Chemicals
Showing 25651–25800 of 41137 results
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Lusutrombopag is an agonist of the thrombopoietin receptor.{45125} It induces proliferation of Ba/F3 cells expressing human MPL, the gene for the thrombopoietin receptor, with an EC50 value of 84 nM but not of those expressing mouse Mpl.{45126} Lusutrombopag (0.3-10 mg/kg per day) increases the number of circulating platelets in a transgenic mouse model expressing human MPL and increases the number of megakaryocytes in the bone marrow when administered at a dose of 10 mg/kg per day. Formulations containing lusutrombopag have been used in the treatment of thrombocytopenia in adult patients with chronic liver disease scheduled to undergo invasive procedures.
Brand:CaymanSKU:26533 - 50 mgAvailable on backorder
Lutein is a dietary carotenoid that has been found in eggs and yellow-colored fruits and vegetables and has diverse biological activities.{56228,56230,56229,56231} It reduces hyperglycemia-induced mitochondrial DNA damage and production of reactive oxygen species (ROS) and promotes mitochondrial biogenesis in ARPE-19 cells when used at a concentration of 10 µM.{56228} Lutein (20 mg/kg) increases nitric oxide (NO) production and decreases serum levels of endothelin-1 (Item No. 24127) in a rat model of hyperhomocysteinemia.{56230} Dietary administration of lutein (0.2%) decreases monocyte migration and lesion size in an ApoE-/- and Ldlr-/- mouse models of atherosclerosis. Lutein reduces infarct size and cardiac malondialdehyde (MDA), lactate dehydrogenase (LDH), and troponin T levels, and increases cardiac levels of catalase (CAT), superoxide dismutase (SOD), heme oxygenase-1 (HO-1), and Nrf2 in a rat model of heart failure induced by isoproterenol (Item No. 15592).{56229} It forms a retinal pigment in human eyes, and high dietary intake of lutein is positively correlated with reduced risk of age-related macular degeneration and cataracts in humans.{56231}
Brand:CaymanSKU:10010811 - 1 mgAvailable on backorder
Lutein is a dietary carotenoid that has been found in eggs and yellow-colored fruits and vegetables and has diverse biological activities.{56228,56230,56229,56231} It reduces hyperglycemia-induced mitochondrial DNA damage and production of reactive oxygen species (ROS) and promotes mitochondrial biogenesis in ARPE-19 cells when used at a concentration of 10 µM.{56228} Lutein (20 mg/kg) increases nitric oxide (NO) production and decreases serum levels of endothelin-1 (Item No. 24127) in a rat model of hyperhomocysteinemia.{56230} Dietary administration of lutein (0.2%) decreases monocyte migration and lesion size in an ApoE-/- and Ldlr-/- mouse models of atherosclerosis. Lutein reduces infarct size and cardiac malondialdehyde (MDA), lactate dehydrogenase (LDH), and troponin T levels, and increases cardiac levels of catalase (CAT), superoxide dismutase (SOD), heme oxygenase-1 (HO-1), and Nrf2 in a rat model of heart failure induced by isoproterenol (Item No. 15592).{56229} It forms a retinal pigment in human eyes, and high dietary intake of lutein is positively correlated with reduced risk of age-related macular degeneration and cataracts in humans.{56231}
Brand:CaymanSKU:10010811 - 10 mgAvailable on backorder
Lutein is a dietary carotenoid that has been found in eggs and yellow-colored fruits and vegetables and has diverse biological activities.{56228,56230,56229,56231} It reduces hyperglycemia-induced mitochondrial DNA damage and production of reactive oxygen species (ROS) and promotes mitochondrial biogenesis in ARPE-19 cells when used at a concentration of 10 µM.{56228} Lutein (20 mg/kg) increases nitric oxide (NO) production and decreases serum levels of endothelin-1 (Item No. 24127) in a rat model of hyperhomocysteinemia.{56230} Dietary administration of lutein (0.2%) decreases monocyte migration and lesion size in an ApoE-/- and Ldlr-/- mouse models of atherosclerosis. Lutein reduces infarct size and cardiac malondialdehyde (MDA), lactate dehydrogenase (LDH), and troponin T levels, and increases cardiac levels of catalase (CAT), superoxide dismutase (SOD), heme oxygenase-1 (HO-1), and Nrf2 in a rat model of heart failure induced by isoproterenol (Item No. 15592).{56229} It forms a retinal pigment in human eyes, and high dietary intake of lutein is positively correlated with reduced risk of age-related macular degeneration and cataracts in humans.{56231}
Brand:CaymanSKU:10010811 - 25 mgAvailable on backorder
Lutein is a dietary carotenoid that has been found in eggs and yellow-colored fruits and vegetables and has diverse biological activities.{56228,56230,56229,56231} It reduces hyperglycemia-induced mitochondrial DNA damage and production of reactive oxygen species (ROS) and promotes mitochondrial biogenesis in ARPE-19 cells when used at a concentration of 10 µM.{56228} Lutein (20 mg/kg) increases nitric oxide (NO) production and decreases serum levels of endothelin-1 (Item No. 24127) in a rat model of hyperhomocysteinemia.{56230} Dietary administration of lutein (0.2%) decreases monocyte migration and lesion size in an ApoE-/- and Ldlr-/- mouse models of atherosclerosis. Lutein reduces infarct size and cardiac malondialdehyde (MDA), lactate dehydrogenase (LDH), and troponin T levels, and increases cardiac levels of catalase (CAT), superoxide dismutase (SOD), heme oxygenase-1 (HO-1), and Nrf2 in a rat model of heart failure induced by isoproterenol (Item No. 15592).{56229} It forms a retinal pigment in human eyes, and high dietary intake of lutein is positively correlated with reduced risk of age-related macular degeneration and cataracts in humans.{56231}
Brand:CaymanSKU:10010811 - 5 mgAvailable on backorder
Luteolin is a polyphenolic flavone found in many plants including soybeans and perilla leaves.{11740} Luteolin is one of the most potent flavanoid inhibitors of soybean and reticulocyte 15-lipoxygenases, with an IC50 of 0.6 µM.{11260} Luteolin has also been found to inhibit the release of TNFα from neutrophils, and to inhibit matrix metalloproteinases.{11743}
Brand:CaymanSKU:10004161 - 10 mgAvailable on backorder
Luteolin is a polyphenolic flavone found in many plants including soybeans and perilla leaves.{11740} Luteolin is one of the most potent flavanoid inhibitors of soybean and reticulocyte 15-lipoxygenases, with an IC50 of 0.6 µM.{11260} Luteolin has also been found to inhibit the release of TNFα from neutrophils, and to inhibit matrix metalloproteinases.{11743}
Brand:CaymanSKU:10004161 - 100 mgAvailable on backorder
Luteolin is a polyphenolic flavone found in many plants including soybeans and perilla leaves.{11740} Luteolin is one of the most potent flavanoid inhibitors of soybean and reticulocyte 15-lipoxygenases, with an IC50 of 0.6 µM.{11260} Luteolin has also been found to inhibit the release of TNFα from neutrophils, and to inhibit matrix metalloproteinases.{11743}
Brand:CaymanSKU:10004161 - 50 mgAvailable on backorder
Luteolin is a polyphenolic flavone found in many plants including soybeans and perilla leaves.{11740} Luteolin is one of the most potent flavanoid inhibitors of soybean and reticulocyte 15-lipoxygenases, with an IC50 of 0.6 µM.{11260} Luteolin has also been found to inhibit the release of TNFα from neutrophils, and to inhibit matrix metalloproteinases.{11743}
Brand:CaymanSKU:10004161 - 500 mgAvailable on backorder
Luteoreticulin is a nitro-containing bacterial metabolite originally isolated from S. luteoreticuli.{43157} It has mosquitocidal activity against A. aegypti when used at a concentration of 6.25 mg/L and nematocidal activity against C. elegans.{43156}
Brand:CaymanSKU:25515 - 2.5 mgAvailable on backorder
Luteoreticulin is a nitro-containing bacterial metabolite originally isolated from S. luteoreticuli.{43157} It has mosquitocidal activity against A. aegypti when used at a concentration of 6.25 mg/L and nematocidal activity against C. elegans.{43156}
Brand:CaymanSKU:25515 - 500 µgAvailable on backorder
In addition to intrinsic antioxidant activities, melatonin (Item No. 14427) evokes its effects through the G protein-coupled receptors MT1A (MT1) and MT1B (MT2).{26016} Luzindole is a melatonin receptor antagonist that preferentially targets MT1B over MT1A (Ki values are = 10-27 and 158-513 nM, respectively).{26020,26015,26017} Luzindole is used both in vitro and in vivo to evaluate the roles of melatonin receptor signaling in diverse pathways, including circadian rhythms, animal behavior, and melanophore response.{26018,26019,26020}
Brand:CaymanSKU:- In addition to intrinsic antioxidant activities, melatonin (Item No. 14427) evokes its effects through the G protein-coupled receptors MT1A (MT1) and MT1B (MT2).{26016} Luzindole is a melatonin receptor antagonist that preferentially targets MT1B over MT1A (Ki values are = 10-27 and 158-513 nM, respectively).{26020,26015,26017} Luzindole is used both in vitro and in vivo to evaluate the roles of melatonin receptor signaling in diverse pathways, including circadian rhythms, animal behavior, and melanophore response.{26018,26019,26020}
Brand:CaymanSKU:- In addition to intrinsic antioxidant activities, melatonin (Item No. 14427) evokes its effects through the G protein-coupled receptors MT1A (MT1) and MT1B (MT2).{26016} Luzindole is a melatonin receptor antagonist that preferentially targets MT1B over MT1A (Ki values are = 10-27 and 158-513 nM, respectively).{26020,26015,26017} Luzindole is used both in vitro and in vivo to evaluate the roles of melatonin receptor signaling in diverse pathways, including circadian rhythms, animal behavior, and melanophore response.{26018,26019,26020}
Brand:CaymanSKU:- In addition to intrinsic antioxidant activities, melatonin (Item No. 14427) evokes its effects through the G protein-coupled receptors MT1A (MT1) and MT1B (MT2).{26016} Luzindole is a melatonin receptor antagonist that preferentially targets MT1B over MT1A (Ki values are = 10-27 and 158-513 nM, respectively).{26020,26015,26017} Luzindole is used both in vitro and in vivo to evaluate the roles of melatonin receptor signaling in diverse pathways, including circadian rhythms, animal behavior, and melanophore response.{26018,26019,26020}
Brand:CaymanSKU:-
Luzopeptin A is a cyclic depsipeptide antibiotic first isolated from an actinomycete strain.{29678,29676} It displays antitumor activity, as it is highly active in mice against a variety of experimental tumors.{29678} Luzopeptin A acts as a bifunctional DNA intercalator that strongly binds DNA and forms crosslinks between DNA molecules.{29675} It also inhibits reverse transcriptases from HIV-1 and HIV-2 (IC50s = 7 and 68 nM, respectively), as well as cellular DNA polymerases.{29677,29679}
Brand:CaymanSKU:-Available on backorder
Luzopeptin A is a cyclic depsipeptide antibiotic first isolated from an actinomycete strain.{29678,29676} It displays antitumor activity, as it is highly active in mice against a variety of experimental tumors.{29678} Luzopeptin A acts as a bifunctional DNA intercalator that strongly binds DNA and forms crosslinks between DNA molecules.{29675} It also inhibits reverse transcriptases from HIV-1 and HIV-2 (IC50s = 7 and 68 nM, respectively), as well as cellular DNA polymerases.{29677,29679}
Brand:CaymanSKU:-Available on backorder
LX2343 is an inhibitor of β-site amyloid protein cleaving enzyme 1 (BACE1/β-secretase; IC50 = 11.43 μM) and PI3K (IC50 = 15.99 μM).{47505} It inhibits accumulation of Aβ (1-40) (Aβ40) and Aβ42 induced by streptozotocin (STZ; Item No. 13104) in both HEK293-APPSW and CHO-APP cells, which express mutant and wild-type amyloid precursor protein (APP), respectively, in a concentration-dependent manner. It also inhibits STZ-induced increases in JNK and APPThr668 phosphorylation as well as soluble APPβ (sAPPβ) protein levels. LX2343 (10 mg/kg per day) reduces levels of Aβ40 and Aβ42, as well as thioflavine S staining, in the cortex and hippocampus in the APP/PS1 transgenic mouse model of Alzheimer’s disease. It also reduces cortical levels of PI3K, Akt, and mTOR phosphorylation and accumulation of the autophagy substrate p62, indicating increased autophagy. LX2343 (10 mg/kg per day) decreases path length and escape latency time in the Morris water maze in APP/PS1 mice.
Brand:CaymanSKU:27799 - 1 mgAvailable on backorder
LX2343 is an inhibitor of β-site amyloid protein cleaving enzyme 1 (BACE1/β-secretase; IC50 = 11.43 μM) and PI3K (IC50 = 15.99 μM).{47505} It inhibits accumulation of Aβ (1-40) (Aβ40) and Aβ42 induced by streptozotocin (STZ; Item No. 13104) in both HEK293-APPSW and CHO-APP cells, which express mutant and wild-type amyloid precursor protein (APP), respectively, in a concentration-dependent manner. It also inhibits STZ-induced increases in JNK and APPThr668 phosphorylation as well as soluble APPβ (sAPPβ) protein levels. LX2343 (10 mg/kg per day) reduces levels of Aβ40 and Aβ42, as well as thioflavine S staining, in the cortex and hippocampus in the APP/PS1 transgenic mouse model of Alzheimer’s disease. It also reduces cortical levels of PI3K, Akt, and mTOR phosphorylation and accumulation of the autophagy substrate p62, indicating increased autophagy. LX2343 (10 mg/kg per day) decreases path length and escape latency time in the Morris water maze in APP/PS1 mice.
Brand:CaymanSKU:27799 - 10 mgAvailable on backorder
LX2343 is an inhibitor of β-site amyloid protein cleaving enzyme 1 (BACE1/β-secretase; IC50 = 11.43 μM) and PI3K (IC50 = 15.99 μM).{47505} It inhibits accumulation of Aβ (1-40) (Aβ40) and Aβ42 induced by streptozotocin (STZ; Item No. 13104) in both HEK293-APPSW and CHO-APP cells, which express mutant and wild-type amyloid precursor protein (APP), respectively, in a concentration-dependent manner. It also inhibits STZ-induced increases in JNK and APPThr668 phosphorylation as well as soluble APPβ (sAPPβ) protein levels. LX2343 (10 mg/kg per day) reduces levels of Aβ40 and Aβ42, as well as thioflavine S staining, in the cortex and hippocampus in the APP/PS1 transgenic mouse model of Alzheimer’s disease. It also reduces cortical levels of PI3K, Akt, and mTOR phosphorylation and accumulation of the autophagy substrate p62, indicating increased autophagy. LX2343 (10 mg/kg per day) decreases path length and escape latency time in the Morris water maze in APP/PS1 mice.
Brand:CaymanSKU:27799 - 5 mgAvailable on backorder
LX7101 is a potent inhibitor of LIM kinase (LIMK) 1 and 2 and Rho-associated kinase 1 (ROCK-1) and ROCK-2 with IC50 values of 32, 4.3, 69, and 32 nM, respectively.{38221} It is selective, showing no cross reactivity in a panel of binding assays including 78 receptors and transporters and 430 additional kinases, at a concentration of 10 μM. Topical administration (3 μl of 1 mg/ml solution) of LX7101 to the eye reduces intraocular pressure in a dexamethasone-induced mouse model of glaucoma.
Brand:CaymanSKU:21209 -Out of stock
LX7101 is a potent inhibitor of LIM kinase (LIMK) 1 and 2 and Rho-associated kinase 1 (ROCK-1) and ROCK-2 with IC50 values of 32, 4.3, 69, and 32 nM, respectively.{38221} It is selective, showing no cross reactivity in a panel of binding assays including 78 receptors and transporters and 430 additional kinases, at a concentration of 10 μM. Topical administration (3 μl of 1 mg/ml solution) of LX7101 to the eye reduces intraocular pressure in a dexamethasone-induced mouse model of glaucoma.
Brand:CaymanSKU:21209 -Out of stock
LX7101 is a potent inhibitor of LIM kinase (LIMK) 1 and 2 and Rho-associated kinase 1 (ROCK-1) and ROCK-2 with IC50 values of 32, 4.3, 69, and 32 nM, respectively.{38221} It is selective, showing no cross reactivity in a panel of binding assays including 78 receptors and transporters and 430 additional kinases, at a concentration of 10 μM. Topical administration (3 μl of 1 mg/ml solution) of LX7101 to the eye reduces intraocular pressure in a dexamethasone-induced mouse model of glaucoma.
Brand:CaymanSKU:21209 -Out of stock
LXH254 is a pan-RAF inhibitor that selectively inhibits B-RAF and C-RAF over a panel of 456 human kinases.{46358} It inhibits MAPK signaling in tumor cells expressing mutant B-RAFV600. LXH254 induces tumor regression in various mouse xenograft models.
Brand:CaymanSKU:28231 - 1 mgAvailable on backorder
LXH254 is a pan-RAF inhibitor that selectively inhibits B-RAF and C-RAF over a panel of 456 human kinases.{46358} It inhibits MAPK signaling in tumor cells expressing mutant B-RAFV600. LXH254 induces tumor regression in various mouse xenograft models.
Brand:CaymanSKU:28231 - 10 mgAvailable on backorder
LXH254 is a pan-RAF inhibitor that selectively inhibits B-RAF and C-RAF over a panel of 456 human kinases.{46358} It inhibits MAPK signaling in tumor cells expressing mutant B-RAFV600. LXH254 induces tumor regression in various mouse xenograft models.
Brand:CaymanSKU:28231 - 25 mgAvailable on backorder
LXH254 is a pan-RAF inhibitor that selectively inhibits B-RAF and C-RAF over a panel of 456 human kinases.{46358} It inhibits MAPK signaling in tumor cells expressing mutant B-RAFV600. LXH254 induces tumor regression in various mouse xenograft models.
Brand:CaymanSKU:28231 - 5 mgAvailable on backorder
LXR-623 is a liver X receptor (LXR) modulator that acts as a partial agonist at LXRα and a full agonist at LXRβ (IC50s = 179 and 24 nM, respectively).{33455,32907} It is orally bioavailable and readily passes the blood-brain barrier.{33455,32907,32909} LXR-623 is anti-atherogenic in animal models of atherosclerosis, showing synergistic effects when combined with simvastatin (Item Nos. 10010344 | 10010345).{33455,33456,32907}
Brand:CaymanSKU:21117 -Out of stock
LXR-623 is a liver X receptor (LXR) modulator that acts as a partial agonist at LXRα and a full agonist at LXRβ (IC50s = 179 and 24 nM, respectively).{33455,32907} It is orally bioavailable and readily passes the blood-brain barrier.{33455,32907,32909} LXR-623 is anti-atherogenic in animal models of atherosclerosis, showing synergistic effects when combined with simvastatin (Item Nos. 10010344 | 10010345).{33455,33456,32907}
Brand:CaymanSKU:21117 -Out of stock
LXR-623 is a liver X receptor (LXR) modulator that acts as a partial agonist at LXRα and a full agonist at LXRβ (IC50s = 179 and 24 nM, respectively).{33455,32907} It is orally bioavailable and readily passes the blood-brain barrier.{33455,32907,32909} LXR-623 is anti-atherogenic in animal models of atherosclerosis, showing synergistic effects when combined with simvastatin (Item Nos. 10010344 | 10010345).{33455,33456,32907}
Brand:CaymanSKU:21117 -Out of stock
LXS-196 is a PKC inhibitor (IC50s = 1.9 and 0.4 nM for PKCα and PKCθ, respectively).{52782} It is selective for PKCα and PKCθ over GSK3β (IC50 = 3,100 nM). It inhibits proliferation of TMD8 B cell lymphoma and 92.1 uveal melanoma cells (IC50s = 900 and 184 nM, respectively) but not SK-MEL-28 skin melanoma cells (IC50 = >10,000 nM).
Brand:CaymanSKU:31455 - 1 mgAvailable on backorder
LXS-196 is a PKC inhibitor (IC50s = 1.9 and 0.4 nM for PKCα and PKCθ, respectively).{52782} It is selective for PKCα and PKCθ over GSK3β (IC50 = 3,100 nM). It inhibits proliferation of TMD8 B cell lymphoma and 92.1 uveal melanoma cells (IC50s = 900 and 184 nM, respectively) but not SK-MEL-28 skin melanoma cells (IC50 = >10,000 nM).
Brand:CaymanSKU:31455 - 10 mgAvailable on backorder
LXS-196 is a PKC inhibitor (IC50s = 1.9 and 0.4 nM for PKCα and PKCθ, respectively).{52782} It is selective for PKCα and PKCθ over GSK3β (IC50 = 3,100 nM). It inhibits proliferation of TMD8 B cell lymphoma and 92.1 uveal melanoma cells (IC50s = 900 and 184 nM, respectively) but not SK-MEL-28 skin melanoma cells (IC50 = >10,000 nM).
Brand:CaymanSKU:31455 - 25 mgAvailable on backorder
LXS-196 is a PKC inhibitor (IC50s = 1.9 and 0.4 nM for PKCα and PKCθ, respectively).{52782} It is selective for PKCα and PKCθ over GSK3β (IC50 = 3,100 nM). It inhibits proliferation of TMD8 B cell lymphoma and 92.1 uveal melanoma cells (IC50s = 900 and 184 nM, respectively) but not SK-MEL-28 skin melanoma cells (IC50 = >10,000 nM).
Brand:CaymanSKU:31455 - 5 mgAvailable on backorder
LY171883 is a selective, potent, orally active antagonist of the leukotriene D4 receptor.{1741} Dissociation constants (KB) for LY171883 on guinea pig ileum and parenchyma are 0.07 and 0.34 µM, respectively.{1741} LY171883 is an inhibitor of phosphodiesterase obtained from human polymorphonuclear leukocytes (IC50 of 22.6 µM) and various guinea pig tissues (IC50s range from 6.9-209 µM).{1741} At a concentration of 50-100 µM, LY171883 binds to the PPARγ nuclear receptor, inducing adipogenesis in cultured NIH3T3 fibroblasts.{1618,1425}
Brand:CaymanSKU:70710 - 10 mgAvailable on backorder
LY171883 is a selective, potent, orally active antagonist of the leukotriene D4 receptor.{1741} Dissociation constants (KB) for LY171883 on guinea pig ileum and parenchyma are 0.07 and 0.34 µM, respectively.{1741} LY171883 is an inhibitor of phosphodiesterase obtained from human polymorphonuclear leukocytes (IC50 of 22.6 µM) and various guinea pig tissues (IC50s range from 6.9-209 µM).{1741} At a concentration of 50-100 µM, LY171883 binds to the PPARγ nuclear receptor, inducing adipogenesis in cultured NIH3T3 fibroblasts.{1618,1425}
Brand:CaymanSKU:70710 - 100 mgAvailable on backorder
LY171883 is a selective, potent, orally active antagonist of the leukotriene D4 receptor.{1741} Dissociation constants (KB) for LY171883 on guinea pig ileum and parenchyma are 0.07 and 0.34 µM, respectively.{1741} LY171883 is an inhibitor of phosphodiesterase obtained from human polymorphonuclear leukocytes (IC50 of 22.6 µM) and various guinea pig tissues (IC50s range from 6.9-209 µM).{1741} At a concentration of 50-100 µM, LY171883 binds to the PPARγ nuclear receptor, inducing adipogenesis in cultured NIH3T3 fibroblasts.{1618,1425}
Brand:CaymanSKU:70710 - 5 mgAvailable on backorder
LY171883 is a selective, potent, orally active antagonist of the leukotriene D4 receptor.{1741} Dissociation constants (KB) for LY171883 on guinea pig ileum and parenchyma are 0.07 and 0.34 µM, respectively.{1741} LY171883 is an inhibitor of phosphodiesterase obtained from human polymorphonuclear leukocytes (IC50 of 22.6 µM) and various guinea pig tissues (IC50s range from 6.9-209 µM).{1741} At a concentration of 50-100 µM, LY171883 binds to the PPARγ nuclear receptor, inducing adipogenesis in cultured NIH3T3 fibroblasts.{1618,1425}
Brand:CaymanSKU:70710 - 50 mgAvailable on backorder
LY2090314 is potent and selective inhibitor of glycogen synthase kinase 3 (GSK3) with IC50 values of 1.5 and 0.9 nM for human recombinant GSK3α and GSK3β, respectively.{39184} It has >10-fold selectivity for GSK3 over a panel of 40 kinases at a concentration of 20 μM. LY2090314 induces time-dependent stabilization of β-catenin total protein and activates Wnt signaling in vitro. It has potent antiproliferative activity in BRAF wild-type/NRAS mutant and BRAF mutant melanoma cell lines (IC50s = 6.0-11.8 nM) but has limited to no activity in non-melanoma cell lines with (IC50s = 430 to >20,000 nM). Knockdown of β-catenin in A375 and M14 melanoma cells induces LY2090314 resistance in vitro, indicating that LY2090314-induced cell death is dependent upon Wnt activation. In vivo, LY2090314 reduces tumor volume in a murine A375 melanoma xenograft model as a single agent and synergizes with decabarzine for a greater antitumor effect. Formulations containing LY2090314 are under clinical investigation for the treatment of advanced solid tumors.{39185}
Brand:CaymanSKU:22211 -Out of stock
LY2090314 is potent and selective inhibitor of glycogen synthase kinase 3 (GSK3) with IC50 values of 1.5 and 0.9 nM for human recombinant GSK3α and GSK3β, respectively.{39184} It has >10-fold selectivity for GSK3 over a panel of 40 kinases at a concentration of 20 μM. LY2090314 induces time-dependent stabilization of β-catenin total protein and activates Wnt signaling in vitro. It has potent antiproliferative activity in BRAF wild-type/NRAS mutant and BRAF mutant melanoma cell lines (IC50s = 6.0-11.8 nM) but has limited to no activity in non-melanoma cell lines with (IC50s = 430 to >20,000 nM). Knockdown of β-catenin in A375 and M14 melanoma cells induces LY2090314 resistance in vitro, indicating that LY2090314-induced cell death is dependent upon Wnt activation. In vivo, LY2090314 reduces tumor volume in a murine A375 melanoma xenograft model as a single agent and synergizes with decabarzine for a greater antitumor effect. Formulations containing LY2090314 are under clinical investigation for the treatment of advanced solid tumors.{39185}
Brand:CaymanSKU:22211 -Out of stock
LY2090314 is potent and selective inhibitor of glycogen synthase kinase 3 (GSK3) with IC50 values of 1.5 and 0.9 nM for human recombinant GSK3α and GSK3β, respectively.{39184} It has >10-fold selectivity for GSK3 over a panel of 40 kinases at a concentration of 20 μM. LY2090314 induces time-dependent stabilization of β-catenin total protein and activates Wnt signaling in vitro. It has potent antiproliferative activity in BRAF wild-type/NRAS mutant and BRAF mutant melanoma cell lines (IC50s = 6.0-11.8 nM) but has limited to no activity in non-melanoma cell lines with (IC50s = 430 to >20,000 nM). Knockdown of β-catenin in A375 and M14 melanoma cells induces LY2090314 resistance in vitro, indicating that LY2090314-induced cell death is dependent upon Wnt activation. In vivo, LY2090314 reduces tumor volume in a murine A375 melanoma xenograft model as a single agent and synergizes with decabarzine for a greater antitumor effect. Formulations containing LY2090314 are under clinical investigation for the treatment of advanced solid tumors.{39185}
Brand:CaymanSKU:22211 -Out of stock
LY2090314 is potent and selective inhibitor of glycogen synthase kinase 3 (GSK3) with IC50 values of 1.5 and 0.9 nM for human recombinant GSK3α and GSK3β, respectively.{39184} It has >10-fold selectivity for GSK3 over a panel of 40 kinases at a concentration of 20 μM. LY2090314 induces time-dependent stabilization of β-catenin total protein and activates Wnt signaling in vitro. It has potent antiproliferative activity in BRAF wild-type/NRAS mutant and BRAF mutant melanoma cell lines (IC50s = 6.0-11.8 nM) but has limited to no activity in non-melanoma cell lines with (IC50s = 430 to >20,000 nM). Knockdown of β-catenin in A375 and M14 melanoma cells induces LY2090314 resistance in vitro, indicating that LY2090314-induced cell death is dependent upon Wnt activation. In vivo, LY2090314 reduces tumor volume in a murine A375 melanoma xenograft model as a single agent and synergizes with decabarzine for a greater antitumor effect. Formulations containing LY2090314 are under clinical investigation for the treatment of advanced solid tumors.{39185}
Brand:CaymanSKU:22211 -Out of stock
LY2157299 is a small molecule inhibitor of the TGF-β receptor type 1/type II kinases (IC50 = 69 nM).{25084} It has been used to study the role of TGF-β signaling in tumor cell migration and metastasis in pancreatic tumor cell lines where 5 μM of the compound completely disrupts Smad-2 phosphorylation, an immediate downstream target of the kinase activity.{25082} It can also suppress radiation-induced inflammatory cytokine signaling and proangiogenic genes, including ID1, in human primary fibrobalsts.{25083}
Brand:CaymanSKU:- LY2157299 is a small molecule inhibitor of the TGF-β receptor type 1/type II kinases (IC50 = 69 nM).{25084} It has been used to study the role of TGF-β signaling in tumor cell migration and metastasis in pancreatic tumor cell lines where 5 μM of the compound completely disrupts Smad-2 phosphorylation, an immediate downstream target of the kinase activity.{25082} It can also suppress radiation-induced inflammatory cytokine signaling and proangiogenic genes, including ID1, in human primary fibrobalsts.{25083}
Brand:CaymanSKU:- LY2157299 is a small molecule inhibitor of the TGF-β receptor type 1/type II kinases (IC50 = 69 nM).{25084} It has been used to study the role of TGF-β signaling in tumor cell migration and metastasis in pancreatic tumor cell lines where 5 μM of the compound completely disrupts Smad-2 phosphorylation, an immediate downstream target of the kinase activity.{25082} It can also suppress radiation-induced inflammatory cytokine signaling and proangiogenic genes, including ID1, in human primary fibrobalsts.{25083}
Brand:CaymanSKU:-
LY2119620 is a positive allosteric modulator of the M2 and M4 muscarinic acetylcholine receptors (mAChRs).{48128} It binds to allosteric sites on M2 and M4 receptors with KB values ranging from 1.8 to 3.4 μM. LY2119620 potentiates the activity of the AChR agonist acetylcholine (ACh; Item No. 23829) and the mAChR agonists iperoxo and oxotremorine M (Item No. 20847) at human recombinant M2 and M4 receptors expressed in CHO cell membranes. LY2119620 also exhibits allosteric agonism at M2 and M4 receptors (23.2 and 16.8%, respectively, of the maximal ACh response).
Brand:CaymanSKU:26373 - 1 mgAvailable on backorder
LY2119620 is a positive allosteric modulator of the M2 and M4 muscarinic acetylcholine receptors (mAChRs).{48128} It binds to allosteric sites on M2 and M4 receptors with KB values ranging from 1.8 to 3.4 μM. LY2119620 potentiates the activity of the AChR agonist acetylcholine (ACh; Item No. 23829) and the mAChR agonists iperoxo and oxotremorine M (Item No. 20847) at human recombinant M2 and M4 receptors expressed in CHO cell membranes. LY2119620 also exhibits allosteric agonism at M2 and M4 receptors (23.2 and 16.8%, respectively, of the maximal ACh response).
Brand:CaymanSKU:26373 - 10 mgAvailable on backorder
LY2119620 is a positive allosteric modulator of the M2 and M4 muscarinic acetylcholine receptors (mAChRs).{48128} It binds to allosteric sites on M2 and M4 receptors with KB values ranging from 1.8 to 3.4 μM. LY2119620 potentiates the activity of the AChR agonist acetylcholine (ACh; Item No. 23829) and the mAChR agonists iperoxo and oxotremorine M (Item No. 20847) at human recombinant M2 and M4 receptors expressed in CHO cell membranes. LY2119620 also exhibits allosteric agonism at M2 and M4 receptors (23.2 and 16.8%, respectively, of the maximal ACh response).
Brand:CaymanSKU:26373 - 5 mgAvailable on backorder
LY2157299 is a small molecule inhibitor of the TGF-β receptor type 1 kinase (IC50 = 56 nM).{24957} It has been used to study the role of TGF-β signaling in chemotherapy-induced expansion of cancer stem-like cells in triple negative breast cancer cell lines and xenografts.{24958} LY2157299 has also been shown to inhibit the migration and tumor growth of hepatocellular carcinoma cell lines by disrupting Smad-2 phosphorylation.{24959}
Brand:CaymanSKU:- LY2157299 is a small molecule inhibitor of the TGF-β receptor type 1 kinase (IC50 = 56 nM).{24957} It has been used to study the role of TGF-β signaling in chemotherapy-induced expansion of cancer stem-like cells in triple negative breast cancer cell lines and xenografts.{24958} LY2157299 has also been shown to inhibit the migration and tumor growth of hepatocellular carcinoma cell lines by disrupting Smad-2 phosphorylation.{24959}
Brand:CaymanSKU:- LY2157299 is a small molecule inhibitor of the TGF-β receptor type 1 kinase (IC50 = 56 nM).{24957} It has been used to study the role of TGF-β signaling in chemotherapy-induced expansion of cancer stem-like cells in triple negative breast cancer cell lines and xenografts.{24958} LY2157299 has also been shown to inhibit the migration and tumor growth of hepatocellular carcinoma cell lines by disrupting Smad-2 phosphorylation.{24959}
Brand:CaymanSKU:- LY2157299 is a small molecule inhibitor of the TGF-β receptor type 1 kinase (IC50 = 56 nM).{24957} It has been used to study the role of TGF-β signaling in chemotherapy-induced expansion of cancer stem-like cells in triple negative breast cancer cell lines and xenografts.{24958} LY2157299 has also been shown to inhibit the migration and tumor growth of hepatocellular carcinoma cell lines by disrupting Smad-2 phosphorylation.{24959}
Brand:CaymanSKU:-
LY2183240 is a potent, competitive inhibitor of anandamide uptake (IC50 = 270 pM; Ki = 540 pM) and hydrolysis.{14134,15431,16339} It increases anandamide levels in rat cerebellum (ED50 = 1.37 mg/kg) and displays dose-dependent efficacy (3-30 mg/kg) in several rodent models of persistent pain.{14134}
Brand:CaymanSKU:10008663 - 1 mgAvailable on backorder
LY2183240 is a potent, competitive inhibitor of anandamide uptake (IC50 = 270 pM; Ki = 540 pM) and hydrolysis.{14134,15431,16339} It increases anandamide levels in rat cerebellum (ED50 = 1.37 mg/kg) and displays dose-dependent efficacy (3-30 mg/kg) in several rodent models of persistent pain.{14134}
Brand:CaymanSKU:10008663 - 5 mgAvailable on backorder
LY2183240 (Item No. 10008663) is a potent, competitive small molecule inhibitor of anandamide uptake (IC50 = 270 pM; Ki = 540 pM) and hydrolysis.{14134,15431,16339} It has been shown to increase anandamide levels in rat cerebellum (ED50 = 1.37 mg/kg) and displays dose-dependent efficacy (3-30 mg/kg) in several rodent models of persistent pain.{14134} LY2183240 2’-isomer is a less potent, 2,5-regioisomer of LY2183240 that inhibits anandamide hydrolysis and uptake with IC50 values of 33 and 998 nM, respectively.{15431}
Brand:CaymanSKU:- LY2183240 (Item No. 10008663) is a potent, competitive small molecule inhibitor of anandamide uptake (IC50 = 270 pM; Ki = 540 pM) and hydrolysis.{14134,15431,16339} It has been shown to increase anandamide levels in rat cerebellum (ED50 = 1.37 mg/kg) and displays dose-dependent efficacy (3-30 mg/kg) in several rodent models of persistent pain.{14134} LY2183240 2’-isomer is a less potent, 2,5-regioisomer of LY2183240 that inhibits anandamide hydrolysis and uptake with IC50 values of 33 and 998 nM, respectively.{15431}
Brand:CaymanSKU:- LY2183240 (Item No. 10008663) is a potent, competitive small molecule inhibitor of anandamide uptake (IC50 = 270 pM; Ki = 540 pM) and hydrolysis.{14134,15431,16339} It has been shown to increase anandamide levels in rat cerebellum (ED50 = 1.37 mg/kg) and displays dose-dependent efficacy (3-30 mg/kg) in several rodent models of persistent pain.{14134} LY2183240 2’-isomer is a less potent, 2,5-regioisomer of LY2183240 that inhibits anandamide hydrolysis and uptake with IC50 values of 33 and 998 nM, respectively.{15431}
Brand:CaymanSKU:-
LY2228820 is a potent inhibitor of p38α MAP kinase (IC50 = 7 nM for human recombinant p38α).{39389} It inhibits LPS-induced TNF-α production in murine peritoneal macrophages and reduces phosphorylation of MAPKAPK-2 (MK2) in RAW 264.7 cells (IC50s = 5.2 and 34.3 nM, respectively). LY2228820 inhibits TNF-α production in LPS-treated mice and reduces paw swelling and cartilage destruction in a rat model of chronic inflammation with threshold minimum 50% doses (TMED50) values of <1, 1.5, and 1.5 mg/kg, respectively.
Brand:CaymanSKU:23259 - 1 mgAvailable on backorder
LY2228820 is a potent inhibitor of p38α MAP kinase (IC50 = 7 nM for human recombinant p38α).{39389} It inhibits LPS-induced TNF-α production in murine peritoneal macrophages and reduces phosphorylation of MAPKAPK-2 (MK2) in RAW 264.7 cells (IC50s = 5.2 and 34.3 nM, respectively). LY2228820 inhibits TNF-α production in LPS-treated mice and reduces paw swelling and cartilage destruction in a rat model of chronic inflammation with threshold minimum 50% doses (TMED50) values of <1, 1.5, and 1.5 mg/kg, respectively.
Brand:CaymanSKU:23259 - 10 mgAvailable on backorder
LY2228820 is a potent inhibitor of p38α MAP kinase (IC50 = 7 nM for human recombinant p38α).{39389} It inhibits LPS-induced TNF-α production in murine peritoneal macrophages and reduces phosphorylation of MAPKAPK-2 (MK2) in RAW 264.7 cells (IC50s = 5.2 and 34.3 nM, respectively). LY2228820 inhibits TNF-α production in LPS-treated mice and reduces paw swelling and cartilage destruction in a rat model of chronic inflammation with threshold minimum 50% doses (TMED50) values of <1, 1.5, and 1.5 mg/kg, respectively.
Brand:CaymanSKU:23259 - 25 mgAvailable on backorder
LY2228820 is a potent inhibitor of p38α MAP kinase (IC50 = 7 nM for human recombinant p38α).{39389} It inhibits LPS-induced TNF-α production in murine peritoneal macrophages and reduces phosphorylation of MAPKAPK-2 (MK2) in RAW 264.7 cells (IC50s = 5.2 and 34.3 nM, respectively). LY2228820 inhibits TNF-α production in LPS-treated mice and reduces paw swelling and cartilage destruction in a rat model of chronic inflammation with threshold minimum 50% doses (TMED50) values of <1, 1.5, and 1.5 mg/kg, respectively.
Brand:CaymanSKU:23259 - 5 mgAvailable on backorder
![A potent LTB4 receptor antagonist that inhibits the specific binding of [3H]-LTB4 to isolated human neutrophils with an IC50 value of 13.2 nM; inhibits the LTB4-induced aggregation of guinea pig and human neutrophils with IC50 values of 74 and 100 nM](https://interpriseusa.com/wp-content/uploads/2021/06/10010024.png)
Leukotriene B4 (LTB4) is a dihydroxy fatty acid derived from the 5-lipoxygenase pathway of arachidonic acid metabolism and is an important mediator of the inflammatory process. The benzophenone dicarboxylic acid derivative LY223982 is a potent BLT1 receptor antagonist. It inhibits the specific binding of radiolabeled-LTB4 to isolated human neutrophils with an IC50 value of 13.2 nM.{16067} LY223982 inhibits the leukotriene B4 (LTB4)-induced aggregation of guinea pig and human neutrophils with IC50 values of 74 and 100 nM, respectively.{16065} However, concentrations of LY223982 up to 10 µM do not inhibit binding of LTB4 to human BLT1 or BLT2 expressed in CHO cells.{9270}
Brand:CaymanSKU:10010024 - 1 mgAvailable on backorder
Leukotriene B4 (LTB4) is a dihydroxy fatty acid derived from the 5-lipoxygenase pathway of arachidonic acid metabolism and is an important mediator of the inflammatory process. The benzophenone dicarboxylic acid derivative LY223982 is a potent BLT1 receptor antagonist. It inhibits the specific binding of radiolabeled-LTB4 to isolated human neutrophils with an IC50 value of 13.2 nM.{16067} LY223982 inhibits the leukotriene B4 (LTB4)-induced aggregation of guinea pig and human neutrophils with IC50 values of 74 and 100 nM, respectively.{16065} However, concentrations of LY223982 up to 10 µM do not inhibit binding of LTB4 to human BLT1 or BLT2 expressed in CHO cells.{9270}
Brand:CaymanSKU:10010024 - 10 mgAvailable on backorder
Leukotriene B4 (LTB4) is a dihydroxy fatty acid derived from the 5-lipoxygenase pathway of arachidonic acid metabolism and is an important mediator of the inflammatory process. The benzophenone dicarboxylic acid derivative LY223982 is a potent BLT1 receptor antagonist. It inhibits the specific binding of radiolabeled-LTB4 to isolated human neutrophils with an IC50 value of 13.2 nM.{16067} LY223982 inhibits the leukotriene B4 (LTB4)-induced aggregation of guinea pig and human neutrophils with IC50 values of 74 and 100 nM, respectively.{16065} However, concentrations of LY223982 up to 10 µM do not inhibit binding of LTB4 to human BLT1 or BLT2 expressed in CHO cells.{9270}
Brand:CaymanSKU:10010024 - 25 mgAvailable on backorder
Leukotriene B4 (LTB4) is a dihydroxy fatty acid derived from the 5-lipoxygenase pathway of arachidonic acid metabolism and is an important mediator of the inflammatory process. The benzophenone dicarboxylic acid derivative LY223982 is a potent BLT1 receptor antagonist. It inhibits the specific binding of radiolabeled-LTB4 to isolated human neutrophils with an IC50 value of 13.2 nM.{16067} LY223982 inhibits the leukotriene B4 (LTB4)-induced aggregation of guinea pig and human neutrophils with IC50 values of 74 and 100 nM, respectively.{16065} However, concentrations of LY223982 up to 10 µM do not inhibit binding of LTB4 to human BLT1 or BLT2 expressed in CHO cells.{9270}
Brand:CaymanSKU:10010024 - 5 mgAvailable on backorder
LY2409881 is a selective inhibitor of IκB kinase β (IKK2; IC50 = 30 nM).{32487} It inhibits IKK1 and other common kinases at ≥10-fold higher concentrations.{32487} LY2409881 has been shown to suppress constitutively activated NF-κB and to induce apoptosis in lymphoma cells both in vitro and in preclinical mouse models of B and T cell lymphoma both as a single agent and in combination with histone deacetylase inhibitors.{32487}
Brand:CaymanSKU:-Available on backorder
LY2409881 is a selective inhibitor of IκB kinase β (IKK2; IC50 = 30 nM).{32487} It inhibits IKK1 and other common kinases at ≥10-fold higher concentrations.{32487} LY2409881 has been shown to suppress constitutively activated NF-κB and to induce apoptosis in lymphoma cells both in vitro and in preclinical mouse models of B and T cell lymphoma both as a single agent and in combination with histone deacetylase inhibitors.{32487}
Brand:CaymanSKU:-Available on backorder
LY2409881 is a selective inhibitor of IκB kinase β (IKK2; IC50 = 30 nM).{32487} It inhibits IKK1 and other common kinases at ≥10-fold higher concentrations.{32487} LY2409881 has been shown to suppress constitutively activated NF-κB and to induce apoptosis in lymphoma cells both in vitro and in preclinical mouse models of B and T cell lymphoma both as a single agent and in combination with histone deacetylase inhibitors.{32487}
Brand:CaymanSKU:-Available on backorder
LY2409881 is a selective inhibitor of IκB kinase β (IKK2; IC50 = 30 nM).{32487} It inhibits IKK1 and other common kinases at ≥10-fold higher concentrations.{32487} LY2409881 has been shown to suppress constitutively activated NF-κB and to induce apoptosis in lymphoma cells both in vitro and in preclinical mouse models of B and T cell lymphoma both as a single agent and in combination with histone deacetylase inhibitors.{32487}
Brand:CaymanSKU:-Available on backorder
Antagonists of the chemotactic and inflammatory lipoxygenase product leukotriene B4 (LTB4) have been potential drug development targets for several years.{4552,4553} The tetrazole LY255283 is a competitive antagonist of the BLT2 receptor. It displaces radiolabeled LTB4 from guinea pig lung membrane, with an IC50 of about 100 nM.{2084} LY255283 exhibits IC50 values of ~950 nM and >10 µM at human recombinant BLT2 and BLT1 receptors, respectively.{9270} LY255283 inhibits eosinophil chemotaxis by 80% at a concentration of 10 µM, and inhibits the binding of radiolabeled LTB4 to eosinophil membranes with an IC50 of 260 nM.{4552}
Brand:CaymanSKU:70715 - 1 mgAvailable on backorder
Antagonists of the chemotactic and inflammatory lipoxygenase product leukotriene B4 (LTB4) have been potential drug development targets for several years.{4552,4553} The tetrazole LY255283 is a competitive antagonist of the BLT2 receptor. It displaces radiolabeled LTB4 from guinea pig lung membrane, with an IC50 of about 100 nM.{2084} LY255283 exhibits IC50 values of ~950 nM and >10 µM at human recombinant BLT2 and BLT1 receptors, respectively.{9270} LY255283 inhibits eosinophil chemotaxis by 80% at a concentration of 10 µM, and inhibits the binding of radiolabeled LTB4 to eosinophil membranes with an IC50 of 260 nM.{4552}
Brand:CaymanSKU:70715 - 10 mgAvailable on backorder
Antagonists of the chemotactic and inflammatory lipoxygenase product leukotriene B4 (LTB4) have been potential drug development targets for several years.{4552,4553} The tetrazole LY255283 is a competitive antagonist of the BLT2 receptor. It displaces radiolabeled LTB4 from guinea pig lung membrane, with an IC50 of about 100 nM.{2084} LY255283 exhibits IC50 values of ~950 nM and >10 µM at human recombinant BLT2 and BLT1 receptors, respectively.{9270} LY255283 inhibits eosinophil chemotaxis by 80% at a concentration of 10 µM, and inhibits the binding of radiolabeled LTB4 to eosinophil membranes with an IC50 of 260 nM.{4552}
Brand:CaymanSKU:70715 - 25 mgAvailable on backorder
Antagonists of the chemotactic and inflammatory lipoxygenase product leukotriene B4 (LTB4) have been potential drug development targets for several years.{4552,4553} The tetrazole LY255283 is a competitive antagonist of the BLT2 receptor. It displaces radiolabeled LTB4 from guinea pig lung membrane, with an IC50 of about 100 nM.{2084} LY255283 exhibits IC50 values of ~950 nM and >10 µM at human recombinant BLT2 and BLT1 receptors, respectively.{9270} LY255283 inhibits eosinophil chemotaxis by 80% at a concentration of 10 µM, and inhibits the binding of radiolabeled LTB4 to eosinophil membranes with an IC50 of 260 nM.{4552}
Brand:CaymanSKU:70715 - 5 mgAvailable on backorder
LY2562175 is a farnesoid X receptor (FXR) agonist (EC50 = 193 nM in a reporter assay).{48622} It is selective for FXR over the glucocorticoid, androgen, mineralocorticoid, and progesterone receptors in HEK293 cells overexpressing the human receptors (EC50s = >10 µM for all in a radioligand binding assay). LY2562175 increases the interaction between FXR and steroid receptor coactivator 1 (SRC-1) with an EC50 value of 121 nM in a cell-free assay. It reduces plasma triglyceride and total cholesterol levels in LDL receptor-null mice (ED50s = 3.4 and 2 mg/kg, respectively). LY2562175 also decreases plasma LDL and increases HDL levels in Zucker diabetic fatty (ZDF) rats when administered at doses of 3, 10, and 30 mg/kg for nine days.
Brand:CaymanSKU:28912 - 1 mgAvailable on backorder
LY2562175 is a farnesoid X receptor (FXR) agonist (EC50 = 193 nM in a reporter assay).{48622} It is selective for FXR over the glucocorticoid, androgen, mineralocorticoid, and progesterone receptors in HEK293 cells overexpressing the human receptors (EC50s = >10 µM for all in a radioligand binding assay). LY2562175 increases the interaction between FXR and steroid receptor coactivator 1 (SRC-1) with an EC50 value of 121 nM in a cell-free assay. It reduces plasma triglyceride and total cholesterol levels in LDL receptor-null mice (ED50s = 3.4 and 2 mg/kg, respectively). LY2562175 also decreases plasma LDL and increases HDL levels in Zucker diabetic fatty (ZDF) rats when administered at doses of 3, 10, and 30 mg/kg for nine days.
Brand:CaymanSKU:28912 - 10 mgAvailable on backorder
LY2562175 is a farnesoid X receptor (FXR) agonist (EC50 = 193 nM in a reporter assay).{48622} It is selective for FXR over the glucocorticoid, androgen, mineralocorticoid, and progesterone receptors in HEK293 cells overexpressing the human receptors (EC50s = >10 µM for all in a radioligand binding assay). LY2562175 increases the interaction between FXR and steroid receptor coactivator 1 (SRC-1) with an EC50 value of 121 nM in a cell-free assay. It reduces plasma triglyceride and total cholesterol levels in LDL receptor-null mice (ED50s = 3.4 and 2 mg/kg, respectively). LY2562175 also decreases plasma LDL and increases HDL levels in Zucker diabetic fatty (ZDF) rats when administered at doses of 3, 10, and 30 mg/kg for nine days.
Brand:CaymanSKU:28912 - 25 mgAvailable on backorder
LY2562175 is a farnesoid X receptor (FXR) agonist (EC50 = 193 nM in a reporter assay).{48622} It is selective for FXR over the glucocorticoid, androgen, mineralocorticoid, and progesterone receptors in HEK293 cells overexpressing the human receptors (EC50s = >10 µM for all in a radioligand binding assay). LY2562175 increases the interaction between FXR and steroid receptor coactivator 1 (SRC-1) with an EC50 value of 121 nM in a cell-free assay. It reduces plasma triglyceride and total cholesterol levels in LDL receptor-null mice (ED50s = 3.4 and 2 mg/kg, respectively). LY2562175 also decreases plasma LDL and increases HDL levels in Zucker diabetic fatty (ZDF) rats when administered at doses of 3, 10, and 30 mg/kg for nine days.
Brand:CaymanSKU:28912 - 5 mgAvailable on backorder
p70 Ribosomal S6 kinase (p70S6K) is a serine/threonine kinase that is activated by insulin and growth factors through PI3K and mTORC1 signaling pathways. LY2584702 is a selective, cell-permeable p70S6K inhibitor (IC50 = 4 nM). It blocks phosphorylation of p70S6K in primary rat hepatocytes without affecting the phosphorylation of other signaling kinases, including GSK-3β and ERK1/2.{30510} LY2584702 inhibits phosphorylation of p70S6K in HCT116 colon cancer cells (IC50 = 0.1-0.24 μM in vitro) and demonstrates significant antitumor efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models.{30512} It also reverses the effects of mTORC1 hyperactivation on triglyceride metabolism in human hepatoma cells.{30511} LY2584702, alone or in combination with the mTOR inhibitor everolimus (Item No. 11597), has been evaluated in clinical trials against solid tumors.{30512,30509}
Brand:CaymanSKU:- p70 Ribosomal S6 kinase (p70S6K) is a serine/threonine kinase that is activated by insulin and growth factors through PI3K and mTORC1 signaling pathways. LY2584702 is a selective, cell-permeable p70S6K inhibitor (IC50 = 4 nM). It blocks phosphorylation of p70S6K in primary rat hepatocytes without affecting the phosphorylation of other signaling kinases, including GSK-3β and ERK1/2.{30510} LY2584702 inhibits phosphorylation of p70S6K in HCT116 colon cancer cells (IC50 = 0.1-0.24 μM in vitro) and demonstrates significant antitumor efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models.{30512} It also reverses the effects of mTORC1 hyperactivation on triglyceride metabolism in human hepatoma cells.{30511} LY2584702, alone or in combination with the mTOR inhibitor everolimus (Item No. 11597), has been evaluated in clinical trials against solid tumors.{30512,30509}
Brand:CaymanSKU:- p70 Ribosomal S6 kinase (p70S6K) is a serine/threonine kinase that is activated by insulin and growth factors through PI3K and mTORC1 signaling pathways. LY2584702 is a selective, cell-permeable p70S6K inhibitor (IC50 = 4 nM). It blocks phosphorylation of p70S6K in primary rat hepatocytes without affecting the phosphorylation of other signaling kinases, including GSK-3β and ERK1/2.{30510} LY2584702 inhibits phosphorylation of p70S6K in HCT116 colon cancer cells (IC50 = 0.1-0.24 μM in vitro) and demonstrates significant antitumor efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models.{30512} It also reverses the effects of mTORC1 hyperactivation on triglyceride metabolism in human hepatoma cells.{30511} LY2584702, alone or in combination with the mTOR inhibitor everolimus (Item No. 11597), has been evaluated in clinical trials against solid tumors.{30512,30509}
Brand:CaymanSKU:- p70 Ribosomal S6 kinase (p70S6K) is a serine/threonine kinase that is activated by insulin and growth factors through PI3K and mTORC1 signaling pathways. LY2584702 is a selective, cell-permeable p70S6K inhibitor (IC50 = 4 nM). It blocks phosphorylation of p70S6K in primary rat hepatocytes without affecting the phosphorylation of other signaling kinases, including GSK-3β and ERK1/2.{30510} LY2584702 inhibits phosphorylation of p70S6K in HCT116 colon cancer cells (IC50 = 0.1-0.24 μM in vitro) and demonstrates significant antitumor efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models.{30512} It also reverses the effects of mTORC1 hyperactivation on triglyceride metabolism in human hepatoma cells.{30511} LY2584702, alone or in combination with the mTOR inhibitor everolimus (Item No. 11597), has been evaluated in clinical trials against solid tumors.{30512,30509}
Brand:CaymanSKU:-