Chemicals
Showing 25801–25950 of 41137 results
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LY3009120 is an inhibitor of Raf kinases, including A-Raf, B-Raf, and c-Raf (IC50s = 44, 31-47, and 42 nM, respectively, in whole cell lysates).{33835,33836} It also inhibits B-Raf mutants V600E and V600E+G468A (IC50s = 5.8 and 17 nM, respectively, in biochemical assays).{33836} LY3009120 induces Raf dimerization and, unlike vemurafenib (PLX4032; Item No. 10618) and dabrafenib (Item No. 16989), inhibits kinase activity of induced dimers.{33836} It inhibits cell cycling in B-Raf or Ras mutant cancer cells and has significant antitumor activity in B-Raf and K-Ras mutant preclinical models of colorectal cancer.{33836,33837} LY3009120 is also active against B-Raf in-frame deletions in vitro and in mouse models.{33834}
Brand:CaymanSKU:21504 -Out of stock
LY3009120 is an inhibitor of Raf kinases, including A-Raf, B-Raf, and c-Raf (IC50s = 44, 31-47, and 42 nM, respectively, in whole cell lysates).{33835,33836} It also inhibits B-Raf mutants V600E and V600E+G468A (IC50s = 5.8 and 17 nM, respectively, in biochemical assays).{33836} LY3009120 induces Raf dimerization and, unlike vemurafenib (PLX4032; Item No. 10618) and dabrafenib (Item No. 16989), inhibits kinase activity of induced dimers.{33836} It inhibits cell cycling in B-Raf or Ras mutant cancer cells and has significant antitumor activity in B-Raf and K-Ras mutant preclinical models of colorectal cancer.{33836,33837} LY3009120 is also active against B-Raf in-frame deletions in vitro and in mouse models.{33834}
Brand:CaymanSKU:21504 -Out of stock
LY3009120 is an inhibitor of Raf kinases, including A-Raf, B-Raf, and c-Raf (IC50s = 44, 31-47, and 42 nM, respectively, in whole cell lysates).{33835,33836} It also inhibits B-Raf mutants V600E and V600E+G468A (IC50s = 5.8 and 17 nM, respectively, in biochemical assays).{33836} LY3009120 induces Raf dimerization and, unlike vemurafenib (PLX4032; Item No. 10618) and dabrafenib (Item No. 16989), inhibits kinase activity of induced dimers.{33836} It inhibits cell cycling in B-Raf or Ras mutant cancer cells and has significant antitumor activity in B-Raf and K-Ras mutant preclinical models of colorectal cancer.{33836,33837} LY3009120 is also active against B-Raf in-frame deletions in vitro and in mouse models.{33834}
Brand:CaymanSKU:21504 -Out of stock
LY303511 is a close structural analog of LY294002 (Item No. 70920), a selective phosphatidylinositol 3-kinase (PI3K) inhibitor.{32629} LY303511, however, does not inhibit PI3K-dependent phosphorylation of Akt but instead has been shown to inhibit mTOR-dependent phosphorylation of S6K.{32629} It can reduce cell proliferation in human lung epithelial adenocarcinoma cells, blocking G2/M progression and inhibiting casein kinase 2 activity.{32629} LY303511 demonstrates tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) sensitizing activity in HeLa cells that are refractory to TRAIL-induced apoptosis.{32630} LY303511 is also reported to block voltage-gated potassium (Kv) channels.{32631}
Brand:CaymanSKU:- LY303511 is a close structural analog of LY294002 (Item No. 70920), a selective phosphatidylinositol 3-kinase (PI3K) inhibitor.{32629} LY303511, however, does not inhibit PI3K-dependent phosphorylation of Akt but instead has been shown to inhibit mTOR-dependent phosphorylation of S6K.{32629} It can reduce cell proliferation in human lung epithelial adenocarcinoma cells, blocking G2/M progression and inhibiting casein kinase 2 activity.{32629} LY303511 demonstrates tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) sensitizing activity in HeLa cells that are refractory to TRAIL-induced apoptosis.{32630} LY303511 is also reported to block voltage-gated potassium (Kv) channels.{32631}
Brand:CaymanSKU:-
LY310762 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT1D (Ki = 249 nM for guinea pig receptors).{40403} It is selective for 5-HT1D over the 5-HT1B receptor, where it inhibits binding of radiolabeled citalopram by only 32% when used at a concentration of 1,000 nM. LY310762 potentiates 5-HT (Item No. 14332) release stimulated by potassium in guinea pig cortex (EC50 = 31 nM). It also reverses vasodilation induced by 5-HT in rat kidney perfused by phenylephrine (Item Nos. 17205 | 18619) when administered at a dose of 1 mg/kg.{40402}
Brand:CaymanSKU:22938 - 10 mgAvailable on backorder
LY310762 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT1D (Ki = 249 nM for guinea pig receptors).{40403} It is selective for 5-HT1D over the 5-HT1B receptor, where it inhibits binding of radiolabeled citalopram by only 32% when used at a concentration of 1,000 nM. LY310762 potentiates 5-HT (Item No. 14332) release stimulated by potassium in guinea pig cortex (EC50 = 31 nM). It also reverses vasodilation induced by 5-HT in rat kidney perfused by phenylephrine (Item Nos. 17205 | 18619) when administered at a dose of 1 mg/kg.{40402}
Brand:CaymanSKU:22938 - 25 mgAvailable on backorder
LY310762 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT1D (Ki = 249 nM for guinea pig receptors).{40403} It is selective for 5-HT1D over the 5-HT1B receptor, where it inhibits binding of radiolabeled citalopram by only 32% when used at a concentration of 1,000 nM. LY310762 potentiates 5-HT (Item No. 14332) release stimulated by potassium in guinea pig cortex (EC50 = 31 nM). It also reverses vasodilation induced by 5-HT in rat kidney perfused by phenylephrine (Item Nos. 17205 | 18619) when administered at a dose of 1 mg/kg.{40402}
Brand:CaymanSKU:22938 - 5 mgAvailable on backorder
Secreted phospholipase A2 (sPLA2) isoforms are low molecular weight, millimolar calcium-dependent enzymes that hydrolyze the fatty acid from the sn-2 position of membrane phospholipids.{18627} Group IIA sPLA2, also known as sPLA2IIA and non-pancreatic sPLA2, has roles in the regulation of eicosanoid synthesis and may modulate inflammatory signaling.{18627,10619} LY311727 is an inhibitor of Group IIA sPLA2 (IC50 = 0.47 µM) that interacts with the active site of the enzyme in a non-covalent manner.{10619,29121} It shows greater than 1,500-fold selectivity over pancreatic sPLA2 (Group IB sPLA2).{29121} LY311727 is commonly used to distinguish the actions of Group IIA sPLA2 from those of other sPLA2 isoforms in biological systems.{4458,7824,9354,8035}
Brand:CaymanSKU:-Available on backorder
Secreted phospholipase A2 (sPLA2) isoforms are low molecular weight, millimolar calcium-dependent enzymes that hydrolyze the fatty acid from the sn-2 position of membrane phospholipids.{18627} Group IIA sPLA2, also known as sPLA2IIA and non-pancreatic sPLA2, has roles in the regulation of eicosanoid synthesis and may modulate inflammatory signaling.{18627,10619} LY311727 is an inhibitor of Group IIA sPLA2 (IC50 = 0.47 µM) that interacts with the active site of the enzyme in a non-covalent manner.{10619,29121} It shows greater than 1,500-fold selectivity over pancreatic sPLA2 (Group IB sPLA2).{29121} LY311727 is commonly used to distinguish the actions of Group IIA sPLA2 from those of other sPLA2 isoforms in biological systems.{4458,7824,9354,8035}
Brand:CaymanSKU:-Available on backorder
Secreted phospholipase A2 (sPLA2) isoforms are low molecular weight, millimolar calcium-dependent enzymes that hydrolyze the fatty acid from the sn-2 position of membrane phospholipids.{18627} Group IIA sPLA2, also known as sPLA2IIA and non-pancreatic sPLA2, has roles in the regulation of eicosanoid synthesis and may modulate inflammatory signaling.{18627,10619} LY311727 is an inhibitor of Group IIA sPLA2 (IC50 = 0.47 µM) that interacts with the active site of the enzyme in a non-covalent manner.{10619,29121} It shows greater than 1,500-fold selectivity over pancreatic sPLA2 (Group IB sPLA2).{29121} LY311727 is commonly used to distinguish the actions of Group IIA sPLA2 from those of other sPLA2 isoforms in biological systems.{4458,7824,9354,8035}
Brand:CaymanSKU:-Available on backorder
LY315920 is an inhibitor of human group IIA (hGIIA) secretory phospholipase A2 (sPLA2; IC50 = 9 nM).{3601} It also potently inhibits human GIIE and GX isoforms, as well as the corresponding mouse isoforms, but poorly inhibits other PLA2 enzymes.{3601,30706,30705,12332} LY315920 inhibits sPLA2-induced release of thromboxane A2 from isolated guinea pig lung bronchoalveolar lavage cells (IC50 = 0.79 µM).{30706} Intravenous or oral administration of LY315920 to transgenic mice expressing human sPLA2 inhibits serum sPLA2 activity in a dose-related manner over four hours.{30706}
Brand:CaymanSKU:-Available on backorder
LY315920 is an inhibitor of human group IIA (hGIIA) secretory phospholipase A2 (sPLA2; IC50 = 9 nM).{3601} It also potently inhibits human GIIE and GX isoforms, as well as the corresponding mouse isoforms, but poorly inhibits other PLA2 enzymes.{3601,30706,30705,12332} LY315920 inhibits sPLA2-induced release of thromboxane A2 from isolated guinea pig lung bronchoalveolar lavage cells (IC50 = 0.79 µM).{30706} Intravenous or oral administration of LY315920 to transgenic mice expressing human sPLA2 inhibits serum sPLA2 activity in a dose-related manner over four hours.{30706}
Brand:CaymanSKU:-Available on backorder
LY315920 is an inhibitor of human group IIA (hGIIA) secretory phospholipase A2 (sPLA2; IC50 = 9 nM).{3601} It also potently inhibits human GIIE and GX isoforms, as well as the corresponding mouse isoforms, but poorly inhibits other PLA2 enzymes.{3601,30706,30705,12332} LY315920 inhibits sPLA2-induced release of thromboxane A2 from isolated guinea pig lung bronchoalveolar lavage cells (IC50 = 0.79 µM).{30706} Intravenous or oral administration of LY315920 to transgenic mice expressing human sPLA2 inhibits serum sPLA2 activity in a dose-related manner over four hours.{30706}
Brand:CaymanSKU:-Available on backorder
LY315920 is an inhibitor of human group IIA (hGIIA) secretory phospholipase A2 (sPLA2; IC50 = 9 nM).{3601} It also potently inhibits human GIIE and GX isoforms, as well as the corresponding mouse isoforms, but poorly inhibits other PLA2 enzymes.{3601,30706,30705,12332} LY315920 inhibits sPLA2-induced release of thromboxane A2 from isolated guinea pig lung bronchoalveolar lavage cells (IC50 = 0.79 µM).{30706} Intravenous or oral administration of LY315920 to transgenic mice expressing human sPLA2 inhibits serum sPLA2 activity in a dose-related manner over four hours.{30706}
Brand:CaymanSKU:-Available on backorder
LY3177833 is an orally bioavailable inhibitor of Cdc7 kinase (IC50 = 3.3 nM for ADP production in an enzyme assay).{48053} It inhibits phosphorylation of MCM2-S53 in H1299 cells (IC50 = 0.29 µM). LY3177833 reduces tumor growth in an SW620 human colorectal adenocarcinoma mouse xenograft model when administered at doses of 10, 20, and 30 mg/kg twice per day.
Brand:CaymanSKU:25988 - 10 mgAvailable on backorder
LY3177833 is an orally bioavailable inhibitor of Cdc7 kinase (IC50 = 3.3 nM for ADP production in an enzyme assay).{48053} It inhibits phosphorylation of MCM2-S53 in H1299 cells (IC50 = 0.29 µM). LY3177833 reduces tumor growth in an SW620 human colorectal adenocarcinoma mouse xenograft model when administered at doses of 10, 20, and 30 mg/kg twice per day.
Brand:CaymanSKU:25988 - 25 mgAvailable on backorder
LY3177833 is an orally bioavailable inhibitor of Cdc7 kinase (IC50 = 3.3 nM for ADP production in an enzyme assay).{48053} It inhibits phosphorylation of MCM2-S53 in H1299 cells (IC50 = 0.29 µM). LY3177833 reduces tumor growth in an SW620 human colorectal adenocarcinoma mouse xenograft model when administered at doses of 10, 20, and 30 mg/kg twice per day.
Brand:CaymanSKU:25988 - 5 mgAvailable on backorder
LY3177833 is an orally bioavailable inhibitor of Cdc7 kinase (IC50 = 3.3 nM for ADP production in an enzyme assay).{48053} It inhibits phosphorylation of MCM2-S53 in H1299 cells (IC50 = 0.29 µM). LY3177833 reduces tumor growth in an SW620 human colorectal adenocarcinoma mouse xenograft model when administered at doses of 10, 20, and 30 mg/kg twice per day.
Brand:CaymanSKU:25988 - 50 mgAvailable on backorder
LY3200882 is an ATP-competitive inhibitor of TGF-β receptor type 1 (TGF-βRI).{43234} It inhibits TGF-β-induced SMAD phosphorylation in vitro and in vivo and exhibits antitumor activity in the 4T1-LP triple negative breast cancer orthotopic tumor model.
Brand:CaymanSKU:25276 - 1 mgAvailable on backorder
LY3200882 is an ATP-competitive inhibitor of TGF-β receptor type 1 (TGF-βRI).{43234} It inhibits TGF-β-induced SMAD phosphorylation in vitro and in vivo and exhibits antitumor activity in the 4T1-LP triple negative breast cancer orthotopic tumor model.
Brand:CaymanSKU:25276 - 10 mgAvailable on backorder
LY3200882 is an ATP-competitive inhibitor of TGF-β receptor type 1 (TGF-βRI).{43234} It inhibits TGF-β-induced SMAD phosphorylation in vitro and in vivo and exhibits antitumor activity in the 4T1-LP triple negative breast cancer orthotopic tumor model.
Brand:CaymanSKU:25276 - 25 mgAvailable on backorder
LY3200882 is an ATP-competitive inhibitor of TGF-β receptor type 1 (TGF-βRI).{43234} It inhibits TGF-β-induced SMAD phosphorylation in vitro and in vivo and exhibits antitumor activity in the 4T1-LP triple negative breast cancer orthotopic tumor model.
Brand:CaymanSKU:25276 - 5 mgAvailable on backorder
LY320135 is a selective cannabinoid (CB) receptor 1 antagonist (Kis = 224 and >10,000 nM for CB1 and CB2, respectively, in vitro).{36501} It is selective for CB1 over α1- and α2- adrenergic, D1 and D2 dopamine, benzodiazepine, histamine H1, GABA, serotonin (5-HT), and muscarinic receptors. It reverses the inhibition of forskolin-induced cAMP accumulation induced by arachidonoyl ethanolamide (anandamide; Item No. 90050) in CHO cells and inhibits a stimulatory effect of arachidonoyl ethanolamide on adenylate cyclase induced by application of pertussis toxin (IC50 = 734 nM). LY320135 (1 mg/kg) reverses inhibition of light-induced phase shifts in hamsters induced by the CB1 agonist CP 55,940 (Item No. 90084).{36502}
Brand:CaymanSKU:11738 - 1 mgAvailable on backorder
LY320135 is a selective cannabinoid (CB) receptor 1 antagonist (Kis = 224 and >10,000 nM for CB1 and CB2, respectively, in vitro).{36501} It is selective for CB1 over α1- and α2- adrenergic, D1 and D2 dopamine, benzodiazepine, histamine H1, GABA, serotonin (5-HT), and muscarinic receptors. It reverses the inhibition of forskolin-induced cAMP accumulation induced by arachidonoyl ethanolamide (anandamide; Item No. 90050) in CHO cells and inhibits a stimulatory effect of arachidonoyl ethanolamide on adenylate cyclase induced by application of pertussis toxin (IC50 = 734 nM). LY320135 (1 mg/kg) reverses inhibition of light-induced phase shifts in hamsters induced by the CB1 agonist CP 55,940 (Item No. 90084).{36502}
Brand:CaymanSKU:11738 - 10 mgAvailable on backorder
LY320135 is a selective cannabinoid (CB) receptor 1 antagonist (Kis = 224 and >10,000 nM for CB1 and CB2, respectively, in vitro).{36501} It is selective for CB1 over α1- and α2- adrenergic, D1 and D2 dopamine, benzodiazepine, histamine H1, GABA, serotonin (5-HT), and muscarinic receptors. It reverses the inhibition of forskolin-induced cAMP accumulation induced by arachidonoyl ethanolamide (anandamide; Item No. 90050) in CHO cells and inhibits a stimulatory effect of arachidonoyl ethanolamide on adenylate cyclase induced by application of pertussis toxin (IC50 = 734 nM). LY320135 (1 mg/kg) reverses inhibition of light-induced phase shifts in hamsters induced by the CB1 agonist CP 55,940 (Item No. 90084).{36502}
Brand:CaymanSKU:11738 - 5 mgAvailable on backorder
LY3214996 is an inhibitor of ERK1 and ERK2 (IC50 = 5 nM for both).{42884} It inhibits cell proliferation of tumor cells in vitro, including those expressing B-RAF, N-Ras, or K-Ras mutations. LY3214996 inhibits tumor growth in B-RAF or N-Ras mutant melanoma, B-RAF or K-Ras mutant colorectal, lung, and pancreatic cancer mouse xenograft models, as well as patient-derived xenograft (PDX) mouse models.
Brand:CaymanSKU:27936 - 1 mgAvailable on backorder
LY3214996 is an inhibitor of ERK1 and ERK2 (IC50 = 5 nM for both).{42884} It inhibits cell proliferation of tumor cells in vitro, including those expressing B-RAF, N-Ras, or K-Ras mutations. LY3214996 inhibits tumor growth in B-RAF or N-Ras mutant melanoma, B-RAF or K-Ras mutant colorectal, lung, and pancreatic cancer mouse xenograft models, as well as patient-derived xenograft (PDX) mouse models.
Brand:CaymanSKU:27936 - 10 mgAvailable on backorder
LY3214996 is an inhibitor of ERK1 and ERK2 (IC50 = 5 nM for both).{42884} It inhibits cell proliferation of tumor cells in vitro, including those expressing B-RAF, N-Ras, or K-Ras mutations. LY3214996 inhibits tumor growth in B-RAF or N-Ras mutant melanoma, B-RAF or K-Ras mutant colorectal, lung, and pancreatic cancer mouse xenograft models, as well as patient-derived xenograft (PDX) mouse models.
Brand:CaymanSKU:27936 - 25 mgAvailable on backorder
LY3214996 is an inhibitor of ERK1 and ERK2 (IC50 = 5 nM for both).{42884} It inhibits cell proliferation of tumor cells in vitro, including those expressing B-RAF, N-Ras, or K-Ras mutations. LY3214996 inhibits tumor growth in B-RAF or N-Ras mutant melanoma, B-RAF or K-Ras mutant colorectal, lung, and pancreatic cancer mouse xenograft models, as well as patient-derived xenograft (PDX) mouse models.
Brand:CaymanSKU:27936 - 5 mgAvailable on backorder
The protein kinase C (PKC) isoforms PKCβ1 and PKCβ2 have central roles in cell signaling in diabetes, diffuse large B-cell lymphoma, and cardiovascular diseases.{21723,21721,21722,21725} LY333531 is a selective and potent inhibitor of PKCβ1 and PKCβ2 (IC50 = 4.7 and 5.9 nM, respectively).{21724} For comparison, its IC50 values for PKC isoforms α, γ, δ, ε, ζ, and η are 360, 300, 250, 600, >100,000, and 52 nM, respectively.{21724} LY333531 is effective in vivo.{21723,21721}
Brand:CaymanSKU:- The protein kinase C (PKC) isoforms PKCβ1 and PKCβ2 have central roles in cell signaling in diabetes, diffuse large B-cell lymphoma, and cardiovascular diseases.{21723,21721,21722,21725} LY333531 is a selective and potent inhibitor of PKCβ1 and PKCβ2 (IC50 = 4.7 and 5.9 nM, respectively).{21724} For comparison, its IC50 values for PKC isoforms α, γ, δ, ε, ζ, and η are 360, 300, 250, 600, >100,000, and 52 nM, respectively.{21724} LY333531 is effective in vivo.{21723,21721}
Brand:CaymanSKU:-
LY334370 is an agonist of the serotonin (5-HT) receptor subtype 5-HT1F (Kd = 0.446 nM).{52208} It is selective for 5-HT1F over other G protein-coupled 5-HT receptor subtypes with Ki values ranging from 16.4 to greater than 3,000 nM in radioligand binding assays. LY334370 inhibits forskolin-induced cAMP accumulation in mouse L-M(TK-) cell membranes expressing the recombinant human 5-HT1F receptor (EC50 = 1.51 nM).{52209} It decreases electrically stimulated extravasation of plasma proteins in the dura mater in a guinea pig trigeminal nerve model of migraine headache.
Brand:CaymanSKU:29481 - 1 mgAvailable on backorder
LY334370 is an agonist of the serotonin (5-HT) receptor subtype 5-HT1F (Kd = 0.446 nM).{52208} It is selective for 5-HT1F over other G protein-coupled 5-HT receptor subtypes with Ki values ranging from 16.4 to greater than 3,000 nM in radioligand binding assays. LY334370 inhibits forskolin-induced cAMP accumulation in mouse L-M(TK-) cell membranes expressing the recombinant human 5-HT1F receptor (EC50 = 1.51 nM).{52209} It decreases electrically stimulated extravasation of plasma proteins in the dura mater in a guinea pig trigeminal nerve model of migraine headache.
Brand:CaymanSKU:29481 - 10 mgAvailable on backorder
LY334370 is an agonist of the serotonin (5-HT) receptor subtype 5-HT1F (Kd = 0.446 nM).{52208} It is selective for 5-HT1F over other G protein-coupled 5-HT receptor subtypes with Ki values ranging from 16.4 to greater than 3,000 nM in radioligand binding assays. LY334370 inhibits forskolin-induced cAMP accumulation in mouse L-M(TK-) cell membranes expressing the recombinant human 5-HT1F receptor (EC50 = 1.51 nM).{52209} It decreases electrically stimulated extravasation of plasma proteins in the dura mater in a guinea pig trigeminal nerve model of migraine headache.
Brand:CaymanSKU:29481 - 5 mgAvailable on backorder
LY341495 is a potent and selective antagonist of the group II metabotropic glutamate receptors (mGluR), mGluR2 and mGluR3 (IC50s = 21 and 14 nM, respectively, for human isoforms).{24137,24136,24138} It less effectively blocks mGluR8 and mGluR7 (IC50s = 173 and 990 nM, respectively) and weakly antagonizes mGluR1, mGluR5, and mGluR4 (IC50s = 6.8, 8.2, and 22 μM, respectively).{24136} In rat forebrain tissue, LY341495 may bind mGluR3 more avidly than mGluR2.{24135} LY341495 can be effectively used in isolated cells, tissues, and in vivo.{24135,24134,24133} In mice, it penetrates the blood-brain barrier and has been used to study the roles of mGlu2/3 receptors in the brain.{24134,21982,21984}
Brand:CaymanSKU:- LY341495 is a potent and selective antagonist of the group II metabotropic glutamate receptors (mGluR), mGluR2 and mGluR3 (IC50s = 21 and 14 nM, respectively, for human isoforms).{24137,24136,24138} It less effectively blocks mGluR8 and mGluR7 (IC50s = 173 and 990 nM, respectively) and weakly antagonizes mGluR1, mGluR5, and mGluR4 (IC50s = 6.8, 8.2, and 22 μM, respectively).{24136} In rat forebrain tissue, LY341495 may bind mGluR3 more avidly than mGluR2.{24135} LY341495 can be effectively used in isolated cells, tissues, and in vivo.{24135,24134,24133} In mice, it penetrates the blood-brain barrier and has been used to study the roles of mGlu2/3 receptors in the brain.{24134,21982,21984}
Brand:CaymanSKU:- LY341495 is a potent and selective antagonist of the group II metabotropic glutamate receptors (mGluR), mGluR2 and mGluR3 (IC50s = 21 and 14 nM, respectively, for human isoforms).{24137,24136,24138} It less effectively blocks mGluR8 and mGluR7 (IC50s = 173 and 990 nM, respectively) and weakly antagonizes mGluR1, mGluR5, and mGluR4 (IC50s = 6.8, 8.2, and 22 μM, respectively).{24136} In rat forebrain tissue, LY341495 may bind mGluR3 more avidly than mGluR2.{24135} LY341495 can be effectively used in isolated cells, tissues, and in vivo.{24135,24134,24133} In mice, it penetrates the blood-brain barrier and has been used to study the roles of mGlu2/3 receptors in the brain.{24134,21982,21984}
Brand:CaymanSKU:-
LY344864 is an agonist of the serotonin (5-HT) receptor subtype 5-HT1F (Ki = 6 nM).{53306} It is selective for 5-HT1F over 5-HT1A-E , 5-HT2A-C, and 5-HT7 receptors (Kis = 0.53-4.85 µM), as well as dopamine D1 and D2, GABAA, histamine H1, muscarinic, and α1-, α2-, and β-adrenergic receptors with Ki values ranging from 3.69 to greater than 100 µM. LY344864 inhibits forskolin-induced cAMP accumulation in L-M(TK-) cells expressing recombinant human 5-HT1F receptors with an EC50 value of 3 nM. It decreases electrically stimulated extravasation of plasma proteins in the dura mater in a rat trigeminal nerve model of migraine headache (ID50s = 0.6 and 2.1 ng/kg for i.v. and oral administration, respectively).
Brand:CaymanSKU:29496 - 10 mgAvailable on backorder
LY344864 is an agonist of the serotonin (5-HT) receptor subtype 5-HT1F (Ki = 6 nM).{53306} It is selective for 5-HT1F over 5-HT1A-E , 5-HT2A-C, and 5-HT7 receptors (Kis = 0.53-4.85 µM), as well as dopamine D1 and D2, GABAA, histamine H1, muscarinic, and α1-, α2-, and β-adrenergic receptors with Ki values ranging from 3.69 to greater than 100 µM. LY344864 inhibits forskolin-induced cAMP accumulation in L-M(TK-) cells expressing recombinant human 5-HT1F receptors with an EC50 value of 3 nM. It decreases electrically stimulated extravasation of plasma proteins in the dura mater in a rat trigeminal nerve model of migraine headache (ID50s = 0.6 and 2.1 ng/kg for i.v. and oral administration, respectively).
Brand:CaymanSKU:29496 - 25 mgAvailable on backorder
LY344864 is an agonist of the serotonin (5-HT) receptor subtype 5-HT1F (Ki = 6 nM).{53306} It is selective for 5-HT1F over 5-HT1A-E , 5-HT2A-C, and 5-HT7 receptors (Kis = 0.53-4.85 µM), as well as dopamine D1 and D2, GABAA, histamine H1, muscarinic, and α1-, α2-, and β-adrenergic receptors with Ki values ranging from 3.69 to greater than 100 µM. LY344864 inhibits forskolin-induced cAMP accumulation in L-M(TK-) cells expressing recombinant human 5-HT1F receptors with an EC50 value of 3 nM. It decreases electrically stimulated extravasation of plasma proteins in the dura mater in a rat trigeminal nerve model of migraine headache (ID50s = 0.6 and 2.1 ng/kg for i.v. and oral administration, respectively).
Brand:CaymanSKU:29496 - 5 mgAvailable on backorder
LY344864 is an agonist of the serotonin (5-HT) receptor subtype 5-HT1F (Ki = 6 nM).{53306} It is selective for 5-HT1F over 5-HT1A-E , 5-HT2A-C, and 5-HT7 receptors (Kis = 0.53-4.85 µM), as well as dopamine D1 and D2, GABAA, histamine H1, muscarinic, and α1-, α2-, and β-adrenergic receptors with Ki values ranging from 3.69 to greater than 100 µM. LY344864 inhibits forskolin-induced cAMP accumulation in L-M(TK-) cells expressing recombinant human 5-HT1F receptors with an EC50 value of 3 nM. It decreases electrically stimulated extravasation of plasma proteins in the dura mater in a rat trigeminal nerve model of migraine headache (ID50s = 0.6 and 2.1 ng/kg for i.v. and oral administration, respectively).
Brand:CaymanSKU:29496 - 50 mgAvailable on backorder
LY354740 is an agonist of the group II metabotropic glutamate receptor (mGluR) subtypes mGluR2 and mGluR3 (Kis = 99 and 94 nM, respectively).{32438} It inhibits forskolin-stimulated cAMP accumulation in cells expressing human mGluR2 and mGluR3 (EC50s = 5.1 and 24.3 nM, respectively) and is selective for mGluR2 and mGluR3 over mGluR4, mGluR7, mGluR1a, and mGluR5a (EC50s = >100 µM).{38897,34626} LY354740 suppresses electrically stimulated excitatory postsynaptic potentials (EPSPs) in rat striatal neurons (EC50 = 20 nM) and excitatory postsynaptic currents (EPSCs) induced by serotonin (Item No. 14332) in rat medial prefrontal cortex in vitro (EC50 = 89.1 nM).{32438,38898} LY354740 (5 mM) iontophoretically ejected into the ventrobasal thalamus of rats reduces sensory inhibition by 20% compared to control in an alternating test, condition-test paradigm.{31730} It attenuates the effects of PCP on working memory, stereotypy, locomotion, and cortical glutamate efflux in a rat model of schizophrenia when administered at a dose of 10 mg/kg.{38899} LY354740 also shows efficacy in animal models of anxiety, epilepsy, and withdrawal from nicotine and morphine.{32438,21635}
Brand:CaymanSKU:24215 - 1 mgAvailable on backorder
LY354740 is an agonist of the group II metabotropic glutamate receptor (mGluR) subtypes mGluR2 and mGluR3 (Kis = 99 and 94 nM, respectively).{32438} It inhibits forskolin-stimulated cAMP accumulation in cells expressing human mGluR2 and mGluR3 (EC50s = 5.1 and 24.3 nM, respectively) and is selective for mGluR2 and mGluR3 over mGluR4, mGluR7, mGluR1a, and mGluR5a (EC50s = >100 µM).{38897,34626} LY354740 suppresses electrically stimulated excitatory postsynaptic potentials (EPSPs) in rat striatal neurons (EC50 = 20 nM) and excitatory postsynaptic currents (EPSCs) induced by serotonin (Item No. 14332) in rat medial prefrontal cortex in vitro (EC50 = 89.1 nM).{32438,38898} LY354740 (5 mM) iontophoretically ejected into the ventrobasal thalamus of rats reduces sensory inhibition by 20% compared to control in an alternating test, condition-test paradigm.{31730} It attenuates the effects of PCP on working memory, stereotypy, locomotion, and cortical glutamate efflux in a rat model of schizophrenia when administered at a dose of 10 mg/kg.{38899} LY354740 also shows efficacy in animal models of anxiety, epilepsy, and withdrawal from nicotine and morphine.{32438,21635}
Brand:CaymanSKU:24215 - 10 mgAvailable on backorder
LY354740 is an agonist of the group II metabotropic glutamate receptor (mGluR) subtypes mGluR2 and mGluR3 (Kis = 99 and 94 nM, respectively).{32438} It inhibits forskolin-stimulated cAMP accumulation in cells expressing human mGluR2 and mGluR3 (EC50s = 5.1 and 24.3 nM, respectively) and is selective for mGluR2 and mGluR3 over mGluR4, mGluR7, mGluR1a, and mGluR5a (EC50s = >100 µM).{38897,34626} LY354740 suppresses electrically stimulated excitatory postsynaptic potentials (EPSPs) in rat striatal neurons (EC50 = 20 nM) and excitatory postsynaptic currents (EPSCs) induced by serotonin (Item No. 14332) in rat medial prefrontal cortex in vitro (EC50 = 89.1 nM).{32438,38898} LY354740 (5 mM) iontophoretically ejected into the ventrobasal thalamus of rats reduces sensory inhibition by 20% compared to control in an alternating test, condition-test paradigm.{31730} It attenuates the effects of PCP on working memory, stereotypy, locomotion, and cortical glutamate efflux in a rat model of schizophrenia when administered at a dose of 10 mg/kg.{38899} LY354740 also shows efficacy in animal models of anxiety, epilepsy, and withdrawal from nicotine and morphine.{32438,21635}
Brand:CaymanSKU:24215 - 5 mgAvailable on backorder
Transforming growth factor-β (TGF-β) signals through a cell surface heteromeric complex involving type I (TGF-β RI) and type II (TGF-β RII) receptors. Downstream signal transduction is mediated by the TGF-β RI kinase domain through the phosphorylation of Smad proteins. LY364947 is a selective inhibitor of TGF-β RI (TGFR-I, TβR-I, ALK-5), with an IC50 value of 59 nM.{17263} LY364947 less effectively inhibits TGF-β RII (IC50 = 400 nM), p38 MAPK (IC50 = 740 nM), and mixed-lineage kinase 7 (MLK7; IC50 = 1,400 nM).{17263,17264} It inhibits TGF-β-induced cell growth (IC50 = 89 nM) in NIH 3T3 mouse fibroblasts{17263} and TGF-β-directed Smad phosphorylation, synthesis of fibronectin, PAI-1 and uPA protein, and matrigel invasion in MDA-MB-231 cells.{17265}
Brand:CaymanSKU:- Transforming growth factor-β (TGF-β) signals through a cell surface heteromeric complex involving type I (TGF-β RI) and type II (TGF-β RII) receptors. Downstream signal transduction is mediated by the TGF-β RI kinase domain through the phosphorylation of Smad proteins. LY364947 is a selective inhibitor of TGF-β RI (TGFR-I, TβR-I, ALK-5), with an IC50 value of 59 nM.{17263} LY364947 less effectively inhibits TGF-β RII (IC50 = 400 nM), p38 MAPK (IC50 = 740 nM), and mixed-lineage kinase 7 (MLK7; IC50 = 1,400 nM).{17263,17264} It inhibits TGF-β-induced cell growth (IC50 = 89 nM) in NIH 3T3 mouse fibroblasts{17263} and TGF-β-directed Smad phosphorylation, synthesis of fibronectin, PAI-1 and uPA protein, and matrigel invasion in MDA-MB-231 cells.{17265}
Brand:CaymanSKU:- Transforming growth factor-β (TGF-β) signals through a cell surface heteromeric complex involving type I (TGF-β RI) and type II (TGF-β RII) receptors. Downstream signal transduction is mediated by the TGF-β RI kinase domain through the phosphorylation of Smad proteins. LY364947 is a selective inhibitor of TGF-β RI (TGFR-I, TβR-I, ALK-5), with an IC50 value of 59 nM.{17263} LY364947 less effectively inhibits TGF-β RII (IC50 = 400 nM), p38 MAPK (IC50 = 740 nM), and mixed-lineage kinase 7 (MLK7; IC50 = 1,400 nM).{17263,17264} It inhibits TGF-β-induced cell growth (IC50 = 89 nM) in NIH 3T3 mouse fibroblasts{17263} and TGF-β-directed Smad phosphorylation, synthesis of fibronectin, PAI-1 and uPA protein, and matrigel invasion in MDA-MB-231 cells.{17265}
Brand:CaymanSKU:- Transforming growth factor-β (TGF-β) signals through a cell surface heteromeric complex involving type I (TGF-β RI) and type II (TGF-β RII) receptors. Downstream signal transduction is mediated by the TGF-β RI kinase domain through the phosphorylation of Smad proteins. LY364947 is a selective inhibitor of TGF-β RI (TGFR-I, TβR-I, ALK-5), with an IC50 value of 59 nM.{17263} LY364947 less effectively inhibits TGF-β RII (IC50 = 400 nM), p38 MAPK (IC50 = 740 nM), and mixed-lineage kinase 7 (MLK7; IC50 = 1,400 nM).{17263,17264} It inhibits TGF-β-induced cell growth (IC50 = 89 nM) in NIH 3T3 mouse fibroblasts{17263} and TGF-β-directed Smad phosphorylation, synthesis of fibronectin, PAI-1 and uPA protein, and matrigel invasion in MDA-MB-231 cells.{17265}
Brand:CaymanSKU:-
LY379268 is a potent, brain-permeable, and selective agonist of group II metabotropic glutamate receptors (mGluRs), subtypes mGluR2 and mGluR3.{34626} In an assay of second messenger response, LY379268 exhibits EC50 values of 2.69 and 4.48 nM for human mGluR2 and mGluR3, respectively, with at least 80-fold selectivity over group I and III mGluRs.{34626} In a displacement assay, LY379268 displays no agonist or antagonist activity against NMDA, AMPA, or kainate receptors up to a concentration of 100 µM.{34626} However, it may influence the level of AMPA receptor trafficking in rat prefrontal cortical neurons.{34629} LY379268 confers a neuroprotective effect to the CA1 of the hippocampus in a gerbil model of induced ischemia at a dose of 10 mg/kg.{34627} In rats, LY379268 (3 mg/kg) raises the extracellular dopamine level to 168% of the basal level in the prefrontal cortex.{34628}
Brand:CaymanSKU:- LY379268 is a potent, brain-permeable, and selective agonist of group II metabotropic glutamate receptors (mGluRs), subtypes mGluR2 and mGluR3.{34626} In an assay of second messenger response, LY379268 exhibits EC50 values of 2.69 and 4.48 nM for human mGluR2 and mGluR3, respectively, with at least 80-fold selectivity over group I and III mGluRs.{34626} In a displacement assay, LY379268 displays no agonist or antagonist activity against NMDA, AMPA, or kainate receptors up to a concentration of 100 µM.{34626} However, it may influence the level of AMPA receptor trafficking in rat prefrontal cortical neurons.{34629} LY379268 confers a neuroprotective effect to the CA1 of the hippocampus in a gerbil model of induced ischemia at a dose of 10 mg/kg.{34627} In rats, LY379268 (3 mg/kg) raises the extracellular dopamine level to 168% of the basal level in the prefrontal cortex.{34628}
Brand:CaymanSKU:- LY379268 is a potent, brain-permeable, and selective agonist of group II metabotropic glutamate receptors (mGluRs), subtypes mGluR2 and mGluR3.{34626} In an assay of second messenger response, LY379268 exhibits EC50 values of 2.69 and 4.48 nM for human mGluR2 and mGluR3, respectively, with at least 80-fold selectivity over group I and III mGluRs.{34626} In a displacement assay, LY379268 displays no agonist or antagonist activity against NMDA, AMPA, or kainate receptors up to a concentration of 100 µM.{34626} However, it may influence the level of AMPA receptor trafficking in rat prefrontal cortical neurons.{34629} LY379268 confers a neuroprotective effect to the CA1 of the hippocampus in a gerbil model of induced ischemia at a dose of 10 mg/kg.{34627} In rats, LY379268 (3 mg/kg) raises the extracellular dopamine level to 168% of the basal level in the prefrontal cortex.{34628}
Brand:CaymanSKU:-
LY393558 is an inhibitor of serotonin (5-HT) reuptake (IC50 = 3.3 nM in rat cortical synaptosomes).{57349} It is selective for serotonin reuptake over norepinephrine reuptake in rat cortical synaptosomes (IC50 = 2,510 nM) but does inhibit 5-HT-induced [35S]GTPγS binding in cells expressing human 5-HT1B or 5-HT1D receptors (Kbs = 0.89 and 10.4 nM, respectively). LY393558 (30 mg/kg per day) reduces pulmonary vascular remodeling, increases in right ventricular systolic pressure, and the development of right ventricular hypertrophy in a mouse model of pulmonary arterial hypertension induced by overexpression of the serotonin transporter and hypoxia.{57350}
Brand:CaymanSKU:32775 - 1 mgAvailable on backorder
LY393558 is an inhibitor of serotonin (5-HT) reuptake (IC50 = 3.3 nM in rat cortical synaptosomes).{57349} It is selective for serotonin reuptake over norepinephrine reuptake in rat cortical synaptosomes (IC50 = 2,510 nM) but does inhibit 5-HT-induced [35S]GTPγS binding in cells expressing human 5-HT1B or 5-HT1D receptors (Kbs = 0.89 and 10.4 nM, respectively). LY393558 (30 mg/kg per day) reduces pulmonary vascular remodeling, increases in right ventricular systolic pressure, and the development of right ventricular hypertrophy in a mouse model of pulmonary arterial hypertension induced by overexpression of the serotonin transporter and hypoxia.{57350}
Brand:CaymanSKU:32775 - 10 mgAvailable on backorder
LY393558 is an inhibitor of serotonin (5-HT) reuptake (IC50 = 3.3 nM in rat cortical synaptosomes).{57349} It is selective for serotonin reuptake over norepinephrine reuptake in rat cortical synaptosomes (IC50 = 2,510 nM) but does inhibit 5-HT-induced [35S]GTPγS binding in cells expressing human 5-HT1B or 5-HT1D receptors (Kbs = 0.89 and 10.4 nM, respectively). LY393558 (30 mg/kg per day) reduces pulmonary vascular remodeling, increases in right ventricular systolic pressure, and the development of right ventricular hypertrophy in a mouse model of pulmonary arterial hypertension induced by overexpression of the serotonin transporter and hypoxia.{57350}
Brand:CaymanSKU:32775 - 5 mgAvailable on backorder
LY404039 is a potent agonist of metabotropic glutamate (mGlu) group II receptors mGluR2 and mGluR3 (Kis = 149 and 62 nM, respectively, for recombinant human isoforms).{32438} It displays 100-fold selectivity for mGluR2/3 over ionotropic glutamate receptors, glutamate transporters, and several other receptors targeted by known anxiolytic and antipsychotic medications.{32438} LY404039 inhibits the binding of domperidone (Item No. 18875) by 15.5% to dopamine D2 receptors (Kd = ~10 nM in vitro), indicating interaction with this receptor.{32439} LY404039 is orally bioavailable and demonstrates antipsychotic and anxiolytic efficacy in several animal models.{32437}
Brand:CaymanSKU:-Available on backorder
LY404039 is a potent agonist of metabotropic glutamate (mGlu) group II receptors mGluR2 and mGluR3 (Kis = 149 and 62 nM, respectively, for recombinant human isoforms).{32438} It displays 100-fold selectivity for mGluR2/3 over ionotropic glutamate receptors, glutamate transporters, and several other receptors targeted by known anxiolytic and antipsychotic medications.{32438} LY404039 inhibits the binding of domperidone (Item No. 18875) by 15.5% to dopamine D2 receptors (Kd = ~10 nM in vitro), indicating interaction with this receptor.{32439} LY404039 is orally bioavailable and demonstrates antipsychotic and anxiolytic efficacy in several animal models.{32437}
Brand:CaymanSKU:-Available on backorder
LY404039 is a potent agonist of metabotropic glutamate (mGlu) group II receptors mGluR2 and mGluR3 (Kis = 149 and 62 nM, respectively, for recombinant human isoforms).{32438} It displays 100-fold selectivity for mGluR2/3 over ionotropic glutamate receptors, glutamate transporters, and several other receptors targeted by known anxiolytic and antipsychotic medications.{32438} LY404039 inhibits the binding of domperidone (Item No. 18875) by 15.5% to dopamine D2 receptors (Kd = ~10 nM in vitro), indicating interaction with this receptor.{32439} LY404039 is orally bioavailable and demonstrates antipsychotic and anxiolytic efficacy in several animal models.{32437}
Brand:CaymanSKU:-Available on backorder
LY404039 is a potent agonist of metabotropic glutamate (mGlu) group II receptors mGluR2 and mGluR3 (Kis = 149 and 62 nM, respectively, for recombinant human isoforms).{32438} It displays 100-fold selectivity for mGluR2/3 over ionotropic glutamate receptors, glutamate transporters, and several other receptors targeted by known anxiolytic and antipsychotic medications.{32438} LY404039 inhibits the binding of domperidone (Item No. 18875) by 15.5% to dopamine D2 receptors (Kd = ~10 nM in vitro), indicating interaction with this receptor.{32439} LY404039 is orally bioavailable and demonstrates antipsychotic and anxiolytic efficacy in several animal models.{32437}
Brand:CaymanSKU:-Available on backorder
LY404187 is a benzothiadiazide positive allosteric modulator of AMPA receptors.{46485} It increases glutamate-induced activation of GluR1i, -2i, -2o, -3i, and -4i subunit-containing AMPA receptors with EC50 values of 5.65, 0.15, 1.44, 1.66, and 0.21 µM, respectively, in a calcium influx assay. LY404187 is selective for these AMPA receptors over GluR6 subunit-containing kainate receptors at 10 µM. LY404187 increases currents induced by glutamate and AMPA in rat prefrontal cortex pyramidal neurons (EC50s = 1.3 and 1.2 µM, respectively) but not in AMPA-stimulated primary rat embryonic hippocampal or primary cerebellar Purkinje neurons.{46486,46487} LY404187 prevents decreases in the number of dopaminergic neurons in the substantia nigra induced by MPTP and 6-OHDA (Item No. 25330) in mouse and rat, respectively, models of Parkinson’s disease when administered at a dose of 0.5 mg/kg per day.{46488}
Brand:CaymanSKU:28741 - 10 mgAvailable on backorder
LY404187 is a benzothiadiazide positive allosteric modulator of AMPA receptors.{46485} It increases glutamate-induced activation of GluR1i, -2i, -2o, -3i, and -4i subunit-containing AMPA receptors with EC50 values of 5.65, 0.15, 1.44, 1.66, and 0.21 µM, respectively, in a calcium influx assay. LY404187 is selective for these AMPA receptors over GluR6 subunit-containing kainate receptors at 10 µM. LY404187 increases currents induced by glutamate and AMPA in rat prefrontal cortex pyramidal neurons (EC50s = 1.3 and 1.2 µM, respectively) but not in AMPA-stimulated primary rat embryonic hippocampal or primary cerebellar Purkinje neurons.{46486,46487} LY404187 prevents decreases in the number of dopaminergic neurons in the substantia nigra induced by MPTP and 6-OHDA (Item No. 25330) in mouse and rat, respectively, models of Parkinson’s disease when administered at a dose of 0.5 mg/kg per day.{46488}
Brand:CaymanSKU:28741 - 25 mgAvailable on backorder
LY404187 is a benzothiadiazide positive allosteric modulator of AMPA receptors.{46485} It increases glutamate-induced activation of GluR1i, -2i, -2o, -3i, and -4i subunit-containing AMPA receptors with EC50 values of 5.65, 0.15, 1.44, 1.66, and 0.21 µM, respectively, in a calcium influx assay. LY404187 is selective for these AMPA receptors over GluR6 subunit-containing kainate receptors at 10 µM. LY404187 increases currents induced by glutamate and AMPA in rat prefrontal cortex pyramidal neurons (EC50s = 1.3 and 1.2 µM, respectively) but not in AMPA-stimulated primary rat embryonic hippocampal or primary cerebellar Purkinje neurons.{46486,46487} LY404187 prevents decreases in the number of dopaminergic neurons in the substantia nigra induced by MPTP and 6-OHDA (Item No. 25330) in mouse and rat, respectively, models of Parkinson’s disease when administered at a dose of 0.5 mg/kg per day.{46488}
Brand:CaymanSKU:28741 - 5 mgAvailable on backorder
LY404187 is a benzothiadiazide positive allosteric modulator of AMPA receptors.{46485} It increases glutamate-induced activation of GluR1i, -2i, -2o, -3i, and -4i subunit-containing AMPA receptors with EC50 values of 5.65, 0.15, 1.44, 1.66, and 0.21 µM, respectively, in a calcium influx assay. LY404187 is selective for these AMPA receptors over GluR6 subunit-containing kainate receptors at 10 µM. LY404187 increases currents induced by glutamate and AMPA in rat prefrontal cortex pyramidal neurons (EC50s = 1.3 and 1.2 µM, respectively) but not in AMPA-stimulated primary rat embryonic hippocampal or primary cerebellar Purkinje neurons.{46486,46487} LY404187 prevents decreases in the number of dopaminergic neurons in the substantia nigra induced by MPTP and 6-OHDA (Item No. 25330) in mouse and rat, respectively, models of Parkinson’s disease when administered at a dose of 0.5 mg/kg per day.{46488}
Brand:CaymanSKU:28741 - 50 mgAvailable on backorder
γ-Secretase is a multi-subunit aspartyl protease that regulates signaling pathways by proteolytically cleaving substrates, abrogating or releasing signaling molecules. One well-known substrate of this enzyme is Notch, a transmembrane receptor that plays a key role in cell fate decisions including cell proliferation, differentiation, and apoptosis. LY411575 is a cell-permeable γ-secretase inhibitor (IC50 = 0.14 nM) that has been shown to block Notch activation in vitro at 500 µM.{26489,26490} LY411575 can induce apoptosis in Kaposi’s sarcoma cells as well as promote intestinal goblet cell differentiation in a mouse model of colitis.{26490,26491} It has also been observed to promote neural differentiation of mouse embryonic stem cells.{26492}
Brand:CaymanSKU:- γ-Secretase is a multi-subunit aspartyl protease that regulates signaling pathways by proteolytically cleaving substrates, abrogating or releasing signaling molecules. One well-known substrate of this enzyme is Notch, a transmembrane receptor that plays a key role in cell fate decisions including cell proliferation, differentiation, and apoptosis. LY411575 is a cell-permeable γ-secretase inhibitor (IC50 = 0.14 nM) that has been shown to block Notch activation in vitro at 500 µM.{26489,26490} LY411575 can induce apoptosis in Kaposi’s sarcoma cells as well as promote intestinal goblet cell differentiation in a mouse model of colitis.{26490,26491} It has also been observed to promote neural differentiation of mouse embryonic stem cells.{26492}
Brand:CaymanSKU:- γ-Secretase is a multi-subunit aspartyl protease that regulates signaling pathways by proteolytically cleaving substrates, abrogating or releasing signaling molecules. One well-known substrate of this enzyme is Notch, a transmembrane receptor that plays a key role in cell fate decisions including cell proliferation, differentiation, and apoptosis. LY411575 is a cell-permeable γ-secretase inhibitor (IC50 = 0.14 nM) that has been shown to block Notch activation in vitro at 500 µM.{26489,26490} LY411575 can induce apoptosis in Kaposi’s sarcoma cells as well as promote intestinal goblet cell differentiation in a mouse model of colitis.{26490,26491} It has also been observed to promote neural differentiation of mouse embryonic stem cells.{26492}
Brand:CaymanSKU:- γ-Secretase is a multi-subunit aspartyl protease that regulates signaling pathways by proteolytically cleaving substrates, abrogating or releasing signaling molecules. One well-known substrate of this enzyme is Notch, a transmembrane receptor that plays a key role in cell fate decisions including cell proliferation, differentiation, and apoptosis. LY411575 is a cell-permeable γ-secretase inhibitor (IC50 = 0.14 nM) that has been shown to block Notch activation in vitro at 500 µM.{26489,26490} LY411575 can induce apoptosis in Kaposi’s sarcoma cells as well as promote intestinal goblet cell differentiation in a mouse model of colitis.{26490,26491} It has also been observed to promote neural differentiation of mouse embryonic stem cells.{26492}
Brand:CaymanSKU:-
LY83583 is an inhibitor of soluble guanylate cyclase and of cGMP production. It inhibits soluble guanylate cyclase in human platelets with an IC50 value of 2 µM.{4156} LY83583 also inhibits leukotriene synthesis in guinea pig lung and rat peritoneal cells with an IC50 value of 1.8 µM and is a noncompetitive inhibitor of glutathione reductase in bovine intestinal mucosa with a Ki value of 3 µM.{4155,4372}
Brand:CaymanSKU:70230 - 1 mgAvailable on backorder
LY83583 is an inhibitor of soluble guanylate cyclase and of cGMP production. It inhibits soluble guanylate cyclase in human platelets with an IC50 value of 2 µM.{4156} LY83583 also inhibits leukotriene synthesis in guinea pig lung and rat peritoneal cells with an IC50 value of 1.8 µM and is a noncompetitive inhibitor of glutathione reductase in bovine intestinal mucosa with a Ki value of 3 µM.{4155,4372}
Brand:CaymanSKU:70230 - 10 mgAvailable on backorder
LY83583 is an inhibitor of soluble guanylate cyclase and of cGMP production. It inhibits soluble guanylate cyclase in human platelets with an IC50 value of 2 µM.{4156} LY83583 also inhibits leukotriene synthesis in guinea pig lung and rat peritoneal cells with an IC50 value of 1.8 µM and is a noncompetitive inhibitor of glutathione reductase in bovine intestinal mucosa with a Ki value of 3 µM.{4155,4372}
Brand:CaymanSKU:70230 - 5 mgAvailable on backorder
LY83583 is an inhibitor of soluble guanylate cyclase and of cGMP production. It inhibits soluble guanylate cyclase in human platelets with an IC50 value of 2 µM.{4156} LY83583 also inhibits leukotriene synthesis in guinea pig lung and rat peritoneal cells with an IC50 value of 1.8 µM and is a noncompetitive inhibitor of glutathione reductase in bovine intestinal mucosa with a Ki value of 3 µM.{4155,4372}
Brand:CaymanSKU:70230 - 50 mgAvailable on backorder
Lycopene is a red-colored carotenoid found in tomatoes and other red fruits and vegetables.{24655} Carotenoids, including lycopene, are powerful antioxidants that efficiently quench singlet oxygen.{24657,24655} Presumably through this action, carotenoids may protect against cancers, cardiovascular stress, and other diseases.{24654,24653,24656,24652}
Brand:CaymanSKU:70945 - 1 mgAvailable on backorder
Lycopene is a red-colored carotenoid found in tomatoes and other red fruits and vegetables.{24655} Carotenoids, including lycopene, are powerful antioxidants that efficiently quench singlet oxygen.{24657,24655} Presumably through this action, carotenoids may protect against cancers, cardiovascular stress, and other diseases.{24654,24653,24656,24652}
Brand:CaymanSKU:70945 - 10 mgAvailable on backorder
Lycopene is a red-colored carotenoid found in tomatoes and other red fruits and vegetables.{24655} Carotenoids, including lycopene, are powerful antioxidants that efficiently quench singlet oxygen.{24657,24655} Presumably through this action, carotenoids may protect against cancers, cardiovascular stress, and other diseases.{24654,24653,24656,24652}
Brand:CaymanSKU:70945 - 5 mgAvailable on backorder
Lycorine is an alkaloid that has been found in Amaryllidaceae and has diverse biological activities.{57080,57081,57082,57083} It is active against P. falciparum (IC50 = 1.026 µg/ml).{57080} Lycorine inhibits severe acute respiratory syndrome coronavirus (SARS-CoV) viral infection in Vero cells (EC50 = 15.7 µM).{57081} It inhibits migration of A549 non-small cell lung cancer (NSCLC) and U373 MG glioblastoma cells when used at a concentration of 5 µM.{57082} Lycorine (0.4 mg/kg) increases survival and reduces virus-induced paralysis in a mouse model of enterovirus 71 infection.{57083}
Brand:CaymanSKU:30650 - 10 mgAvailable on backorder
Lycorine is an alkaloid that has been found in Amaryllidaceae and has diverse biological activities.{57080,57081,57082,57083} It is active against P. falciparum (IC50 = 1.026 µg/ml).{57080} Lycorine inhibits severe acute respiratory syndrome coronavirus (SARS-CoV) viral infection in Vero cells (EC50 = 15.7 µM).{57081} It inhibits migration of A549 non-small cell lung cancer (NSCLC) and U373 MG glioblastoma cells when used at a concentration of 5 µM.{57082} Lycorine (0.4 mg/kg) increases survival and reduces virus-induced paralysis in a mouse model of enterovirus 71 infection.{57083}
Brand:CaymanSKU:30650 - 25 mgAvailable on backorder
Lycorine is an alkaloid that has been found in Amaryllidaceae and has diverse biological activities.{57080,57081,57082,57083} It is active against P. falciparum (IC50 = 1.026 µg/ml).{57080} Lycorine inhibits severe acute respiratory syndrome coronavirus (SARS-CoV) viral infection in Vero cells (EC50 = 15.7 µM).{57081} It inhibits migration of A549 non-small cell lung cancer (NSCLC) and U373 MG glioblastoma cells when used at a concentration of 5 µM.{57082} Lycorine (0.4 mg/kg) increases survival and reduces virus-induced paralysis in a mouse model of enterovirus 71 infection.{57083}
Brand:CaymanSKU:30650 - 5 mgAvailable on backorder
Lycorine is an alkaloid that has been found in Amaryllidaceae and has diverse biological activities.{57080,57081,57082,57083} It is active against P. falciparum (IC50 = 1.026 µg/ml).{57080} Lycorine inhibits severe acute respiratory syndrome coronavirus (SARS-CoV) viral infection in Vero cells (EC50 = 15.7 µM).{57081} It inhibits migration of A549 non-small cell lung cancer (NSCLC) and U373 MG glioblastoma cells when used at a concentration of 5 µM.{57082} Lycorine (0.4 mg/kg) increases survival and reduces virus-induced paralysis in a mouse model of enterovirus 71 infection.{57083}
Brand:CaymanSKU:30650 - 50 mgAvailable on backorder
Lydicamycin is an antibiotic first isolated from Streptomyces. It is particularly cytotoxic against S. aureus, including the methicillin resistant 535 strain (MICs = 3.1-6.2 µg/ml).{32121} Lydicamycin also inhibits the growth of C. neoformans (MIC = 25 µg/ml) but is ineffective against Gram-negative bacteria.{32121}
Brand:CaymanSKU:20584 -Available on backorder
Lydicamycin is an antibiotic first isolated from Streptomyces. It is particularly cytotoxic against S. aureus, including the methicillin resistant 535 strain (MICs = 3.1-6.2 µg/ml).{32121} Lydicamycin also inhibits the growth of C. neoformans (MIC = 25 µg/ml) but is ineffective against Gram-negative bacteria.{32121}
Brand:CaymanSKU:20584 -Available on backorder
LYG-202 is a synthetic flavonoid with anticancer and anti-angiogenic activities.{39094, 39095} It inhibits proliferation of HepG2, MCF-7, HeLa, BGC-823, MDA-MB-435, and HCT116 cancer cells in vitro (IC50s = 4.74-27.70 μM) via induction of apoptosis and dissipation of the mitochondrial membrane potential.{39094} LYG-202 reduces tumor growth in S180 sarcoma cell-inoculated mice. It also inhibits VEGF-stimulated human umbilical vein endothelial cells (HUVEC) cell migration and tube formation in vitro and decreases capillary sprouting in isolated rat aortic rings and the chicken chorioallantoic membrane (CAM) model of angiogenesis.{39095}
Brand:CaymanSKU:21976 -Out of stock