0.36-0.85 nM).{25877,25875} It weakly binds 5-HT2C, α1-adrenergic, and sigma receptors (Ki = 88, 128, and 87 nM) and much less effectively associates with other serotonin, dopamine, adrenergic, muscarinic acetylcholine receptors and monoamine transporters.{25875,25876} Volinanserin displays antipsychotic activity, attenuates impulsivity, and augments antidepressant effects in vivo.{25877,25878,23022}
Brand:CaymanSKU:-
Vonoprazan is a selective, reversible, and potassium-competitive proton pump inhibitor that inhibits gastric H+/K+ ATPase (IC50 = 17 nM) but does not inhibit porcine Na+/K+ ATPase activity when used at a concentration of 10 µM.{40933,40934} It maintains its inhibitory effect in both weakly acidic (pH 6.5) and neutral (pH 7.5) conditions with IC50 values of 19 and 28 nM, respectively. In vivo, vonoprazan (1, 2, and 4 mg/kg) inhibits histamine-stimulated acid secretion in a dose-dependent manner in rats, with complete inhibition when administered at a dose of 4 mg/kg.{40935} It also inhibits acid secretion for more than 48 hours in dogs when administered at doses ranging from 0.1 to 1 mg/kg.
Brand:CaymanSKU:24200 - 1 gAvailable on backorder
Vonoprazan is a selective, reversible, and potassium-competitive proton pump inhibitor that inhibits gastric H+/K+ ATPase (IC50 = 17 nM) but does not inhibit porcine Na+/K+ ATPase activity when used at a concentration of 10 µM.{40933,40934} It maintains its inhibitory effect in both weakly acidic (pH 6.5) and neutral (pH 7.5) conditions with IC50 values of 19 and 28 nM, respectively. In vivo, vonoprazan (1, 2, and 4 mg/kg) inhibits histamine-stimulated acid secretion in a dose-dependent manner in rats, with complete inhibition when administered at a dose of 4 mg/kg.{40935} It also inhibits acid secretion for more than 48 hours in dogs when administered at doses ranging from 0.1 to 1 mg/kg.
Brand:CaymanSKU:24200 - 10 gAvailable on backorder
Vonoprazan is a selective, reversible, and potassium-competitive proton pump inhibitor that inhibits gastric H+/K+ ATPase (IC50 = 17 nM) but does not inhibit porcine Na+/K+ ATPase activity when used at a concentration of 10 µM.{40933,40934} It maintains its inhibitory effect in both weakly acidic (pH 6.5) and neutral (pH 7.5) conditions with IC50 values of 19 and 28 nM, respectively. In vivo, vonoprazan (1, 2, and 4 mg/kg) inhibits histamine-stimulated acid secretion in a dose-dependent manner in rats, with complete inhibition when administered at a dose of 4 mg/kg.{40935} It also inhibits acid secretion for more than 48 hours in dogs when administered at doses ranging from 0.1 to 1 mg/kg.
Brand:CaymanSKU:24200 - 5 gAvailable on backorder
Vonoprazan is a selective, reversible, and potassium-competitive proton pump inhibitor that inhibits gastric H+/K+ ATPase (IC50 = 17 nM) but does not inhibit porcine Na+/K+ ATPase activity when used at a concentration of 10 µM.{40933,40934} It maintains its inhibitory effect in both weakly acidic (pH 6.5) and neutral (pH 7.5) conditions with IC50 values of 19 and 28 nM, respectively. In vivo, vonoprazan (1, 2, and 4 mg/kg) inhibits histamine-stimulated acid secretion in a dose-dependent manner in rats, with complete inhibition when administered at a dose of 4 mg/kg.{40935} It also inhibits acid secretion for more than 48 hours in dogs when administered at doses ranging from 0.1 to 1 mg/kg.
Brand:CaymanSKU:24200 - 500 mgAvailable on backorder
Vorapaxar is an orally bioavailable competitive antagonist of the proteinase-activated receptor (PAR1; Ki = 8.1 nM), also known as the thrombin receptor.{37192} It is selective for PAR1 over other PARs, as well as a number of GPCRs, ion channels, and receptors. It inhibits platelet aggregation induced by thrombin (Item No. 13188) and haTRAP (IC50s = 47 and 25 nM, respectively). Vorapaxar (0.1 mg/kg, i.v.) completely inhibits platelet aggregation in cynomolgus monkeys ex vivo. Formulations containing vorapaxar are used in the prevention of thrombotic cardiovascular events.
Brand:CaymanSKU:23119 - 1 mgAvailable on backorder
Vorapaxar is an orally bioavailable competitive antagonist of the proteinase-activated receptor (PAR1; Ki = 8.1 nM), also known as the thrombin receptor.{37192} It is selective for PAR1 over other PARs, as well as a number of GPCRs, ion channels, and receptors. It inhibits platelet aggregation induced by thrombin (Item No. 13188) and haTRAP (IC50s = 47 and 25 nM, respectively). Vorapaxar (0.1 mg/kg, i.v.) completely inhibits platelet aggregation in cynomolgus monkeys ex vivo. Formulations containing vorapaxar are used in the prevention of thrombotic cardiovascular events.
Brand:CaymanSKU:23119 - 5 mgAvailable on backorder
Vorsidenib is an inhibitor of mutant isocitrate dehydrogenase (IDH; IC50s = 31.9 and 31.7 nM for IDH1R132H and IDH2R140Q, respectively).{45449} It also inhibits wild-type-IDH1R132H and wild-type-IDH2R140Q heterodimers (IC50s = 4 and 251 nM, respectively).{45451} Vorsidenib decreases the production of D-2-hydroxyglutarate (2-HG; Item Nos. 25895 | 11605) in TF-1 leukemia cells expressing IDH1R132H or IDH2R140Q (IC50s = 3.2 and 14 nM, respectively). It reduces tumor growth in a TS603-IDH1R132H mouse xenograft model when administered at a dose of 50 mg/kg.{45450}
Brand:CaymanSKU:28462 - 1 mgAvailable on backorder
Vorsidenib is an inhibitor of mutant isocitrate dehydrogenase (IDH; IC50s = 31.9 and 31.7 nM for IDH1R132H and IDH2R140Q, respectively).{45449} It also inhibits wild-type-IDH1R132H and wild-type-IDH2R140Q heterodimers (IC50s = 4 and 251 nM, respectively).{45451} Vorsidenib decreases the production of D-2-hydroxyglutarate (2-HG; Item Nos. 25895 | 11605) in TF-1 leukemia cells expressing IDH1R132H or IDH2R140Q (IC50s = 3.2 and 14 nM, respectively). It reduces tumor growth in a TS603-IDH1R132H mouse xenograft model when administered at a dose of 50 mg/kg.{45450}
Brand:CaymanSKU:28462 - 10 mgAvailable on backorder
Vorsidenib is an inhibitor of mutant isocitrate dehydrogenase (IDH; IC50s = 31.9 and 31.7 nM for IDH1R132H and IDH2R140Q, respectively).{45449} It also inhibits wild-type-IDH1R132H and wild-type-IDH2R140Q heterodimers (IC50s = 4 and 251 nM, respectively).{45451} Vorsidenib decreases the production of D-2-hydroxyglutarate (2-HG; Item Nos. 25895 | 11605) in TF-1 leukemia cells expressing IDH1R132H or IDH2R140Q (IC50s = 3.2 and 14 nM, respectively). It reduces tumor growth in a TS603-IDH1R132H mouse xenograft model when administered at a dose of 50 mg/kg.{45450}
Brand:CaymanSKU:28462 - 5 mgAvailable on backorder
Voriconazole is a triazole antifungal agent and a derivative of fluconazole (Item No. 11594).{48762,48763} It is active against a variety of yeast and fungi, including clinical isolates of A. flavus, A. fumigatus, F. oxysporum, F. solani, C. albicans, and C. neoformans (MICs = C. albicans (MICs = 0.015-8 µg/ml).{48763} It inhibits ergosterol biosynthesis in C. albicans, C. glabrata, A. fumigatus, and A. flavus (IC50s = 0.03-1 µg/ml).{24400} Voriconazole (10 mg/kg twice per day, i.v.) decreases the number of lung colony-forming units (CFUs), reduces alveolar collapse and lung inflammatory cell infiltration and necrosis, and increases survival in a rat model of invasive pulmonary aspergillosis.{48764} Formulations containing voriconazole have been used in the treatment of fungal infections.
Brand:CaymanSKU:- Voriconazole is a triazole antifungal agent and a derivative of fluconazole (Item No. 11594).{48762,48763} It is active against a variety of yeast and fungi, including clinical isolates of A. flavus, A. fumigatus, F. oxysporum, F. solani, C. albicans, and C. neoformans (MICs = C. albicans (MICs = 0.015-8 µg/ml).{48763} It inhibits ergosterol biosynthesis in C. albicans, C. glabrata, A. fumigatus, and A. flavus (IC50s = 0.03-1 µg/ml).{24400} Voriconazole (10 mg/kg twice per day, i.v.) decreases the number of lung colony-forming units (CFUs), reduces alveolar collapse and lung inflammatory cell infiltration and necrosis, and increases survival in a rat model of invasive pulmonary aspergillosis.{48764} Formulations containing voriconazole have been used in the treatment of fungal infections.
Brand:CaymanSKU:- Voriconazole is a triazole antifungal agent and a derivative of fluconazole (Item No. 11594).{48762,48763} It is active against a variety of yeast and fungi, including clinical isolates of A. flavus, A. fumigatus, F. oxysporum, F. solani, C. albicans, and C. neoformans (MICs = C. albicans (MICs = 0.015-8 µg/ml).{48763} It inhibits ergosterol biosynthesis in C. albicans, C. glabrata, A. fumigatus, and A. flavus (IC50s = 0.03-1 µg/ml).{24400} Voriconazole (10 mg/kg twice per day, i.v.) decreases the number of lung colony-forming units (CFUs), reduces alveolar collapse and lung inflammatory cell infiltration and necrosis, and increases survival in a rat model of invasive pulmonary aspergillosis.{48764} Formulations containing voriconazole have been used in the treatment of fungal infections.
Brand:CaymanSKU:-
Voriconazole N-oxide is a major metabolite of the triazole antifungal voriconazole (Item No. 15633).{48321} It is formed via oxidation of voriconazole by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2C19.
Brand:CaymanSKU:28047 - 1 mgAvailable on backorder
Voriconazole N-oxide is a major metabolite of the triazole antifungal voriconazole (Item No. 15633).{48321} It is formed via oxidation of voriconazole by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2C19.
Brand:CaymanSKU:28047 - 10 mgAvailable on backorder
Voriconazole N-oxide is a major metabolite of the triazole antifungal voriconazole (Item No. 15633).{48321} It is formed via oxidation of voriconazole by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2C19.
Brand:CaymanSKU:28047 - 5 mgAvailable on backorder
Vortioxetine is a multimodal serotonergic agent that acts as a serotonin (5-HT; Item No. 14332) reuptake inhibitor (Ki = 1.6 nM) and binds to the 5-HT1A, 5-HT1B, 5-HT3A, and 5-HT7 receptors (Kis = 15, 33, 3.7, and 19 nM, respectively).{36248} It also binds to the β1-adrenergic receptor (Ki = 46 nM). It acts as an antagonist at 5-HT3A and 5-HT7, a partial agonist at 5-HT1B, and a full agonist at 5-HT1A receptors. Vortioxetine is selective for the serotonin transporter (SERT) over the dopamine and norepinephrine transporters (IC50s = 5.3, 890, and 140 nM, respectively). It has affinity for histamine H2, melanocortin 4, β2-adrenergic, 5-HT2C, and 5-HT6 receptors with Ki values greater than 180 nM, but it is selective over the majority of targets in a panel of 75 ion channels, G protein-coupled receptors, enzymes, and transporters. Vortioxetine (5 or 10 mg/kg per day) increases 5-HT levels in vivo in rat brain and decreases occupancy at SERT. At acute and chronic doses of 5 mg/kg, but not 10 mg/kg, it increases the time mice spend in the center of the open field test, increases mobility in the forced swim test, and decreases the latency to feed in the novelty suppressed feeding test.{36249} It also increases proliferation and survival of adult-born granule cells in the hippocampus. Formulations containing vortioxetine have been used in the treatment of major depressive disorder.
Brand:CaymanSKU:30183 - 10 mgAvailable on backorder
Vortioxetine is a multimodal serotonergic agent that acts as a serotonin (5-HT; Item No. 14332) reuptake inhibitor (Ki = 1.6 nM) and binds to the 5-HT1A, 5-HT1B, 5-HT3A, and 5-HT7 receptors (Kis = 15, 33, 3.7, and 19 nM, respectively).{36248} It also binds to the β1-adrenergic receptor (Ki = 46 nM). It acts as an antagonist at 5-HT3A and 5-HT7, a partial agonist at 5-HT1B, and a full agonist at 5-HT1A receptors. Vortioxetine is selective for the serotonin transporter (SERT) over the dopamine and norepinephrine transporters (IC50s = 5.3, 890, and 140 nM, respectively). It has affinity for histamine H2, melanocortin 4, β2-adrenergic, 5-HT2C, and 5-HT6 receptors with Ki values greater than 180 nM, but it is selective over the majority of targets in a panel of 75 ion channels, G protein-coupled receptors, enzymes, and transporters. Vortioxetine (5 or 10 mg/kg per day) increases 5-HT levels in vivo in rat brain and decreases occupancy at SERT. At acute and chronic doses of 5 mg/kg, but not 10 mg/kg, it increases the time mice spend in the center of the open field test, increases mobility in the forced swim test, and decreases the latency to feed in the novelty suppressed feeding test.{36249} It also increases proliferation and survival of adult-born granule cells in the hippocampus. Formulations containing vortioxetine have been used in the treatment of major depressive disorder.
Brand:CaymanSKU:30183 - 25 mgAvailable on backorder
Vortioxetine is a multimodal serotonergic agent that acts as a serotonin (5-HT; Item No. 14332) reuptake inhibitor (Ki = 1.6 nM) and binds to the 5-HT1A, 5-HT1B, 5-HT3A, and 5-HT7 receptors (Kis = 15, 33, 3.7, and 19 nM, respectively).{36248} It also binds to the β1-adrenergic receptor (Ki = 46 nM). It acts as an antagonist at 5-HT3A and 5-HT7, a partial agonist at 5-HT1B, and a full agonist at 5-HT1A receptors. Vortioxetine is selective for the serotonin transporter (SERT) over the dopamine and norepinephrine transporters (IC50s = 5.3, 890, and 140 nM, respectively). It has affinity for histamine H2, melanocortin 4, β2-adrenergic, 5-HT2C, and 5-HT6 receptors with Ki values greater than 180 nM, but it is selective over the majority of targets in a panel of 75 ion channels, G protein-coupled receptors, enzymes, and transporters. Vortioxetine (5 or 10 mg/kg per day) increases 5-HT levels in vivo in rat brain and decreases occupancy at SERT. At acute and chronic doses of 5 mg/kg, but not 10 mg/kg, it increases the time mice spend in the center of the open field test, increases mobility in the forced swim test, and decreases the latency to feed in the novelty suppressed feeding test.{36249} It also increases proliferation and survival of adult-born granule cells in the hippocampus. Formulations containing vortioxetine have been used in the treatment of major depressive disorder.
Brand:CaymanSKU:30183 - 5 mgAvailable on backorder
Vortioxetine is a multimodal serotonergic agent that acts as a serotonin (5-HT; Item No. 14332) reuptake inhibitor (Ki = 1.6 nM) and binds to the 5-HT1A, 5-HT1B, 5-HT3A, and 5-HT7 receptors (Kis = 15, 33, 3.7, and 19 nM, respectively).{36248} It also binds to the β1-adrenergic receptor (Ki = 46 nM). It acts as an antagonist at 5-HT3A and 5-HT7, a partial agonist at 5-HT1B, and a full agonist at 5-HT1A receptors. Vortioxetine is selective for the serotonin transporter (SERT) over the dopamine and norepinephrine transporters (IC50s = 5.3, 890, and 140 nM, respectively). It has affinity for histamine H2, melanocortin 4, β2-adrenergic, 5-HT2C, and 5-HT6 receptors with Ki values greater than 180 nM, but it is selective over the majority of targets in a panel of 75 ion channels, G protein-coupled receptors, enzymes, and transporters. Vortioxetine (5 or 10 mg/kg per day) increases 5-HT levels in vivo in rat brain and decreases occupancy at SERT. At acute and chronic doses of 5 mg/kg, but not 10 mg/kg, it increases the time mice spend in the center of the open field test, increases mobility in the forced swim test, and decreases the latency to feed in the novelty suppressed feeding test.{36249} It also increases proliferation and survival of adult-born granule cells in the hippocampus. Formulations containing vortioxetine have been used in the treatment of major depressive disorder.
Brand:CaymanSKU:30183 - 50 mgAvailable on backorder
Vortioxetine is a multimodal serotonergic agent that acts as a serotonin (5-HT; Item No. 14332) reuptake inhibitor (Ki = 1.6 nM) and binds to the 5-HT1A, 5-HT1B, 5-HT3A, and 5-HT7 receptors (Kis = 15, 33, 3.7, and 19 nM, respectively).{36248} It also binds to the β1-adrenergic receptor (Ki = 46 nM). It acts as an antagonist at 5-HT3A and 5-HT7, a partial agonist at 5-HT1B, and a full agonist at 5-HT1A receptors. Vortioxetine is selective for the serotonin transporter (SERT) over the dopamine and norepinephrine transporters (IC50s = 5.3, 890, and 140 nM, respectively). It has affinity for histamine H2, melanocortin 4, β2-adrenergic, 5-HT2C, and 5-HT6 receptors with Ki values greater than 180 nM, but it is selective over the majority of targets in a panel of 75 ion channels, G protein-coupled receptors, enzymes, and transporters. Vortioxetine (5 or 10 mg/kg per day) increases 5-HT levels in vivo in rat brain and decreases occupancy at SERT. At acute and chronic doses of 5 mg/kg, but not 10 mg/kg, it increases the time mice spend in the center of the open field test, increases mobility in the forced swim test, and decreases the latency to feed in the novelty suppressed feeding test.{36249} It also increases proliferation and survival of adult-born granule cells in the hippocampus. Formulations containing vortioxetine have been used in the treatment of major depressive disorder.
Brand:CaymanSKU:23694 - 1 mgAvailable on backorder
Vortioxetine is a multimodal serotonergic agent that acts as a serotonin (5-HT; Item No. 14332) reuptake inhibitor (Ki = 1.6 nM) and binds to the 5-HT1A, 5-HT1B, 5-HT3A, and 5-HT7 receptors (Kis = 15, 33, 3.7, and 19 nM, respectively).{36248} It also binds to the β1-adrenergic receptor (Ki = 46 nM). It acts as an antagonist at 5-HT3A and 5-HT7, a partial agonist at 5-HT1B, and a full agonist at 5-HT1A receptors. Vortioxetine is selective for the serotonin transporter (SERT) over the dopamine and norepinephrine transporters (IC50s = 5.3, 890, and 140 nM, respectively). It has affinity for histamine H2, melanocortin 4, β2-adrenergic, 5-HT2C, and 5-HT6 receptors with Ki values greater than 180 nM, but it is selective over the majority of targets in a panel of 75 ion channels, G protein-coupled receptors, enzymes, and transporters. Vortioxetine (5 or 10 mg/kg per day) increases 5-HT levels in vivo in rat brain and decreases occupancy at SERT. At acute and chronic doses of 5 mg/kg, but not 10 mg/kg, it increases the time mice spend in the center of the open field test, increases mobility in the forced swim test, and decreases the latency to feed in the novelty suppressed feeding test.{36249} It also increases proliferation and survival of adult-born granule cells in the hippocampus. Formulations containing vortioxetine have been used in the treatment of major depressive disorder.
Brand:CaymanSKU:23694 - 10 mgAvailable on backorder
Vortioxetine is a multimodal serotonergic agent that acts as a serotonin (5-HT; Item No. 14332) reuptake inhibitor (Ki = 1.6 nM) and binds to the 5-HT1A, 5-HT1B, 5-HT3A, and 5-HT7 receptors (Kis = 15, 33, 3.7, and 19 nM, respectively).{36248} It also binds to the β1-adrenergic receptor (Ki = 46 nM). It acts as an antagonist at 5-HT3A and 5-HT7, a partial agonist at 5-HT1B, and a full agonist at 5-HT1A receptors. Vortioxetine is selective for the serotonin transporter (SERT) over the dopamine and norepinephrine transporters (IC50s = 5.3, 890, and 140 nM, respectively). It has affinity for histamine H2, melanocortin 4, β2-adrenergic, 5-HT2C, and 5-HT6 receptors with Ki values greater than 180 nM, but it is selective over the majority of targets in a panel of 75 ion channels, G protein-coupled receptors, enzymes, and transporters. Vortioxetine (5 or 10 mg/kg per day) increases 5-HT levels in vivo in rat brain and decreases occupancy at SERT. At acute and chronic doses of 5 mg/kg, but not 10 mg/kg, it increases the time mice spend in the center of the open field test, increases mobility in the forced swim test, and decreases the latency to feed in the novelty suppressed feeding test.{36249} It also increases proliferation and survival of adult-born granule cells in the hippocampus. Formulations containing vortioxetine have been used in the treatment of major depressive disorder.
Brand:CaymanSKU:23694 - 5 mgAvailable on backorder
Vortioxetine-d8 is intended for use as an internal standard for the quantification of vortioxetine (Item No. 23694) by GC- or LC-MS. Vortioxetine is a multimodal serotonergic agent that acts as a serotonin (5-HT; Item No. 14332) reuptake inhibitor (Ki = 1.6 nM) and binds to the 5-HT1A, 5-HT1B, 5-HT3A, and 5-HT7 receptors (Kis = 15, 33, 3.7, and 19 nM, respectively).{36248} It also binds to the β1-adrenergic receptor (Ki = 46 nM). It acts as an antagonist at 5-HT3A and 5-HT7, a partial agonist at 5-HT1B, and a full agonist at 5-HT1A receptors. Vortioxetine is selective for the serotonin transporter (SERT) over the dopamine and norepinephrine transporters (IC50s = 5.3, 890, and 140 nM, respectively). It has affinity for histamine H2, melanocortin 4, β2-adrenergic, 5-HT2C, and 5-HT6 receptors with Ki values greater than 180 nM, but it is selective over the majority of targets in a panel of 75 ion channels, G protein-coupled receptors, enzymes, and transporters. Vortioxetine (5 or 10 mg/kg per day) increases 5-HT levels in vivo in rat brain and decreases occupancy at SERT. At acute and chronic doses of 5 mg/kg, but not 10 mg/kg, it increases the time mice spend in the center of the open field test, increases mobility in the forced swim test, and decreases the latency to feed in the novelty suppressed feeding test.{36249} It also increases proliferation and survival of adult-born granule cells in the hippocampus. Formulations containing vortioxetine have been used in the treatment of major depressive disorder.
Brand:CaymanSKU:28163 - 1 mgAvailable on backorder
Voruciclib is a pan-inhibitor of cyclin-dependent kinases (CDKs; Kis = 0.626-9.1 nM).{47780} It is selective for CDKs over male germ cell associated kinase (MAK) and intestinal cell kinase (ICK; Kis = 259 and 481 nM, respectively), in a panel of 48 kinases. Voruciclib decreases myeloid cell leukemia-1 (Mcl-1) levels and increases cleaved poly(ADP-ribose) polymerase (PARP) levels in six diffuse large B-cell lymphoma (DLBCL) cell lines when used at concentrations ranging from 0.5 to 5 µM. It reduces tumor growth by 56.3% in a Ri-1 mouse xenograft model when administered at a dose of 200 mg/kg.
Brand:CaymanSKU:29085 - 1 mgAvailable on backorder
Voruciclib is a pan-inhibitor of cyclin-dependent kinases (CDKs; Kis = 0.626-9.1 nM).{47780} It is selective for CDKs over male germ cell associated kinase (MAK) and intestinal cell kinase (ICK; Kis = 259 and 481 nM, respectively), in a panel of 48 kinases. Voruciclib decreases myeloid cell leukemia-1 (Mcl-1) levels and increases cleaved poly(ADP-ribose) polymerase (PARP) levels in six diffuse large B-cell lymphoma (DLBCL) cell lines when used at concentrations ranging from 0.5 to 5 µM. It reduces tumor growth by 56.3% in a Ri-1 mouse xenograft model when administered at a dose of 200 mg/kg.
Brand:CaymanSKU:29085 - 10 mgAvailable on backorder
Voruciclib is a pan-inhibitor of cyclin-dependent kinases (CDKs; Kis = 0.626-9.1 nM).{47780} It is selective for CDKs over male germ cell associated kinase (MAK) and intestinal cell kinase (ICK; Kis = 259 and 481 nM, respectively), in a panel of 48 kinases. Voruciclib decreases myeloid cell leukemia-1 (Mcl-1) levels and increases cleaved poly(ADP-ribose) polymerase (PARP) levels in six diffuse large B-cell lymphoma (DLBCL) cell lines when used at concentrations ranging from 0.5 to 5 µM. It reduces tumor growth by 56.3% in a Ri-1 mouse xenograft model when administered at a dose of 200 mg/kg.
Brand:CaymanSKU:29085 - 5 mgAvailable on backorder
Vosaroxin is an inhibitor of topoisomerase II.{58000} It induces relaxation of supercoiled DNA with an IC50 value of 3.2 µg/ml in a cell-free assay. It induces DNA double-strand breaks in CCRF-CEM cells and cell cycle arrest at the G2 phase in A549 cells in a concentration-dependent manner.{58001} Vosaroxin inhibits proliferation in a panel of 15 cancer cell lines, including cancer cells resistant to doxorubicin (Item No. 15007), etoposide (Item No. 12092), or cisplatin (Item No. 13119), with IC50 values ranging from 0.04 to 1.15 µM.{58002} It inhibits tumor growth in multidrug-resistant SBC-3/ETP or PC-14/CDDP mouse xenograft models when administered at a dose of 20 mg/kg.
Brand:CaymanSKU:30614 - 1 mgAvailable on backorder
Vosaroxin is an inhibitor of topoisomerase II.{58000} It induces relaxation of supercoiled DNA with an IC50 value of 3.2 µg/ml in a cell-free assay. It induces DNA double-strand breaks in CCRF-CEM cells and cell cycle arrest at the G2 phase in A549 cells in a concentration-dependent manner.{58001} Vosaroxin inhibits proliferation in a panel of 15 cancer cell lines, including cancer cells resistant to doxorubicin (Item No. 15007), etoposide (Item No. 12092), or cisplatin (Item No. 13119), with IC50 values ranging from 0.04 to 1.15 µM.{58002} It inhibits tumor growth in multidrug-resistant SBC-3/ETP or PC-14/CDDP mouse xenograft models when administered at a dose of 20 mg/kg.
Brand:CaymanSKU:30614 - 10 mgAvailable on backorder
Vosaroxin is an inhibitor of topoisomerase II.{58000} It induces relaxation of supercoiled DNA with an IC50 value of 3.2 µg/ml in a cell-free assay. It induces DNA double-strand breaks in CCRF-CEM cells and cell cycle arrest at the G2 phase in A549 cells in a concentration-dependent manner.{58001} Vosaroxin inhibits proliferation in a panel of 15 cancer cell lines, including cancer cells resistant to doxorubicin (Item No. 15007), etoposide (Item No. 12092), or cisplatin (Item No. 13119), with IC50 values ranging from 0.04 to 1.15 µM.{58002} It inhibits tumor growth in multidrug-resistant SBC-3/ETP or PC-14/CDDP mouse xenograft models when administered at a dose of 20 mg/kg.
Brand:CaymanSKU:30614 - 25 mgAvailable on backorder
Vosaroxin is an inhibitor of topoisomerase II.{58000} It induces relaxation of supercoiled DNA with an IC50 value of 3.2 µg/ml in a cell-free assay. It induces DNA double-strand breaks in CCRF-CEM cells and cell cycle arrest at the G2 phase in A549 cells in a concentration-dependent manner.{58001} Vosaroxin inhibits proliferation in a panel of 15 cancer cell lines, including cancer cells resistant to doxorubicin (Item No. 15007), etoposide (Item No. 12092), or cisplatin (Item No. 13119), with IC50 values ranging from 0.04 to 1.15 µM.{58002} It inhibits tumor growth in multidrug-resistant SBC-3/ETP or PC-14/CDDP mouse xenograft models when administered at a dose of 20 mg/kg.
Brand:CaymanSKU:30614 - 5 mgAvailable on backorder
Voxtalisib is a dual inhibitor of PI3K and mammalian target of rapamycin complex (mTORC; IC50s = 39, 110, 43, 9, 160, and 910 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, mTORC1, and mTORC2, respectively).{56000} It is selective for these kinases over vacuolar protein sorting 34 (VPS34; IC50 = 9,100 nM) and a panel of 130 additional protein kinases at 1.5 µM but does inhibit DNA protein kinase (DNA-PK; IC50 = 150 nM). Voxtalisib decreases EGF-induced production of PIP3, a product of PI3K-mediated PIP2 metabolism, in PC3 prostate cancer cells with an IC50 value of 290 nM. It also reduces phosphorylation of the PI3K and mTORC targets Akt and ribosomal protein S6 (S6RP) in the same model (IC50s = 250 and 120 nM, respectively). Voxtalisib inhibits proliferation and colony formation of PC3 cells (IC50s = 1,800 and 270 nM, respectively). It reduces tumor growth and increases survival in a GBM-39 glioblastoma multiforme (GBM) mouse xenograft model when administered at a dose of 30 mg/kg twice per day alone or in combination with temozolomide (Item No. 14163).{27545}
Brand:CaymanSKU:30323 - 10 mgAvailable on backorder
Voxtalisib is a dual inhibitor of PI3K and mammalian target of rapamycin complex (mTORC; IC50s = 39, 110, 43, 9, 160, and 910 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, mTORC1, and mTORC2, respectively).{56000} It is selective for these kinases over vacuolar protein sorting 34 (VPS34; IC50 = 9,100 nM) and a panel of 130 additional protein kinases at 1.5 µM but does inhibit DNA protein kinase (DNA-PK; IC50 = 150 nM). Voxtalisib decreases EGF-induced production of PIP3, a product of PI3K-mediated PIP2 metabolism, in PC3 prostate cancer cells with an IC50 value of 290 nM. It also reduces phosphorylation of the PI3K and mTORC targets Akt and ribosomal protein S6 (S6RP) in the same model (IC50s = 250 and 120 nM, respectively). Voxtalisib inhibits proliferation and colony formation of PC3 cells (IC50s = 1,800 and 270 nM, respectively). It reduces tumor growth and increases survival in a GBM-39 glioblastoma multiforme (GBM) mouse xenograft model when administered at a dose of 30 mg/kg twice per day alone or in combination with temozolomide (Item No. 14163).{27545}
Brand:CaymanSKU:30323 - 25 mgAvailable on backorder
Voxtalisib is a dual inhibitor of PI3K and mammalian target of rapamycin complex (mTORC; IC50s = 39, 110, 43, 9, 160, and 910 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, mTORC1, and mTORC2, respectively).{56000} It is selective for these kinases over vacuolar protein sorting 34 (VPS34; IC50 = 9,100 nM) and a panel of 130 additional protein kinases at 1.5 µM but does inhibit DNA protein kinase (DNA-PK; IC50 = 150 nM). Voxtalisib decreases EGF-induced production of PIP3, a product of PI3K-mediated PIP2 metabolism, in PC3 prostate cancer cells with an IC50 value of 290 nM. It also reduces phosphorylation of the PI3K and mTORC targets Akt and ribosomal protein S6 (S6RP) in the same model (IC50s = 250 and 120 nM, respectively). Voxtalisib inhibits proliferation and colony formation of PC3 cells (IC50s = 1,800 and 270 nM, respectively). It reduces tumor growth and increases survival in a GBM-39 glioblastoma multiforme (GBM) mouse xenograft model when administered at a dose of 30 mg/kg twice per day alone or in combination with temozolomide (Item No. 14163).{27545}
Brand:CaymanSKU:30323 - 5 mgAvailable on backorder
Voxtalisib is a dual inhibitor of PI3K and mammalian target of rapamycin complex (mTORC; IC50s = 39, 110, 43, 9, 160, and 910 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, mTORC1, and mTORC2, respectively).{56000} It is selective for these kinases over vacuolar protein sorting 34 (VPS34; IC50 = 9,100 nM) and a panel of 130 additional protein kinases at 1.5 µM but does inhibit DNA protein kinase (DNA-PK; IC50 = 150 nM). Voxtalisib decreases EGF-induced production of PIP3, a product of PI3K-mediated PIP2 metabolism, in PC3 prostate cancer cells with an IC50 value of 290 nM. It also reduces phosphorylation of the PI3K and mTORC targets Akt and ribosomal protein S6 (S6RP) in the same model (IC50s = 250 and 120 nM, respectively). Voxtalisib inhibits proliferation and colony formation of PC3 cells (IC50s = 1,800 and 270 nM, respectively). It reduces tumor growth and increases survival in a GBM-39 glioblastoma multiforme (GBM) mouse xenograft model when administered at a dose of 30 mg/kg twice per day alone or in combination with temozolomide (Item No. 14163).{27545}
Brand:CaymanSKU:30323 - 50 mgAvailable on backorder
Respiratory syncytial virus (RSV) is the leading cause of respiratory tract infections in humans. RSV F protein, which mediates fusion of the viral envelope with the host cell membrane, has become a target of anti-RSV treatment. VP-14637 is a small molecule inhibitor of RSV that demonstrates antiviral activity with an EC50 value of 1.4 nM.{28943,28944} It interferes directly with RSV fusion (EC50 = 5.4 nM), binding to the viral F protein, which allows simultaneous interaction with both of the heptad repeat domains of the F protein trimer.{28943,28944}
Brand:CaymanSKU:-Available on backorder
Respiratory syncytial virus (RSV) is the leading cause of respiratory tract infections in humans. RSV F protein, which mediates fusion of the viral envelope with the host cell membrane, has become a target of anti-RSV treatment. VP-14637 is a small molecule inhibitor of RSV that demonstrates antiviral activity with an EC50 value of 1.4 nM.{28943,28944} It interferes directly with RSV fusion (EC50 = 5.4 nM), binding to the viral F protein, which allows simultaneous interaction with both of the heptad repeat domains of the F protein trimer.{28943,28944}
Brand:CaymanSKU:-Available on backorder
Respiratory syncytial virus (RSV) is the leading cause of respiratory tract infections in humans. RSV F protein, which mediates fusion of the viral envelope with the host cell membrane, has become a target of anti-RSV treatment. VP-14637 is a small molecule inhibitor of RSV that demonstrates antiviral activity with an EC50 value of 1.4 nM.{28943,28944} It interferes directly with RSV fusion (EC50 = 5.4 nM), binding to the viral F protein, which allows simultaneous interaction with both of the heptad repeat domains of the F protein trimer.{28943,28944}
Brand:CaymanSKU:-Available on backorder
Sphingosine-1-phosphate (S1P; Item No. 62570) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis.{11895,12477,10628} It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8.{11895,12477} VPC 23019 is an aryl amide-containing S1P analog that acts as a competitive antagonist at both S1P1 and S1P3 receptors (pKis = 7.86 and 5.93, respectively).{12407} It can inhibit S1P-induced migration of thyroid cancer cells, ovarian cancer cells, and neural stem cells.{17724}
Brand:CaymanSKU:- Sphingosine-1-phosphate (S1P; Item No. 62570) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis.{11895,12477,10628} It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8.{11895,12477} VPC 23019 is an aryl amide-containing S1P analog that acts as a competitive antagonist at both S1P1 and S1P3 receptors (pKis = 7.86 and 5.93, respectively).{12407} It can inhibit S1P-induced migration of thyroid cancer cells, ovarian cancer cells, and neural stem cells.{17724}
Brand:CaymanSKU:- Sphingosine-1-phosphate (S1P; Item No. 62570) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis.{11895,12477,10628} It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8.{11895,12477} VPC 23019 is an aryl amide-containing S1P analog that acts as a competitive antagonist at both S1P1 and S1P3 receptors (pKis = 7.86 and 5.93, respectively).{12407} It can inhibit S1P-induced migration of thyroid cancer cells, ovarian cancer cells, and neural stem cells.{17724}
Brand:CaymanSKU:- Sphingosine-1-phosphate (S1P; Item No. 62570) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis.{11895,12477,10628} It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8.{11895,12477} VPC 23019 is an aryl amide-containing S1P analog that acts as a competitive antagonist at both S1P1 and S1P3 receptors (pKis = 7.86 and 5.93, respectively).{12407} It can inhibit S1P-induced migration of thyroid cancer cells, ovarian cancer cells, and neural stem cells.{17724}
Brand:CaymanSKU:-
Vps34-IN1 is a potent inhibitor of the class III phosphoinositide 3-kinase (PI3K) vacuolar protein sorting 34 (Vps34; IC50 = 25 nM in vitro).{31851} It does not significantly inhibit the activity of over 340 additional kinases, including class I and II PI3Ks. Vps34-IN1 dose-dependently inhibits generation of PtdIns-(3)-p, which is essential to the formation and trafficking of endsomes and autophagosomes, without affecting the ability of class I PI3K to regulate Akt. It induces a rapid and pronounced loss of phosphorylation on serum- and glucocorticoid-regulated kinase 3.
Brand:CaymanSKU:-Available on backorder
Vps34-IN1 is a potent inhibitor of the class III phosphoinositide 3-kinase (PI3K) vacuolar protein sorting 34 (Vps34; IC50 = 25 nM in vitro).{31851} It does not significantly inhibit the activity of over 340 additional kinases, including class I and II PI3Ks. Vps34-IN1 dose-dependently inhibits generation of PtdIns-(3)-p, which is essential to the formation and trafficking of endsomes and autophagosomes, without affecting the ability of class I PI3K to regulate Akt. It induces a rapid and pronounced loss of phosphorylation on serum- and glucocorticoid-regulated kinase 3.
Brand:CaymanSKU:-Available on backorder
Vps34-IN1 is a potent inhibitor of the class III phosphoinositide 3-kinase (PI3K) vacuolar protein sorting 34 (Vps34; IC50 = 25 nM in vitro).{31851} It does not significantly inhibit the activity of over 340 additional kinases, including class I and II PI3Ks. Vps34-IN1 dose-dependently inhibits generation of PtdIns-(3)-p, which is essential to the formation and trafficking of endsomes and autophagosomes, without affecting the ability of class I PI3K to regulate Akt. It induces a rapid and pronounced loss of phosphorylation on serum- and glucocorticoid-regulated kinase 3.
Brand:CaymanSKU:-Available on backorder
Vps34-IN1 is a potent inhibitor of the class III phosphoinositide 3-kinase (PI3K) vacuolar protein sorting 34 (Vps34; IC50 = 25 nM in vitro).{31851} It does not significantly inhibit the activity of over 340 additional kinases, including class I and II PI3Ks. Vps34-IN1 dose-dependently inhibits generation of PtdIns-(3)-p, which is essential to the formation and trafficking of endsomes and autophagosomes, without affecting the ability of class I PI3K to regulate Akt. It induces a rapid and pronounced loss of phosphorylation on serum- and glucocorticoid-regulated kinase 3.
Brand:CaymanSKU:-Available on backorder
VR23 is a chloroquine (Item No. 14194) derivative that functions as a proteasome inhibitor (IC50s = 1 nM, 50-100 nM, and 3 µM for trypsin-like, chymotrypsin-like, and caspase-like proteasomes, respectively).{30904} It also deregulates the activity of cyclin E and other centrosomal proteins, resulting in the induction of multiple centrosome amplification, abnormal spindle formation, uneven cytokinesis, irreversible mitotic arrest, and eventually apoptosis that is specific to cancer cells.{30904} In combination with the chymotrypsin-like proteasome inhibitor bortezomib (Item No. 10008822), VR23 can produce a synergistic effect in killing multiple myeloma cells, including those that are resistant to bortezomib.{30904}
Brand:CaymanSKU:-Available on backorder
VR23 is a chloroquine (Item No. 14194) derivative that functions as a proteasome inhibitor (IC50s = 1 nM, 50-100 nM, and 3 µM for trypsin-like, chymotrypsin-like, and caspase-like proteasomes, respectively).{30904} It also deregulates the activity of cyclin E and other centrosomal proteins, resulting in the induction of multiple centrosome amplification, abnormal spindle formation, uneven cytokinesis, irreversible mitotic arrest, and eventually apoptosis that is specific to cancer cells.{30904} In combination with the chymotrypsin-like proteasome inhibitor bortezomib (Item No. 10008822), VR23 can produce a synergistic effect in killing multiple myeloma cells, including those that are resistant to bortezomib.{30904}
Brand:CaymanSKU:-Available on backorder
VR23 is a chloroquine (Item No. 14194) derivative that functions as a proteasome inhibitor (IC50s = 1 nM, 50-100 nM, and 3 µM for trypsin-like, chymotrypsin-like, and caspase-like proteasomes, respectively).{30904} It also deregulates the activity of cyclin E and other centrosomal proteins, resulting in the induction of multiple centrosome amplification, abnormal spindle formation, uneven cytokinesis, irreversible mitotic arrest, and eventually apoptosis that is specific to cancer cells.{30904} In combination with the chymotrypsin-like proteasome inhibitor bortezomib (Item No. 10008822), VR23 can produce a synergistic effect in killing multiple myeloma cells, including those that are resistant to bortezomib.{30904}
Brand:CaymanSKU:-Available on backorder
VR23 is a chloroquine (Item No. 14194) derivative that functions as a proteasome inhibitor (IC50s = 1 nM, 50-100 nM, and 3 µM for trypsin-like, chymotrypsin-like, and caspase-like proteasomes, respectively).{30904} It also deregulates the activity of cyclin E and other centrosomal proteins, resulting in the induction of multiple centrosome amplification, abnormal spindle formation, uneven cytokinesis, irreversible mitotic arrest, and eventually apoptosis that is specific to cancer cells.{30904} In combination with the chymotrypsin-like proteasome inhibitor bortezomib (Item No. 10008822), VR23 can produce a synergistic effect in killing multiple myeloma cells, including those that are resistant to bortezomib.{30904}
Brand:CaymanSKU:-Available on backorder
Phosphatidylinositol 3-kinase (PI3K) signaling through Akt/PKB and the mammalian target of rapamycin (mTOR) controls gene expression related to cell proliferation, differentiation, and apoptosis. Increased activity of this pathway is important in many types of cancer. VS-5584 is a purine analog that inhibits mTOR (IC50 = 37 nM) and PI3K (IC50s = 16, 68, 25, and 42 nM for the α, β, γ, and δ isoforms, respectively) without relevant activity against more than 400 additional lipid and protein kinases.{27667} By inhibiting the phosphorylation of substrates downstream of PI3K and mTOR, VS-5584 demonstrates broad anti-proliferative sensitivity leading to tumor growth inhibition in human tumor models.{27667}
Brand:CaymanSKU:-Out of stock
Phosphatidylinositol 3-kinase (PI3K) signaling through Akt/PKB and the mammalian target of rapamycin (mTOR) controls gene expression related to cell proliferation, differentiation, and apoptosis. Increased activity of this pathway is important in many types of cancer. VS-5584 is a purine analog that inhibits mTOR (IC50 = 37 nM) and PI3K (IC50s = 16, 68, 25, and 42 nM for the α, β, γ, and δ isoforms, respectively) without relevant activity against more than 400 additional lipid and protein kinases.{27667} By inhibiting the phosphorylation of substrates downstream of PI3K and mTOR, VS-5584 demonstrates broad anti-proliferative sensitivity leading to tumor growth inhibition in human tumor models.{27667}
Brand:CaymanSKU:-Out of stock
Phosphatidylinositol 3-kinase (PI3K) signaling through Akt/PKB and the mammalian target of rapamycin (mTOR) controls gene expression related to cell proliferation, differentiation, and apoptosis. Increased activity of this pathway is important in many types of cancer. VS-5584 is a purine analog that inhibits mTOR (IC50 = 37 nM) and PI3K (IC50s = 16, 68, 25, and 42 nM for the α, β, γ, and δ isoforms, respectively) without relevant activity against more than 400 additional lipid and protein kinases.{27667} By inhibiting the phosphorylation of substrates downstream of PI3K and mTOR, VS-5584 demonstrates broad anti-proliferative sensitivity leading to tumor growth inhibition in human tumor models.{27667}
Brand:CaymanSKU:-Out of stock
VS-5584 analog is a dual inhibitor of PI3Kα and mammalian target of rapamycin (mTOR; IC50s = 17 and 150 nM, respectively).{46913} It is a desmethyl analog of the dual PI3K/mTOR inhibitor VS-5584 (Item No. 16294).
Brand:CaymanSKU:30324 - 1 mgAvailable on backorder
VS-5584 analog is a dual inhibitor of PI3Kα and mammalian target of rapamycin (mTOR; IC50s = 17 and 150 nM, respectively).{46913} It is a desmethyl analog of the dual PI3K/mTOR inhibitor VS-5584 (Item No. 16294).
Brand:CaymanSKU:30324 - 10 mgAvailable on backorder
VS-5584 analog is a dual inhibitor of PI3Kα and mammalian target of rapamycin (mTOR; IC50s = 17 and 150 nM, respectively).{46913} It is a desmethyl analog of the dual PI3K/mTOR inhibitor VS-5584 (Item No. 16294).
Brand:CaymanSKU:30324 - 25 mgAvailable on backorder
VS-5584 analog is a dual inhibitor of PI3Kα and mammalian target of rapamycin (mTOR; IC50s = 17 and 150 nM, respectively).{46913} It is a desmethyl analog of the dual PI3K/mTOR inhibitor VS-5584 (Item No. 16294).
Brand:CaymanSKU:30324 - 5 mgAvailable on backorder
VTP-27999 is a renin inhibitor (IC50 = 0.47 nM for the recombinant human enzyme).{53713} It is selective for renin over the aspartyl proteases β-secretase, cathepsin D, and cathepsin E at 10 µM and is greater than 1,000-fold selective for renin over a panel of more than 250 receptors, ion channels, and enzymes. VTP-27999 (10 mg/kg, p.o.) reduces mean arterial pressure in rats expressing human renin and angiotensinogen, a double-transgenic model for angiotensin II-dependent hypertension.
Brand:CaymanSKU:27689 - 1 mgAvailable on backorder
VTP-27999 is a renin inhibitor (IC50 = 0.47 nM for the recombinant human enzyme).{53713} It is selective for renin over the aspartyl proteases β-secretase, cathepsin D, and cathepsin E at 10 µM and is greater than 1,000-fold selective for renin over a panel of more than 250 receptors, ion channels, and enzymes. VTP-27999 (10 mg/kg, p.o.) reduces mean arterial pressure in rats expressing human renin and angiotensinogen, a double-transgenic model for angiotensin II-dependent hypertension.
Brand:CaymanSKU:27689 - 10 mgAvailable on backorder
VTP-27999 is a renin inhibitor (IC50 = 0.47 nM for the recombinant human enzyme).{53713} It is selective for renin over the aspartyl proteases β-secretase, cathepsin D, and cathepsin E at 10 µM and is greater than 1,000-fold selective for renin over a panel of more than 250 receptors, ion channels, and enzymes. VTP-27999 (10 mg/kg, p.o.) reduces mean arterial pressure in rats expressing human renin and angiotensinogen, a double-transgenic model for angiotensin II-dependent hypertension.
Brand:CaymanSKU:27689 - 25 mgAvailable on backorder
VTP-27999 is a renin inhibitor (IC50 = 0.47 nM for the recombinant human enzyme).{53713} It is selective for renin over the aspartyl proteases β-secretase, cathepsin D, and cathepsin E at 10 µM and is greater than 1,000-fold selective for renin over a panel of more than 250 receptors, ion channels, and enzymes. VTP-27999 (10 mg/kg, p.o.) reduces mean arterial pressure in rats expressing human renin and angiotensinogen, a double-transgenic model for angiotensin II-dependent hypertension.
Brand:CaymanSKU:27689 - 5 mgAvailable on backorder
VU0029251 is a partial antagonist of metabotropic glutamate receptor 5 (mGluR5; Ki = 1.07 µM).{47575} It inhibits calcium mobilization induced by glutamate in HEK293 cell membranes expressing rat mGluR5 (IC50 = 1.7 µM).
Brand:CaymanSKU:21987 -Out of stock
VU0029251 is a partial antagonist of metabotropic glutamate receptor 5 (mGluR5; Ki = 1.07 µM).{47575} It inhibits calcium mobilization induced by glutamate in HEK293 cell membranes expressing rat mGluR5 (IC50 = 1.7 µM).
Brand:CaymanSKU:21987 -Out of stock
VU0029251 is a partial antagonist of metabotropic glutamate receptor 5 (mGluR5; Ki = 1.07 µM).{47575} It inhibits calcium mobilization induced by glutamate in HEK293 cell membranes expressing rat mGluR5 (IC50 = 1.7 µM).
Brand:CaymanSKU:21987 -Out of stock
VU0029251 is a partial antagonist of metabotropic glutamate receptor 5 (mGluR5; Ki = 1.07 µM).{47575} It inhibits calcium mobilization induced by glutamate in HEK293 cell membranes expressing rat mGluR5 (IC50 = 1.7 µM).
Brand:CaymanSKU:21987 -Out of stock
VU0071063 is a potent and selective activator of the inward-rectifier potassium channel (Kir) 6.2 and sulfonylurea receptor (SUR) 1 (EC50 = 7 µM using whole cell patch clamp electrophysiology).{34016} It is selective for SUR1-containing Kir6.1 or Kir6.2 channels over SUR2A, Kir2.1, Kir2.2, Kir2.3, Kir3.1/3/2, and voltage-gated potassium channel 2.1. VU0071063 inhibits glucose-stimulated calcium entry in isolated mouse pancreatic β-cells.
Brand:CaymanSKU:21897 -Out of stock
VU0071063 is a potent and selective activator of the inward-rectifier potassium channel (Kir) 6.2 and sulfonylurea receptor (SUR) 1 (EC50 = 7 µM using whole cell patch clamp electrophysiology).{34016} It is selective for SUR1-containing Kir6.1 or Kir6.2 channels over SUR2A, Kir2.1, Kir2.2, Kir2.3, Kir3.1/3/2, and voltage-gated potassium channel 2.1. VU0071063 inhibits glucose-stimulated calcium entry in isolated mouse pancreatic β-cells.
Brand:CaymanSKU:21897 -Out of stock