Cayman
Showing 39601–39750 of 45550 results
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Skepinone-L is an ATP-competitive inhibitor of p38 MAPK isoform p38α (IC50s = 5 nM) and p38β (97% inhibition at 1 µM).{26162,26163} It has little effect on a range of other kinases, including p38γ and p38δ. Skepinone-L dose-dependently blocks the phosphorylation of heat shock protein 27 (HSP27), a p38 MAPK substrate, in response to stimulation with anisomycin (Item No. 11308) in HeLa cells (IC50 = 25 nM) or TNF-α in THP-1 cells.{26162,26163} At 1 µM, it prevents phosphorylation of cytosolic phospholipase A2 in platelets in response to collagen-related peptide or thrombin (Item No. 13188), blunting platelet secretion and aggregation.{26164}
Brand:CaymanSKU:-Out of stock
Skepinone-L is an ATP-competitive inhibitor of p38 MAPK isoform p38α (IC50s = 5 nM) and p38β (97% inhibition at 1 µM).{26162,26163} It has little effect on a range of other kinases, including p38γ and p38δ. Skepinone-L dose-dependently blocks the phosphorylation of heat shock protein 27 (HSP27), a p38 MAPK substrate, in response to stimulation with anisomycin (Item No. 11308) in HeLa cells (IC50 = 25 nM) or TNF-α in THP-1 cells.{26162,26163} At 1 µM, it prevents phosphorylation of cytosolic phospholipase A2 in platelets in response to collagen-related peptide or thrombin (Item No. 13188), blunting platelet secretion and aggregation.{26164}
Brand:CaymanSKU:-Out of stock
Skepinone-L is an ATP-competitive inhibitor of p38 MAPK isoform p38α (IC50s = 5 nM) and p38β (97% inhibition at 1 µM).{26162,26163} It has little effect on a range of other kinases, including p38γ and p38δ. Skepinone-L dose-dependently blocks the phosphorylation of heat shock protein 27 (HSP27), a p38 MAPK substrate, in response to stimulation with anisomycin (Item No. 11308) in HeLa cells (IC50 = 25 nM) or TNF-α in THP-1 cells.{26162,26163} At 1 µM, it prevents phosphorylation of cytosolic phospholipase A2 in platelets in response to collagen-related peptide or thrombin (Item No. 13188), blunting platelet secretion and aggregation.{26164}
Brand:CaymanSKU:-Out of stock
Skepinone-L is an ATP-competitive inhibitor of p38 MAPK isoform p38α (IC50s = 5 nM) and p38β (97% inhibition at 1 µM).{26162,26163} It has little effect on a range of other kinases, including p38γ and p38δ. Skepinone-L dose-dependently blocks the phosphorylation of heat shock protein 27 (HSP27), a p38 MAPK substrate, in response to stimulation with anisomycin (Item No. 11308) in HeLa cells (IC50 = 25 nM) or TNF-α in THP-1 cells.{26162,26163} At 1 µM, it prevents phosphorylation of cytosolic phospholipase A2 in platelets in response to collagen-related peptide or thrombin (Item No. 13188), blunting platelet secretion and aggregation.{26164}
Brand:CaymanSKU:-Out of stock
SKF 38393 is a partial agonist of the dopamine D1-like receptors D1 and D5 (Kis = 1 and ~0.5 nM, respectively).{32473} It less potently binds D2, D3, and D4 receptors (Kis = ~150, 5,000, and 1,000 nM, respectively).{23473,24103}
Brand:CaymanSKU:-Available on backorder
SKF 38393 is a partial agonist of the dopamine D1-like receptors D1 and D5 (Kis = 1 and ~0.5 nM, respectively).{32473} It less potently binds D2, D3, and D4 receptors (Kis = ~150, 5,000, and 1,000 nM, respectively).{23473,24103}
Brand:CaymanSKU:-Available on backorder
SKF 38393 is a partial agonist of the dopamine D1-like receptors D1 and D5 (Kis = 1 and ~0.5 nM, respectively).{32473} It less potently binds D2, D3, and D4 receptors (Kis = ~150, 5,000, and 1,000 nM, respectively).{23473,24103}
Brand:CaymanSKU:-Available on backorder
SKF 38393 is a partial agonist of the dopamine D1-like receptors D1 and D5 (Kis = 1 and ~0.5 nM, respectively).{32473} It less potently binds D2, D3, and D4 receptors (Kis = ~150, 5,000, and 1,000 nM, respectively).{23473,24103}
Brand:CaymanSKU:-Available on backorder
SKF 525A is a widely used, nonspecific cytochrome P (CYP)450 inhibitor that demonstrates 100% inhibition of the various CYP450 isoforms at 1-100 μM.{24114} It therefore potentiates the effects of many different drugs by inhibiting their metabolism (IC50 values in the μM range when tested using human liver microsomes).{24115} SKF 525A inhibits CYP450-dependent arachidonic acid conversion to active EET metabolites, antagonizing the recovery of functional calcium pools.{5318} It also acts as a noncompetitive inhibitor of acetylcholine nicotinic receptors (IC50 = 19 μM in mouse skeletal muscle).{9025,24116}
Brand:CaymanSKU:- SKF 525A is a widely used, nonspecific cytochrome P (CYP)450 inhibitor that demonstrates 100% inhibition of the various CYP450 isoforms at 1-100 μM.{24114} It therefore potentiates the effects of many different drugs by inhibiting their metabolism (IC50 values in the μM range when tested using human liver microsomes).{24115} SKF 525A inhibits CYP450-dependent arachidonic acid conversion to active EET metabolites, antagonizing the recovery of functional calcium pools.{5318} It also acts as a noncompetitive inhibitor of acetylcholine nicotinic receptors (IC50 = 19 μM in mouse skeletal muscle).{9025,24116}
Brand:CaymanSKU:- SKF 525A is a widely used, nonspecific cytochrome P (CYP)450 inhibitor that demonstrates 100% inhibition of the various CYP450 isoforms at 1-100 μM.{24114} It therefore potentiates the effects of many different drugs by inhibiting their metabolism (IC50 values in the μM range when tested using human liver microsomes).{24115} SKF 525A inhibits CYP450-dependent arachidonic acid conversion to active EET metabolites, antagonizing the recovery of functional calcium pools.{5318} It also acts as a noncompetitive inhibitor of acetylcholine nicotinic receptors (IC50 = 19 μM in mouse skeletal muscle).{9025,24116}
Brand:CaymanSKU:- SKF 525A is a widely used, nonspecific cytochrome P (CYP)450 inhibitor that demonstrates 100% inhibition of the various CYP450 isoforms at 1-100 μM.{24114} It therefore potentiates the effects of many different drugs by inhibiting their metabolism (IC50 values in the μM range when tested using human liver microsomes).{24115} SKF 525A inhibits CYP450-dependent arachidonic acid conversion to active EET metabolites, antagonizing the recovery of functional calcium pools.{5318} It also acts as a noncompetitive inhibitor of acetylcholine nicotinic receptors (IC50 = 19 μM in mouse skeletal muscle).{9025,24116}
Brand:CaymanSKU:-
SKF 82958 is a dopamine D1 receptor agonist (K0.5 = 4 nM in a radioligand binding assay).{45668} It is selective for dopamine D1 over D2 receptors (K0.5 = 73 nM). SKF 82958 induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC50 = 491 nM). SKF 82958 (3 mg/kg) prevents and reverses fentanyl-induced respiratory depression, without affecting analgesia, in cats.{45669} It also increases locomotion and rearing in rats.{45670}
Brand:CaymanSKU:29033 - 10 mgAvailable on backorder
SKF 82958 is a dopamine D1 receptor agonist (K0.5 = 4 nM in a radioligand binding assay).{45668} It is selective for dopamine D1 over D2 receptors (K0.5 = 73 nM). SKF 82958 induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC50 = 491 nM). SKF 82958 (3 mg/kg) prevents and reverses fentanyl-induced respiratory depression, without affecting analgesia, in cats.{45669} It also increases locomotion and rearing in rats.{45670}
Brand:CaymanSKU:29033 - 25 mgAvailable on backorder
SKF 82958 is a dopamine D1 receptor agonist (K0.5 = 4 nM in a radioligand binding assay).{45668} It is selective for dopamine D1 over D2 receptors (K0.5 = 73 nM). SKF 82958 induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC50 = 491 nM). SKF 82958 (3 mg/kg) prevents and reverses fentanyl-induced respiratory depression, without affecting analgesia, in cats.{45669} It also increases locomotion and rearing in rats.{45670}
Brand:CaymanSKU:29033 - 5 mgAvailable on backorder
SKF 83566 is a dopamine D1 receptor antagonist.{48782,48783,48784} In vivo, SKF 83566 (0.005, 0.01, and 0.03 mg/kg) reduces dexbenzetimide- and scopolamine-induced locomotor stereotypy in rats.{48782} It decreases ghrelin-induced increases in novel object exploration and food intake in rats when administered at a dose of 100 µg/kg.{48783} SKF 83566 also reduces schedule-induced polydipsia in rats.{48784}
Brand:CaymanSKU:29480 - 10 mgAvailable on backorder
SKF 83566 is a dopamine D1 receptor antagonist.{48782,48783,48784} In vivo, SKF 83566 (0.005, 0.01, and 0.03 mg/kg) reduces dexbenzetimide- and scopolamine-induced locomotor stereotypy in rats.{48782} It decreases ghrelin-induced increases in novel object exploration and food intake in rats when administered at a dose of 100 µg/kg.{48783} SKF 83566 also reduces schedule-induced polydipsia in rats.{48784}
Brand:CaymanSKU:29480 - 25 mgAvailable on backorder
SKF 83566 is a dopamine D1 receptor antagonist.{48782,48783,48784} In vivo, SKF 83566 (0.005, 0.01, and 0.03 mg/kg) reduces dexbenzetimide- and scopolamine-induced locomotor stereotypy in rats.{48782} It decreases ghrelin-induced increases in novel object exploration and food intake in rats when administered at a dose of 100 µg/kg.{48783} SKF 83566 also reduces schedule-induced polydipsia in rats.{48784}
Brand:CaymanSKU:29480 - 5 mgAvailable on backorder
SKF 83959 is a partial agonist at the dopamine D1-like receptors (Kis = 1.18 and 7.56 nM, respectively, for D1 and D5) that is selective over the D2-like receptors (Kis = 920 and 399 nM, respectively, for D2 and D3).{24103,40094} It is protective against oxidative stress in retinal ganglion cells after hydrogen peroxide-induced injury in vitro.{40095} In a rat methylazoxymethanol acetate (MAM) model of schizophrenia, it had positive effects on hippocampal function, determined using electrophysiology, but impaired spatial learning.{40096} SKF 83959 can also act as an allosteric modulator of the sigma-1 (σ1) receptor by enhancing the binding to and delaying the dissociation of the selective σ1-receptor agonist pentazocine.{40097}
Brand:CaymanSKU:22220 -Out of stock
SKF 83959 is a partial agonist at the dopamine D1-like receptors (Kis = 1.18 and 7.56 nM, respectively, for D1 and D5) that is selective over the D2-like receptors (Kis = 920 and 399 nM, respectively, for D2 and D3).{24103,40094} It is protective against oxidative stress in retinal ganglion cells after hydrogen peroxide-induced injury in vitro.{40095} In a rat methylazoxymethanol acetate (MAM) model of schizophrenia, it had positive effects on hippocampal function, determined using electrophysiology, but impaired spatial learning.{40096} SKF 83959 can also act as an allosteric modulator of the sigma-1 (σ1) receptor by enhancing the binding to and delaying the dissociation of the selective σ1-receptor agonist pentazocine.{40097}
Brand:CaymanSKU:22220 -Out of stock
SKF 83959 is a partial agonist at the dopamine D1-like receptors (Kis = 1.18 and 7.56 nM, respectively, for D1 and D5) that is selective over the D2-like receptors (Kis = 920 and 399 nM, respectively, for D2 and D3).{24103,40094} It is protective against oxidative stress in retinal ganglion cells after hydrogen peroxide-induced injury in vitro.{40095} In a rat methylazoxymethanol acetate (MAM) model of schizophrenia, it had positive effects on hippocampal function, determined using electrophysiology, but impaired spatial learning.{40096} SKF 83959 can also act as an allosteric modulator of the sigma-1 (σ1) receptor by enhancing the binding to and delaying the dissociation of the selective σ1-receptor agonist pentazocine.{40097}
Brand:CaymanSKU:22220 -Out of stock
SKF 83959 is a partial agonist at the dopamine D1-like receptors (Kis = 1.18 and 7.56 nM, respectively, for D1 and D5) that is selective over the D2-like receptors (Kis = 920 and 399 nM, respectively, for D2 and D3).{24103,40094} It is protective against oxidative stress in retinal ganglion cells after hydrogen peroxide-induced injury in vitro.{40095} In a rat methylazoxymethanol acetate (MAM) model of schizophrenia, it had positive effects on hippocampal function, determined using electrophysiology, but impaired spatial learning.{40096} SKF 83959 can also act as an allosteric modulator of the sigma-1 (σ1) receptor by enhancing the binding to and delaying the dissociation of the selective σ1-receptor agonist pentazocine.{40097}
Brand:CaymanSKU:22220 -Out of stock
SKF 86002 is an anti-inflammatory agent.{53596,16230,53597,53598} It inhibits rat seminal vesicle prostaglandin H2 (PGH2) synthase (IC50 = 120 µM), as well as prostanoid production by rat basophilic leukemia (RBL-1) cells and human monocytes (IC50s = 70 and 1 µM, respectively).{53596} SKF 86002 inhibits leukotriene B4 (LTB4) and LTC4 production induced by A23187 (Item No. 11016) in human neutrophils and monocytes, respectively (IC50 = 20 µM for both). It also inhibits LPS-induced IL-1 production in human monocytes (IC50 = 1.3 µM).{16230} SKF 86002 (10, 30, and 90 mg/kg) reduces hindleg volume in rat models of adjuvant- or collagen-induced arthritis.{53597} It also decreases serum levels of TNF-α and increases survival in a mouse model of LPS and galactosamine-induced endotoxic shock when administered at a dose of 100 mg/kg.{53598}
Brand:CaymanSKU:30202 - 1 mgAvailable on backorder
SKF 86002 is an anti-inflammatory agent.{53596,16230,53597,53598} It inhibits rat seminal vesicle prostaglandin H2 (PGH2) synthase (IC50 = 120 µM), as well as prostanoid production by rat basophilic leukemia (RBL-1) cells and human monocytes (IC50s = 70 and 1 µM, respectively).{53596} SKF 86002 inhibits leukotriene B4 (LTB4) and LTC4 production induced by A23187 (Item No. 11016) in human neutrophils and monocytes, respectively (IC50 = 20 µM for both). It also inhibits LPS-induced IL-1 production in human monocytes (IC50 = 1.3 µM).{16230} SKF 86002 (10, 30, and 90 mg/kg) reduces hindleg volume in rat models of adjuvant- or collagen-induced arthritis.{53597} It also decreases serum levels of TNF-α and increases survival in a mouse model of LPS and galactosamine-induced endotoxic shock when administered at a dose of 100 mg/kg.{53598}
Brand:CaymanSKU:30202 - 10 mgAvailable on backorder
SKF 86002 is an anti-inflammatory agent.{53596,16230,53597,53598} It inhibits rat seminal vesicle prostaglandin H2 (PGH2) synthase (IC50 = 120 µM), as well as prostanoid production by rat basophilic leukemia (RBL-1) cells and human monocytes (IC50s = 70 and 1 µM, respectively).{53596} SKF 86002 inhibits leukotriene B4 (LTB4) and LTC4 production induced by A23187 (Item No. 11016) in human neutrophils and monocytes, respectively (IC50 = 20 µM for both). It also inhibits LPS-induced IL-1 production in human monocytes (IC50 = 1.3 µM).{16230} SKF 86002 (10, 30, and 90 mg/kg) reduces hindleg volume in rat models of adjuvant- or collagen-induced arthritis.{53597} It also decreases serum levels of TNF-α and increases survival in a mouse model of LPS and galactosamine-induced endotoxic shock when administered at a dose of 100 mg/kg.{53598}
Brand:CaymanSKU:30202 - 25 mgAvailable on backorder
SKF 86002 is an anti-inflammatory agent.{53596,16230,53597,53598} It inhibits rat seminal vesicle prostaglandin H2 (PGH2) synthase (IC50 = 120 µM), as well as prostanoid production by rat basophilic leukemia (RBL-1) cells and human monocytes (IC50s = 70 and 1 µM, respectively).{53596} SKF 86002 inhibits leukotriene B4 (LTB4) and LTC4 production induced by A23187 (Item No. 11016) in human neutrophils and monocytes, respectively (IC50 = 20 µM for both). It also inhibits LPS-induced IL-1 production in human monocytes (IC50 = 1.3 µM).{16230} SKF 86002 (10, 30, and 90 mg/kg) reduces hindleg volume in rat models of adjuvant- or collagen-induced arthritis.{53597} It also decreases serum levels of TNF-α and increases survival in a mouse model of LPS and galactosamine-induced endotoxic shock when administered at a dose of 100 mg/kg.{53598}
Brand:CaymanSKU:30202 - 5 mgAvailable on backorder
SKF 86466 is a selective antagonist of α2-adrenoceptors that shows nanomolar Ki values for the three subtypes, α2A, α2B, and α2C.{34495,34497} It is active in vivo, evoking antihypertensive effects in animal studies and clinical trials.{34494,34497} SKF 86466 is used to study the role of α2-adrenoceptors in animals.{34496,34498}
Brand:CaymanSKU:11953 - 1 mgAvailable on backorder
SKF 86466 is a selective antagonist of α2-adrenoceptors that shows nanomolar Ki values for the three subtypes, α2A, α2B, and α2C.{34495,34497} It is active in vivo, evoking antihypertensive effects in animal studies and clinical trials.{34494,34497} SKF 86466 is used to study the role of α2-adrenoceptors in animals.{34496,34498}
Brand:CaymanSKU:11953 - 10 mgAvailable on backorder
SKF 86466 is a selective antagonist of α2-adrenoceptors that shows nanomolar Ki values for the three subtypes, α2A, α2B, and α2C.{34495,34497} It is active in vivo, evoking antihypertensive effects in animal studies and clinical trials.{34494,34497} SKF 86466 is used to study the role of α2-adrenoceptors in animals.{34496,34498}
Brand:CaymanSKU:11953 - 25 mgAvailable on backorder
SKF 86466 is a selective antagonist of α2-adrenoceptors that shows nanomolar Ki values for the three subtypes, α2A, α2B, and α2C.{34495,34497} It is active in vivo, evoking antihypertensive effects in animal studies and clinical trials.{34494,34497} SKF 86466 is used to study the role of α2-adrenoceptors in animals.{34496,34498}
Brand:CaymanSKU:11953 - 5 mgAvailable on backorder
SKF 96365 inhibits the receptor-mediated influx of calcium via voltage-gated calcium channels with an IC50 value of approximately 10 µM.{14573} It inhibits the acetylcholine-induced depolarization of circular smooth muscle in a dose-dependent manner at 3-50 µM.{14572} SKF 96365 can distinguish receptor-mediated release in platelets and neutrophils from the calcium release from internal stores. However, it does not distinguish between receptor-mediated and voltage-gated release.
Brand:CaymanSKU:10009312 - 1 mgAvailable on backorder
SKF 96365 inhibits the receptor-mediated influx of calcium via voltage-gated calcium channels with an IC50 value of approximately 10 µM.{14573} It inhibits the acetylcholine-induced depolarization of circular smooth muscle in a dose-dependent manner at 3-50 µM.{14572} SKF 96365 can distinguish receptor-mediated release in platelets and neutrophils from the calcium release from internal stores. However, it does not distinguish between receptor-mediated and voltage-gated release.
Brand:CaymanSKU:10009312 - 10 mgAvailable on backorder
SKF 96365 inhibits the receptor-mediated influx of calcium via voltage-gated calcium channels with an IC50 value of approximately 10 µM.{14573} It inhibits the acetylcholine-induced depolarization of circular smooth muscle in a dose-dependent manner at 3-50 µM.{14572} SKF 96365 can distinguish receptor-mediated release in platelets and neutrophils from the calcium release from internal stores. However, it does not distinguish between receptor-mediated and voltage-gated release.
Brand:CaymanSKU:10009312 - 5 mgAvailable on backorder
SKF 96365 inhibits the receptor-mediated influx of calcium via voltage-gated calcium channels with an IC50 value of approximately 10 µM.{14573} It inhibits the acetylcholine-induced depolarization of circular smooth muscle in a dose-dependent manner at 3-50 µM.{14572} SKF 96365 can distinguish receptor-mediated release in platelets and neutrophils from the calcium release from internal stores. However, it does not distinguish between receptor-mediated and voltage-gated release.
Brand:CaymanSKU:10009312 - 50 mgAvailable on backorder
SKI 178 is an inhibitor of sphingosine kinase 1 (SPHK1) and SPHK2.{41966} Though previously thought to be selective for SPHK1, cellular thermal shift assay results demonstrate direct target engagement of both SPHK1 and SPHK2 in HEK293 cells overexpressing either SPHK1 or SPHK2. It inhibits SPHK1 by 59.6% when used at a concentration of 10.7 µM and inhibits the production of sphingosine-1-phosphate (S1P; Item No. 62570) in A549 cells.{41964} SKI 178 is cytotoxic to a variety of cancer cell lines including PANC-1, A549, U251, and MCF-7 cells (IC50s = 0.1, 0.3, 0.5, and 1.3 µM, respectively). It prolongs mitosis and induces cell death through the intrinsic apoptotic pathway in a CDK1-dependent manner.{41965} SKI 178 (20 mg/kg every other day) reduces the number of white blood cells to a normal range and increases survival in an MLL-AF9 acute myeloid leukemia (AML) mouse xenograft model.{41966} It also destabilizes and inhibits microtubule polymerization in an SPHK-independent manner.
Brand:CaymanSKU:24880 - 10 mgAvailable on backorder
SKI 178 is an inhibitor of sphingosine kinase 1 (SPHK1) and SPHK2.{41966} Though previously thought to be selective for SPHK1, cellular thermal shift assay results demonstrate direct target engagement of both SPHK1 and SPHK2 in HEK293 cells overexpressing either SPHK1 or SPHK2. It inhibits SPHK1 by 59.6% when used at a concentration of 10.7 µM and inhibits the production of sphingosine-1-phosphate (S1P; Item No. 62570) in A549 cells.{41964} SKI 178 is cytotoxic to a variety of cancer cell lines including PANC-1, A549, U251, and MCF-7 cells (IC50s = 0.1, 0.3, 0.5, and 1.3 µM, respectively). It prolongs mitosis and induces cell death through the intrinsic apoptotic pathway in a CDK1-dependent manner.{41965} SKI 178 (20 mg/kg every other day) reduces the number of white blood cells to a normal range and increases survival in an MLL-AF9 acute myeloid leukemia (AML) mouse xenograft model.{41966} It also destabilizes and inhibits microtubule polymerization in an SPHK-independent manner.
Brand:CaymanSKU:24880 - 5 mgAvailable on backorder
SKL2001 is an activator of Wnt/β-catenin signaling.{47093,47094} It increases β-catenin responsive transcription in a cell-based reporter assay in a concentration-dependent manner, increases β-catenin protein levels in HEK293 cells when used at concentrations of 10 and 30 μM, and disrupts the interaction between Axin and β-catenin.{47093} SKL2001 increases alkaline phosphatase (ALP) activity and mineralization in multipotent mesenchymal ST2 cells in a concentration-dependent manner, indicating increased osteoblastogenesis. SKL2001 (40 μM) reduces HCT116 and HT-29 spheroid growth and inhibits proliferation of HCT116 and HT-29 cells.{47094} It induces cell cycle arrest at the G0/G1 phase and increases E-cadherin and β-catenin protein levels in HCT116 cells when used at a concentration of 40 μM.
Brand:CaymanSKU:26334 - 10 mgAvailable on backorder
SKL2001 is an activator of Wnt/β-catenin signaling.{47093,47094} It increases β-catenin responsive transcription in a cell-based reporter assay in a concentration-dependent manner, increases β-catenin protein levels in HEK293 cells when used at concentrations of 10 and 30 μM, and disrupts the interaction between Axin and β-catenin.{47093} SKL2001 increases alkaline phosphatase (ALP) activity and mineralization in multipotent mesenchymal ST2 cells in a concentration-dependent manner, indicating increased osteoblastogenesis. SKL2001 (40 μM) reduces HCT116 and HT-29 spheroid growth and inhibits proliferation of HCT116 and HT-29 cells.{47094} It induces cell cycle arrest at the G0/G1 phase and increases E-cadherin and β-catenin protein levels in HCT116 cells when used at a concentration of 40 μM.
Brand:CaymanSKU:26334 - 100 mgAvailable on backorder
SKL2001 is an activator of Wnt/β-catenin signaling.{47093,47094} It increases β-catenin responsive transcription in a cell-based reporter assay in a concentration-dependent manner, increases β-catenin protein levels in HEK293 cells when used at concentrations of 10 and 30 μM, and disrupts the interaction between Axin and β-catenin.{47093} SKL2001 increases alkaline phosphatase (ALP) activity and mineralization in multipotent mesenchymal ST2 cells in a concentration-dependent manner, indicating increased osteoblastogenesis. SKL2001 (40 μM) reduces HCT116 and HT-29 spheroid growth and inhibits proliferation of HCT116 and HT-29 cells.{47094} It induces cell cycle arrest at the G0/G1 phase and increases E-cadherin and β-catenin protein levels in HCT116 cells when used at a concentration of 40 μM.
Brand:CaymanSKU:26334 - 25 mgAvailable on backorder
SKL2001 is an activator of Wnt/β-catenin signaling.{47093,47094} It increases β-catenin responsive transcription in a cell-based reporter assay in a concentration-dependent manner, increases β-catenin protein levels in HEK293 cells when used at concentrations of 10 and 30 μM, and disrupts the interaction between Axin and β-catenin.{47093} SKL2001 increases alkaline phosphatase (ALP) activity and mineralization in multipotent mesenchymal ST2 cells in a concentration-dependent manner, indicating increased osteoblastogenesis. SKL2001 (40 μM) reduces HCT116 and HT-29 spheroid growth and inhibits proliferation of HCT116 and HT-29 cells.{47094} It induces cell cycle arrest at the G0/G1 phase and increases E-cadherin and β-catenin protein levels in HCT116 cells when used at a concentration of 40 μM.
Brand:CaymanSKU:26334 - 5 mgAvailable on backorder
SKLB610 is an inhibitor of VEGF receptor 2 (VEGFR2).{52033} It inhibits VEGFR2 activity by 97% but also inhibits FGFR2 and PDGFRβ activity by 65 and 55%, respectively, when used at a concentration of 10 µM. It is selective for VEGFR2, FGFR2, and PDGFRβ over PI3K, EGFR, Aurora A, Cdk2/cyclin E, and Cdk6/cyclin D3 at 10 µM. SKLB610 inhibits phosphorylation of VEGFR2 induced by VEGF in human umbilical vein endothelial cells (HUVECs). It inhibits proliferation of HUVECs induced by VEGF and basic FGF (bFGF; IC50s = 2.2 and 4.7 µM, respectively). It also inhibits HUVEC capillary tube formation and migration when used at concentrations of 2.5 and 10 µM, respectively. SKLB610 inhibits proliferation of a variety of cancer cells, including A549 human lung cancer, HCT116 human colorectal carcinoma, MDA-MB-231 human mammary carcinoma, Raji human Burkitt’s lymphoma, and DU145 human prostate cancer cells (IC50s = 5.7, 5.3, 25.6, 6.4, and 6.3 µM, respectively). It reduces tumor growth in A549 and HCT116 mouse xenograft models when administered at a dose of 50 mg/kg per day.
Brand:CaymanSKU:21561 -Out of stock
SKLB610 is an inhibitor of VEGF receptor 2 (VEGFR2).{52033} It inhibits VEGFR2 activity by 97% but also inhibits FGFR2 and PDGFRβ activity by 65 and 55%, respectively, when used at a concentration of 10 µM. It is selective for VEGFR2, FGFR2, and PDGFRβ over PI3K, EGFR, Aurora A, Cdk2/cyclin E, and Cdk6/cyclin D3 at 10 µM. SKLB610 inhibits phosphorylation of VEGFR2 induced by VEGF in human umbilical vein endothelial cells (HUVECs). It inhibits proliferation of HUVECs induced by VEGF and basic FGF (bFGF; IC50s = 2.2 and 4.7 µM, respectively). It also inhibits HUVEC capillary tube formation and migration when used at concentrations of 2.5 and 10 µM, respectively. SKLB610 inhibits proliferation of a variety of cancer cells, including A549 human lung cancer, HCT116 human colorectal carcinoma, MDA-MB-231 human mammary carcinoma, Raji human Burkitt’s lymphoma, and DU145 human prostate cancer cells (IC50s = 5.7, 5.3, 25.6, 6.4, and 6.3 µM, respectively). It reduces tumor growth in A549 and HCT116 mouse xenograft models when administered at a dose of 50 mg/kg per day.
Brand:CaymanSKU:21561 -Out of stock
SKLB610 is an inhibitor of VEGF receptor 2 (VEGFR2).{52033} It inhibits VEGFR2 activity by 97% but also inhibits FGFR2 and PDGFRβ activity by 65 and 55%, respectively, when used at a concentration of 10 µM. It is selective for VEGFR2, FGFR2, and PDGFRβ over PI3K, EGFR, Aurora A, Cdk2/cyclin E, and Cdk6/cyclin D3 at 10 µM. SKLB610 inhibits phosphorylation of VEGFR2 induced by VEGF in human umbilical vein endothelial cells (HUVECs). It inhibits proliferation of HUVECs induced by VEGF and basic FGF (bFGF; IC50s = 2.2 and 4.7 µM, respectively). It also inhibits HUVEC capillary tube formation and migration when used at concentrations of 2.5 and 10 µM, respectively. SKLB610 inhibits proliferation of a variety of cancer cells, including A549 human lung cancer, HCT116 human colorectal carcinoma, MDA-MB-231 human mammary carcinoma, Raji human Burkitt’s lymphoma, and DU145 human prostate cancer cells (IC50s = 5.7, 5.3, 25.6, 6.4, and 6.3 µM, respectively). It reduces tumor growth in A549 and HCT116 mouse xenograft models when administered at a dose of 50 mg/kg per day.
Brand:CaymanSKU:21561 -Out of stock
SKLB610 is an inhibitor of VEGF receptor 2 (VEGFR2).{52033} It inhibits VEGFR2 activity by 97% but also inhibits FGFR2 and PDGFRβ activity by 65 and 55%, respectively, when used at a concentration of 10 µM. It is selective for VEGFR2, FGFR2, and PDGFRβ over PI3K, EGFR, Aurora A, Cdk2/cyclin E, and Cdk6/cyclin D3 at 10 µM. SKLB610 inhibits phosphorylation of VEGFR2 induced by VEGF in human umbilical vein endothelial cells (HUVECs). It inhibits proliferation of HUVECs induced by VEGF and basic FGF (bFGF; IC50s = 2.2 and 4.7 µM, respectively). It also inhibits HUVEC capillary tube formation and migration when used at concentrations of 2.5 and 10 µM, respectively. SKLB610 inhibits proliferation of a variety of cancer cells, including A549 human lung cancer, HCT116 human colorectal carcinoma, MDA-MB-231 human mammary carcinoma, Raji human Burkitt’s lymphoma, and DU145 human prostate cancer cells (IC50s = 5.7, 5.3, 25.6, 6.4, and 6.3 µM, respectively). It reduces tumor growth in A549 and HCT116 mouse xenograft models when administered at a dose of 50 mg/kg per day.
Brand:CaymanSKU:21561 -Out of stock
SKPin C1 is an inhibitor of Skp1-Cullin1-F-box (SCF) family protein Skp2-mediated p27 degradation.{45107} It binds to Skp2 at the Cdc kinase subunit 1 (Cks1) interaction interface and blocks ubiquitylation of p27 in a Cks1-dependent manner in vitro when used at a concentration of 50 μM. SKPin C1 increases nuclear accumulation of p27 in ECC-1 endometrial carcinoma cells.{45108}
Brand:CaymanSKU:26141 - 10 mgAvailable on backorder
SKPin C1 is an inhibitor of Skp1-Cullin1-F-box (SCF) family protein Skp2-mediated p27 degradation.{45107} It binds to Skp2 at the Cdc kinase subunit 1 (Cks1) interaction interface and blocks ubiquitylation of p27 in a Cks1-dependent manner in vitro when used at a concentration of 50 μM. SKPin C1 increases nuclear accumulation of p27 in ECC-1 endometrial carcinoma cells.{45108}
Brand:CaymanSKU:26141 - 25 mgAvailable on backorder
SKPin C1 is an inhibitor of Skp1-Cullin1-F-box (SCF) family protein Skp2-mediated p27 degradation.{45107} It binds to Skp2 at the Cdc kinase subunit 1 (Cks1) interaction interface and blocks ubiquitylation of p27 in a Cks1-dependent manner in vitro when used at a concentration of 50 μM. SKPin C1 increases nuclear accumulation of p27 in ECC-1 endometrial carcinoma cells.{45108}
Brand:CaymanSKU:26141 - 5 mgAvailable on backorder
SKQ1 (bromide) is a mitochondria-targeted antioxidant that decreases transmembrane potential and production of reactive oxygen species (ROS).{34427} SKQ1 prevents neuronal loss and synaptic damage in a rat model of spontaneous Alzheimer’s disease, as well as decreases severity of arthritic lesions in rats.{34430,34431} SKQ1 slows development of age-related ocular pathologies in murine, porcine, bovine, and canine model systems.{34429} It also prevents acute phenoptosis following rhabdomyolysis, stroke, and myocardial infarction.{34426,34428,34432}
Brand:CaymanSKU:19891 -Available on backorder
SKQ1 (bromide) is a mitochondria-targeted antioxidant that decreases transmembrane potential and production of reactive oxygen species (ROS).{34427} SKQ1 prevents neuronal loss and synaptic damage in a rat model of spontaneous Alzheimer’s disease, as well as decreases severity of arthritic lesions in rats.{34430,34431} SKQ1 slows development of age-related ocular pathologies in murine, porcine, bovine, and canine model systems.{34429} It also prevents acute phenoptosis following rhabdomyolysis, stroke, and myocardial infarction.{34426,34428,34432}
Brand:CaymanSKU:19891 -Available on backorder
SKQ1 (bromide) is a mitochondria-targeted antioxidant that decreases transmembrane potential and production of reactive oxygen species (ROS).{34427} SKQ1 prevents neuronal loss and synaptic damage in a rat model of spontaneous Alzheimer’s disease, as well as decreases severity of arthritic lesions in rats.{34430,34431} SKQ1 slows development of age-related ocular pathologies in murine, porcine, bovine, and canine model systems.{34429} It also prevents acute phenoptosis following rhabdomyolysis, stroke, and myocardial infarction.{34426,34428,34432}
Brand:CaymanSKU:19891 -Available on backorder
SKQ1 (bromide) is a mitochondria-targeted antioxidant that decreases transmembrane potential and production of reactive oxygen species (ROS).{34427} SKQ1 prevents neuronal loss and synaptic damage in a rat model of spontaneous Alzheimer’s disease, as well as decreases severity of arthritic lesions in rats.{34430,34431} SKQ1 slows development of age-related ocular pathologies in murine, porcine, bovine, and canine model systems.{34429} It also prevents acute phenoptosis following rhabdomyolysis, stroke, and myocardial infarction.{34426,34428,34432}
Brand:CaymanSKU:19891 -Available on backorder
Skyrin is a fungal metabolite characterized by a bisanthraquinone structure. It interferes with glucagon signaling through adenylate cyclase without binding to the glucagon receptor.{21666} At 10 μM, skyrin reduces both glucagon-stimulated cAMP production and glycogenolysis.{21666} It does not interfere with epinephrine or glucagon-like peptide 1 effects on these parameters.{21666}
Brand:CaymanSKU:-
SL 01 is a prodrug of gemcitabine (Item No. 11690), the nucleoside analog used intravenously to treat various cancers that was designed for improved oral bioavailability.{24479} SL 01 can inhibit the growth of human non-small cell lung cancer NCI-H460 cells, colon cancer HCT116 cells, and breast cancer MCF-7 cells (IC50s = 0.78, 0.92, and 0.64 μM, respectively), inducing apoptosis.{24480,24481} In nude mice bearing NCI-H460, HCT116, or MCF-7 cancer cell xenografts, SL 01 at 10-50 μM/kg has been shown to delay tumor growth.{24480,24481}
Brand:CaymanSKU:- SL 01 is a prodrug of gemcitabine (Item No. 11690), the nucleoside analog used intravenously to treat various cancers that was designed for improved oral bioavailability.{24479} SL 01 can inhibit the growth of human non-small cell lung cancer NCI-H460 cells, colon cancer HCT116 cells, and breast cancer MCF-7 cells (IC50s = 0.78, 0.92, and 0.64 μM, respectively), inducing apoptosis.{24480,24481} In nude mice bearing NCI-H460, HCT116, or MCF-7 cancer cell xenografts, SL 01 at 10-50 μM/kg has been shown to delay tumor growth.{24480,24481}
Brand:CaymanSKU:- SL 01 is a prodrug of gemcitabine (Item No. 11690), the nucleoside analog used intravenously to treat various cancers that was designed for improved oral bioavailability.{24479} SL 01 can inhibit the growth of human non-small cell lung cancer NCI-H460 cells, colon cancer HCT116 cells, and breast cancer MCF-7 cells (IC50s = 0.78, 0.92, and 0.64 μM, respectively), inducing apoptosis.{24480,24481} In nude mice bearing NCI-H460, HCT116, or MCF-7 cancer cell xenografts, SL 01 at 10-50 μM/kg has been shown to delay tumor growth.{24480,24481}
Brand:CaymanSKU:-
The p90 ribosomal S6 kinases (RSK) 1-4 are downstream members of the extracellular signal-regulated kinase (ERK)/MAPK cascade. SL 0101-1 is a kaempferol glycoside, isolated from the tropical plant F. refracta, that selectively inhibits RSK2 with an IC50 value of 89 nM (Ki = 1 μM) without interfering with upstream activators of RSK, including ERK, MEK, EGFR, and PKC.{22410} At 100 μM, SL 0101-1 inhibits the proliferation of MCF-7 breast cancer cells, arresting cells in the G1 phase of the cell cycle.{22410} SL 0101-1 has been used to characterize the intracellular signaling events associated with angiotensin II-induced tyrosine kinase activation with a concentration of 30 μM attenuating angiotensin II-induced cell proliferation.{22411}
Brand:CaymanSKU:11704 - 1 mgAvailable on backorder
The p90 ribosomal S6 kinases (RSK) 1-4 are downstream members of the extracellular signal-regulated kinase (ERK)/MAPK cascade. SL 0101-1 is a kaempferol glycoside, isolated from the tropical plant F. refracta, that selectively inhibits RSK2 with an IC50 value of 89 nM (Ki = 1 μM) without interfering with upstream activators of RSK, including ERK, MEK, EGFR, and PKC.{22410} At 100 μM, SL 0101-1 inhibits the proliferation of MCF-7 breast cancer cells, arresting cells in the G1 phase of the cell cycle.{22410} SL 0101-1 has been used to characterize the intracellular signaling events associated with angiotensin II-induced tyrosine kinase activation with a concentration of 30 μM attenuating angiotensin II-induced cell proliferation.{22411}
Brand:CaymanSKU:11704 - 10 mgAvailable on backorder
The p90 ribosomal S6 kinases (RSK) 1-4 are downstream members of the extracellular signal-regulated kinase (ERK)/MAPK cascade. SL 0101-1 is a kaempferol glycoside, isolated from the tropical plant F. refracta, that selectively inhibits RSK2 with an IC50 value of 89 nM (Ki = 1 μM) without interfering with upstream activators of RSK, including ERK, MEK, EGFR, and PKC.{22410} At 100 μM, SL 0101-1 inhibits the proliferation of MCF-7 breast cancer cells, arresting cells in the G1 phase of the cell cycle.{22410} SL 0101-1 has been used to characterize the intracellular signaling events associated with angiotensin II-induced tyrosine kinase activation with a concentration of 30 μM attenuating angiotensin II-induced cell proliferation.{22411}
Brand:CaymanSKU:11704 - 5 mgAvailable on backorder
The p90 ribosomal S6 kinases (RSK) 1-4 are downstream members of the extracellular signal-regulated kinase (ERK)/MAPK cascade. SL 0101-1 is a kaempferol glycoside, isolated from the tropical plant F. refracta, that selectively inhibits RSK2 with an IC50 value of 89 nM (Ki = 1 μM) without interfering with upstream activators of RSK, including ERK, MEK, EGFR, and PKC.{22410} At 100 μM, SL 0101-1 inhibits the proliferation of MCF-7 breast cancer cells, arresting cells in the G1 phase of the cell cycle.{22410} SL 0101-1 has been used to characterize the intracellular signaling events associated with angiotensin II-induced tyrosine kinase activation with a concentration of 30 μM attenuating angiotensin II-induced cell proliferation.{22411}
Brand:CaymanSKU:11704 - 500 µgAvailable on backorder
The dual specific threonine/tyrosine kinase MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates a diverse array of cellular processes. SL 327 is an inhibitor of MEK1 and MEK2 (IC50s = 0.18 and 0.22 μM), the kinases upstream of ERK1/2.{10576} It inhibits ERK1, MKK/p38, MKK4, JNK, and PKC at much higher concentrations (IC50s = >50, 21, >100, >100, >10 μM, respectively).{10576} Since SL 327 rapidly passes the blood-brain barrier, it has been used to dissect the effect of RAS/RAF/MEK/ERK signaling pathway inhibition on behavior, including long-term memory, spatial learning, and fear/operant conditioning.{25503}
Brand:CaymanSKU:- The dual specific threonine/tyrosine kinase MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates a diverse array of cellular processes. SL 327 is an inhibitor of MEK1 and MEK2 (IC50s = 0.18 and 0.22 μM), the kinases upstream of ERK1/2.{10576} It inhibits ERK1, MKK/p38, MKK4, JNK, and PKC at much higher concentrations (IC50s = >50, 21, >100, >100, >10 μM, respectively).{10576} Since SL 327 rapidly passes the blood-brain barrier, it has been used to dissect the effect of RAS/RAF/MEK/ERK signaling pathway inhibition on behavior, including long-term memory, spatial learning, and fear/operant conditioning.{25503}
Brand:CaymanSKU:- The dual specific threonine/tyrosine kinase MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates a diverse array of cellular processes. SL 327 is an inhibitor of MEK1 and MEK2 (IC50s = 0.18 and 0.22 μM), the kinases upstream of ERK1/2.{10576} It inhibits ERK1, MKK/p38, MKK4, JNK, and PKC at much higher concentrations (IC50s = >50, 21, >100, >100, >10 μM, respectively).{10576} Since SL 327 rapidly passes the blood-brain barrier, it has been used to dissect the effect of RAS/RAF/MEK/ERK signaling pathway inhibition on behavior, including long-term memory, spatial learning, and fear/operant conditioning.{25503}
Brand:CaymanSKU:- The dual specific threonine/tyrosine kinase MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates a diverse array of cellular processes. SL 327 is an inhibitor of MEK1 and MEK2 (IC50s = 0.18 and 0.22 μM), the kinases upstream of ERK1/2.{10576} It inhibits ERK1, MKK/p38, MKK4, JNK, and PKC at much higher concentrations (IC50s = >50, 21, >100, >100, >10 μM, respectively).{10576} Since SL 327 rapidly passes the blood-brain barrier, it has been used to dissect the effect of RAS/RAF/MEK/ERK signaling pathway inhibition on behavior, including long-term memory, spatial learning, and fear/operant conditioning.{25503}
Brand:CaymanSKU:-
SL-164 (Item No. 28244) is an analytical reference standard categorized as a quinazolinone. SL-164 has sedative properties.{48951} This product is intended for research and forensic applications.
Brand:CaymanSKU:28244 - 1 mgAvailable on backorder
SL-164 (Item No. 28244) is an analytical reference standard categorized as a quinazolinone. SL-164 has sedative properties.{48951} This product is intended for research and forensic applications.
Brand:CaymanSKU:28244 - 5 mgAvailable on backorder
SL-651,498 (Item No. 22008) is an analytical reference standard categorized as a nonbenzodiazepine anxiolytic.{45977} SL-651,498 has anxiolytic and anticonvulsant effects in rodents that are not associated with physical dependence or the development of anticonvulsant tolerance. It also does not induce sedation at anxiolytic-relevant doses in rats. This product is intended for research and forensic applications.
Brand:CaymanSKU:22008 -Out of stock
SLC5111312 is a dual inhibitor of sphingosine kinase 1 (SPHK1) and SPHK2 (Kis = 0.73 and 0.9 µM, respectively, using human recombinant kinases).{38412} SLC5111312 binding is selective for Sphk2 over Sphk1 in mice (Kis = 1 and 20 µM, respectively) but not rat (Kis = 1.1 and 0.8 µM, respectively).{38413} It decreases cell-associated sphingosine-1-phosphate (S1P) and increases sphingosine in U937 monocytic leukemia cells at concentrations of 0.1 and 0.3 µM. SLC5111312 (10 mg/kg) also decreases S1P in vivo in Sphk1-/- but not in Sphk2-/- mice and in rat, showing a functional selectivity for Sphk2 in mice.
Brand:CaymanSKU:23288 - 1 mgAvailable on backorder
SLC5111312 is a dual inhibitor of sphingosine kinase 1 (SPHK1) and SPHK2 (Kis = 0.73 and 0.9 µM, respectively, using human recombinant kinases).{38412} SLC5111312 binding is selective for Sphk2 over Sphk1 in mice (Kis = 1 and 20 µM, respectively) but not rat (Kis = 1.1 and 0.8 µM, respectively).{38413} It decreases cell-associated sphingosine-1-phosphate (S1P) and increases sphingosine in U937 monocytic leukemia cells at concentrations of 0.1 and 0.3 µM. SLC5111312 (10 mg/kg) also decreases S1P in vivo in Sphk1-/- but not in Sphk2-/- mice and in rat, showing a functional selectivity for Sphk2 in mice.
Brand:CaymanSKU:23288 - 5 mgAvailable on backorder
SLC5111312 is a dual inhibitor of sphingosine kinase 1 (SPHK1) and SPHK2 (Kis = 0.73 and 0.9 µM, respectively, using human recombinant kinases).{38412} SLC5111312 binding is selective for Sphk2 over Sphk1 in mice (Kis = 1 and 20 µM, respectively) but not rat (Kis = 1.1 and 0.8 µM, respectively).{38413} It decreases cell-associated sphingosine-1-phosphate (S1P) and increases sphingosine in U937 monocytic leukemia cells at concentrations of 0.1 and 0.3 µM. SLC5111312 (10 mg/kg) also decreases S1P in vivo in Sphk1-/- but not in Sphk2-/- mice and in rat, showing a functional selectivity for Sphk2 in mice.
Brand:CaymanSKU:23288 - 500 µgAvailable on backorder
FK-506 is a potent immunosuppressant that forms a high affinity complex (Ki = 0.2 nM) with FK-506 binding protein 12 (FKBP12). This complex inhibits the activity of the calcium/calmodulin-dependent protein phosphatase, calcineurin, leading to disruption of T-cell activation.{13842} Synthetic ligand of FKBP (SLF) is a cell-permeable analog of FK-506 that binds tightly to FKBP but lacks the ability to inhibit calcineurin.{13706} By itself, SLF does not exhibit a significant cellular response. However, homodimers of SLF or heterodimers with another protein ligand, provide a method to promote the dimerization of ligand-specific fusion proteins to induce signaling events within a cellular environment.{13706,13701} For example, SLF monomers connected with a 10-atom linker activates Fas signaling via Fas-FKBP fusion proteins with an EC50 of 6 nM.{13701}
Brand:CaymanSKU:10007974 - 10 mgAvailable on backorder
FK-506 is a potent immunosuppressant that forms a high affinity complex (Ki = 0.2 nM) with FK-506 binding protein 12 (FKBP12). This complex inhibits the activity of the calcium/calmodulin-dependent protein phosphatase, calcineurin, leading to disruption of T-cell activation.{13842} Synthetic ligand of FKBP (SLF) is a cell-permeable analog of FK-506 that binds tightly to FKBP but lacks the ability to inhibit calcineurin.{13706} By itself, SLF does not exhibit a significant cellular response. However, homodimers of SLF or heterodimers with another protein ligand, provide a method to promote the dimerization of ligand-specific fusion proteins to induce signaling events within a cellular environment.{13706,13701} For example, SLF monomers connected with a 10-atom linker activates Fas signaling via Fas-FKBP fusion proteins with an EC50 of 6 nM.{13701}
Brand:CaymanSKU:10007974 - 100 mgAvailable on backorder
FK-506 is a potent immunosuppressant that forms a high affinity complex (Ki = 0.2 nM) with FK-506 binding protein 12 (FKBP12). This complex inhibits the activity of the calcium/calmodulin-dependent protein phosphatase, calcineurin, leading to disruption of T-cell activation.{13842} Synthetic ligand of FKBP (SLF) is a cell-permeable analog of FK-506 that binds tightly to FKBP but lacks the ability to inhibit calcineurin.{13706} By itself, SLF does not exhibit a significant cellular response. However, homodimers of SLF or heterodimers with another protein ligand, provide a method to promote the dimerization of ligand-specific fusion proteins to induce signaling events within a cellular environment.{13706,13701} For example, SLF monomers connected with a 10-atom linker activates Fas signaling via Fas-FKBP fusion proteins with an EC50 of 6 nM.{13701}
Brand:CaymanSKU:10007974 - 5 mgAvailable on backorder
FK-506 is a potent immunosuppressant that forms a high affinity complex (Ki = 0.2 nM) with FK-506 binding protein 12 (FKBP12). This complex inhibits the activity of the calcium/calmodulin-dependent protein phosphatase, calcineurin, leading to disruption of T-cell activation.{13842} Synthetic ligand of FKBP (SLF) is a cell-permeable analog of FK-506 that binds tightly to FKBP but lacks the ability to inhibit calcineurin.{13706} By itself, SLF does not exhibit a significant cellular response. However, homodimers of SLF or heterodimers with another protein ligand, provide a method to promote the dimerization of ligand-specific fusion proteins to induce signaling events within a cellular environment.{13706,13701} For example, SLF monomers connected with a 10-atom linker activates Fas signaling via Fas-FKBP fusion proteins with an EC50 of 6 nM.{13701}
Brand:CaymanSKU:10007974 - 50 mgAvailable on backorder
SLM6031434 is an inhibitor of sphingosine kinase 2 (SPHK2) (Ki = 0.4 μM for the recombinant mouse enzyme).{38413} It is selective for SPHK2 over SPHK1 (Kis = >20 μM). It decreases sphingosine-1-phosphate (S1P; Item No. 62570) and increases sphingosine levels in U937 monocytic leukemia cells in a concentration-dependent manner. SLM6031434 (5 mg/kg) reduces blood S1P levels in Sphk1-/-, but not Sphk2-/-, mice. SLM6031434 also increases blood S1P levels in wild-type mice and rats.
Brand:CaymanSKU:23289 - 1 mgAvailable on backorder
SLM6031434 is an inhibitor of sphingosine kinase 2 (SPHK2) (Ki = 0.4 μM for the recombinant mouse enzyme).{38413} It is selective for SPHK2 over SPHK1 (Kis = >20 μM). It decreases sphingosine-1-phosphate (S1P; Item No. 62570) and increases sphingosine levels in U937 monocytic leukemia cells in a concentration-dependent manner. SLM6031434 (5 mg/kg) reduces blood S1P levels in Sphk1-/-, but not Sphk2-/-, mice. SLM6031434 also increases blood S1P levels in wild-type mice and rats.
Brand:CaymanSKU:23289 - 10 mgAvailable on backorder
SLM6031434 is an inhibitor of sphingosine kinase 2 (SPHK2) (Ki = 0.4 μM for the recombinant mouse enzyme).{38413} It is selective for SPHK2 over SPHK1 (Kis = >20 μM). It decreases sphingosine-1-phosphate (S1P; Item No. 62570) and increases sphingosine levels in U937 monocytic leukemia cells in a concentration-dependent manner. SLM6031434 (5 mg/kg) reduces blood S1P levels in Sphk1-/-, but not Sphk2-/-, mice. SLM6031434 also increases blood S1P levels in wild-type mice and rats.
Brand:CaymanSKU:23289 - 25 mgAvailable on backorder
SLM6031434 is an inhibitor of sphingosine kinase 2 (SPHK2) (Ki = 0.4 μM for the recombinant mouse enzyme).{38413} It is selective for SPHK2 over SPHK1 (Kis = >20 μM). It decreases sphingosine-1-phosphate (S1P; Item No. 62570) and increases sphingosine levels in U937 monocytic leukemia cells in a concentration-dependent manner. SLM6031434 (5 mg/kg) reduces blood S1P levels in Sphk1-/-, but not Sphk2-/-, mice. SLM6031434 also increases blood S1P levels in wild-type mice and rats.
Brand:CaymanSKU:23289 - 5 mgAvailable on backorder
SLM6031434 is an inhibitor of sphingosine kinase 2 (SPHK2) (Ki = 0.4 μM for the recombinant mouse enzyme).{38413} It is selective for SPHK2 over SPHK1 (Kis = >20 μM). It decreases sphingosine-1-phosphate (S1P; Item No. 62570) and increases sphingosine levels in U937 monocytic leukemia cells in a concentration-dependent manner. SLM6031434 (5 mg/kg) reduces blood S1P levels in Sphk1-/-, but not Sphk2-/-, mice. SLM6031434 also increases blood S1P levels in wild-type mice and rats.
Brand:CaymanSKU:30434 - 10 mgAvailable on backorder
SLM6031434 is an inhibitor of sphingosine kinase 2 (SPHK2) (Ki = 0.4 μM for the recombinant mouse enzyme).{38413} It is selective for SPHK2 over SPHK1 (Kis = >20 μM). It decreases sphingosine-1-phosphate (S1P; Item No. 62570) and increases sphingosine levels in U937 monocytic leukemia cells in a concentration-dependent manner. SLM6031434 (5 mg/kg) reduces blood S1P levels in Sphk1-/-, but not Sphk2-/-, mice. SLM6031434 also increases blood S1P levels in wild-type mice and rats.
Brand:CaymanSKU:30434 - 25 mgAvailable on backorder
SLM6031434 is an inhibitor of sphingosine kinase 2 (SPHK2) (Ki = 0.4 μM for the recombinant mouse enzyme).{38413} It is selective for SPHK2 over SPHK1 (Kis = >20 μM). It decreases sphingosine-1-phosphate (S1P; Item No. 62570) and increases sphingosine levels in U937 monocytic leukemia cells in a concentration-dependent manner. SLM6031434 (5 mg/kg) reduces blood S1P levels in Sphk1-/-, but not Sphk2-/-, mice. SLM6031434 also increases blood S1P levels in wild-type mice and rats.
Brand:CaymanSKU:30434 - 5 mgAvailable on backorder
SLM6031434 is an inhibitor of sphingosine kinase 2 (SPHK2) (Ki = 0.4 μM for the recombinant mouse enzyme).{38413} It is selective for SPHK2 over SPHK1 (Kis = >20 μM). It decreases sphingosine-1-phosphate (S1P; Item No. 62570) and increases sphingosine levels in U937 monocytic leukemia cells in a concentration-dependent manner. SLM6031434 (5 mg/kg) reduces blood S1P levels in Sphk1-/-, but not Sphk2-/-, mice. SLM6031434 also increases blood S1P levels in wild-type mice and rats.
Brand:CaymanSKU:30434 - 50 mgAvailable on backorder