Cayman
Showing 10351–10500 of 45550 results
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Most local anesthetics act by abolishing voltage-gated sodium channel currents indiscriminately in all populations of neurons. Articaine is an amide local anesthetic most commonly used in dentistry.{29049} It possesses a unique ester side chain that is metabolized rapidly by circulating esterases.{29050} Articaine is reported to modify cardiac action potentials and ion currents only at concentrations higher than the therapeutic range needed to inhibit voltage-gated sodium channels.{29050}
Brand:CaymanSKU:-Available on backorder
Most local anesthetics act by abolishing voltage-gated sodium channel currents indiscriminately in all populations of neurons. Articaine is an amide local anesthetic most commonly used in dentistry.{29049} It possesses a unique ester side chain that is metabolized rapidly by circulating esterases.{29050} Articaine is reported to modify cardiac action potentials and ion currents only at concentrations higher than the therapeutic range needed to inhibit voltage-gated sodium channels.{29050}
Brand:CaymanSKU:-Available on backorder
Arundic acid is an inhibitor of astrocyte activation.{53333} It reduces increases in brain glial fibrillary acid protein (GFAP) and S100β levels, markers of astrocyte activation, in a rat model of permanent focal ischemia induced by middle cerebral artery occlusion when administered at a dose of 10 mg/kg. Arundic acid (3 and 10 mg/kg) decreases the number of TUNEL-positive neurons, reduces infarct size, and improves motor performance in the rotarod test in the same model. It also reduces descent time and time to turn in a pole test, indicating reversal of motor deficits, in a mouse model of MPTP-induced Parkinson’s disease when administered at a dose of 30 mg/kg.{53334}
Brand:CaymanSKU:29087 - 1 mgAvailable on backorder
Arundic acid is an inhibitor of astrocyte activation.{53333} It reduces increases in brain glial fibrillary acid protein (GFAP) and S100β levels, markers of astrocyte activation, in a rat model of permanent focal ischemia induced by middle cerebral artery occlusion when administered at a dose of 10 mg/kg. Arundic acid (3 and 10 mg/kg) decreases the number of TUNEL-positive neurons, reduces infarct size, and improves motor performance in the rotarod test in the same model. It also reduces descent time and time to turn in a pole test, indicating reversal of motor deficits, in a mouse model of MPTP-induced Parkinson’s disease when administered at a dose of 30 mg/kg.{53334}
Brand:CaymanSKU:29087 - 10 mgAvailable on backorder
Arundic acid is an inhibitor of astrocyte activation.{53333} It reduces increases in brain glial fibrillary acid protein (GFAP) and S100β levels, markers of astrocyte activation, in a rat model of permanent focal ischemia induced by middle cerebral artery occlusion when administered at a dose of 10 mg/kg. Arundic acid (3 and 10 mg/kg) decreases the number of TUNEL-positive neurons, reduces infarct size, and improves motor performance in the rotarod test in the same model. It also reduces descent time and time to turn in a pole test, indicating reversal of motor deficits, in a mouse model of MPTP-induced Parkinson’s disease when administered at a dose of 30 mg/kg.{53334}
Brand:CaymanSKU:29087 - 25 mgAvailable on backorder
Arundic acid is an inhibitor of astrocyte activation.{53333} It reduces increases in brain glial fibrillary acid protein (GFAP) and S100β levels, markers of astrocyte activation, in a rat model of permanent focal ischemia induced by middle cerebral artery occlusion when administered at a dose of 10 mg/kg. Arundic acid (3 and 10 mg/kg) decreases the number of TUNEL-positive neurons, reduces infarct size, and improves motor performance in the rotarod test in the same model. It also reduces descent time and time to turn in a pole test, indicating reversal of motor deficits, in a mouse model of MPTP-induced Parkinson’s disease when administered at a dose of 30 mg/kg.{53334}
Brand:CaymanSKU:29087 - 5 mgAvailable on backorder
ARV-771 is a proteolysis-targeting chimera (PROTAC) that drives the degradation of bromodomain and extra terminal domain (BET) family proteins.{33349} It is comprised of a BET-binding moiety conjugated via a linker to a von Hippel-Lindau (VHL) E3 ligase-binding moiety. ARV-771 induces degradation of bromodomain-containing protein 2 (BRD2), BRD3, and BRD4 in 22Rv1 castration-resistant prostate cancer (CRPC) cells with half-maximal degradation (DC50) values of less than 5 nM for all. It inhibits proliferation of and increases poly(ADP-ribose) polymerase (PARP) cleavage in 22Rv1 cells in a concentration-dependent manner. ARV-771 reduces full-length androgen receptor protein levels and prevents increases in ERG induced by the synthetic androgen R1881 in VCaP cells in a concentration-dependent manner. ARV-771 (30 mg/kg per day, s.c.) induces tumor regression in a 22Rv1 mouse xenograft model.
Brand:CaymanSKU:21299 -Out of stock
ARV-771 is a proteolysis-targeting chimera (PROTAC) that drives the degradation of bromodomain and extra terminal domain (BET) family proteins.{33349} It is comprised of a BET-binding moiety conjugated via a linker to a von Hippel-Lindau (VHL) E3 ligase-binding moiety. ARV-771 induces degradation of bromodomain-containing protein 2 (BRD2), BRD3, and BRD4 in 22Rv1 castration-resistant prostate cancer (CRPC) cells with half-maximal degradation (DC50) values of less than 5 nM for all. It inhibits proliferation of and increases poly(ADP-ribose) polymerase (PARP) cleavage in 22Rv1 cells in a concentration-dependent manner. ARV-771 reduces full-length androgen receptor protein levels and prevents increases in ERG induced by the synthetic androgen R1881 in VCaP cells in a concentration-dependent manner. ARV-771 (30 mg/kg per day, s.c.) induces tumor regression in a 22Rv1 mouse xenograft model.
Brand:CaymanSKU:21299 -Out of stock
ARV-771 is a proteolysis-targeting chimera (PROTAC) that drives the degradation of bromodomain and extra terminal domain (BET) family proteins.{33349} It is comprised of a BET-binding moiety conjugated via a linker to a von Hippel-Lindau (VHL) E3 ligase-binding moiety. ARV-771 induces degradation of bromodomain-containing protein 2 (BRD2), BRD3, and BRD4 in 22Rv1 castration-resistant prostate cancer (CRPC) cells with half-maximal degradation (DC50) values of less than 5 nM for all. It inhibits proliferation of and increases poly(ADP-ribose) polymerase (PARP) cleavage in 22Rv1 cells in a concentration-dependent manner. ARV-771 reduces full-length androgen receptor protein levels and prevents increases in ERG induced by the synthetic androgen R1881 in VCaP cells in a concentration-dependent manner. ARV-771 (30 mg/kg per day, s.c.) induces tumor regression in a 22Rv1 mouse xenograft model.
Brand:CaymanSKU:21299 -Out of stock
ARV-825 is a hetero-bifunctional molecule that is composed of a BRD4 binding moiety joined to an E3 ligase cereblon binding moiety using proteolysis targeting chimera (PROTAC) technology.{32899} ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of BRD4 by the proteasome (50% maximum degradation at 14643), a competitor for binding to cereblon.{32966}
Brand:CaymanSKU:21109 -Out of stock
ARV-825 is a hetero-bifunctional molecule that is composed of a BRD4 binding moiety joined to an E3 ligase cereblon binding moiety using proteolysis targeting chimera (PROTAC) technology.{32899} ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of BRD4 by the proteasome (50% maximum degradation at 14643), a competitor for binding to cereblon.{32966}
Brand:CaymanSKU:21109 -Out of stock
ARV-825 is a hetero-bifunctional molecule that is composed of a BRD4 binding moiety joined to an E3 ligase cereblon binding moiety using proteolysis targeting chimera (PROTAC) technology.{32899} ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of BRD4 by the proteasome (50% maximum degradation at 14643), a competitor for binding to cereblon.{32966}
Brand:CaymanSKU:21109 -Out of stock
Arvanil is a structural analog of capsaicin, which is the noxious active component of hot peppers of the Capsicum family. It is the amide of vanillylamine and arachidonic acid. Arvanil induces analgesia in rat and mouse models of pain.{7203} Arvanil has complex interactions with the cannabinoid system, in that it potentiates the agonist activity of endogenous cannabinoids by inhibiting the reuptake of arachidonoyl ethanolamide (AEA). It is an agonist at CB1 (Ki values of 0.25 to 0.52 μM), but not CB2, receptors, and is resistant to hydrolysis by FAAH.{7209} The vasodilator, analgesic, and anti-inflammatory properties of arvanil are not clearly explained by its interactions with cannabinoid and vanilloid receptors, suggesting other possible sites of action.
Brand:CaymanSKU:90052 - 10 mgAvailable on backorder
Arvanil is a structural analog of capsaicin, which is the noxious active component of hot peppers of the Capsicum family. It is the amide of vanillylamine and arachidonic acid. Arvanil induces analgesia in rat and mouse models of pain.{7203} Arvanil has complex interactions with the cannabinoid system, in that it potentiates the agonist activity of endogenous cannabinoids by inhibiting the reuptake of arachidonoyl ethanolamide (AEA). It is an agonist at CB1 (Ki values of 0.25 to 0.52 μM), but not CB2, receptors, and is resistant to hydrolysis by FAAH.{7209} The vasodilator, analgesic, and anti-inflammatory properties of arvanil are not clearly explained by its interactions with cannabinoid and vanilloid receptors, suggesting other possible sites of action.
Brand:CaymanSKU:90052 - 100 mgAvailable on backorder
Arvanil is a structural analog of capsaicin, which is the noxious active component of hot peppers of the Capsicum family. It is the amide of vanillylamine and arachidonic acid. Arvanil induces analgesia in rat and mouse models of pain.{7203} Arvanil has complex interactions with the cannabinoid system, in that it potentiates the agonist activity of endogenous cannabinoids by inhibiting the reuptake of arachidonoyl ethanolamide (AEA). It is an agonist at CB1 (Ki values of 0.25 to 0.52 μM), but not CB2, receptors, and is resistant to hydrolysis by FAAH.{7209} The vasodilator, analgesic, and anti-inflammatory properties of arvanil are not clearly explained by its interactions with cannabinoid and vanilloid receptors, suggesting other possible sites of action.
Brand:CaymanSKU:90052 - 5 mgAvailable on backorder
Arvanil is a structural analog of capsaicin, which is the noxious active component of hot peppers of the Capsicum family. It is the amide of vanillylamine and arachidonic acid. Arvanil induces analgesia in rat and mouse models of pain.{7203} Arvanil has complex interactions with the cannabinoid system, in that it potentiates the agonist activity of endogenous cannabinoids by inhibiting the reuptake of arachidonoyl ethanolamide (AEA). It is an agonist at CB1 (Ki values of 0.25 to 0.52 μM), but not CB2, receptors, and is resistant to hydrolysis by FAAH.{7209} The vasodilator, analgesic, and anti-inflammatory properties of arvanil are not clearly explained by its interactions with cannabinoid and vanilloid receptors, suggesting other possible sites of action.
Brand:CaymanSKU:90052 - 50 mgAvailable on backorder
Arylquin 1 is a prostate apoptosis response-4 (Par-4) secretagogue.{27360} It binds to vimentin to displace Par-4 for secretion. Arylquin 1 induces Par-4 secretion from mouse embryonic fibroblasts (MEFs) and prostate cancer cells in vitro, effects that can be blocked by the inhibitor of vesicular transport brefeldin A (Item No. 11861). Arylquin 1 induces paracrine apoptosis of H1299, HOP92, and H460 cancer cells when co-cultured with Par-4+/+, but not Par-4-/-, MEFs.
Brand:CaymanSKU:-Out of stock
Arylquin 1 is a prostate apoptosis response-4 (Par-4) secretagogue.{27360} It binds to vimentin to displace Par-4 for secretion. Arylquin 1 induces Par-4 secretion from mouse embryonic fibroblasts (MEFs) and prostate cancer cells in vitro, effects that can be blocked by the inhibitor of vesicular transport brefeldin A (Item No. 11861). Arylquin 1 induces paracrine apoptosis of H1299, HOP92, and H460 cancer cells when co-cultured with Par-4+/+, but not Par-4-/-, MEFs.
Brand:CaymanSKU:-Out of stock
Arylquin 1 is a prostate apoptosis response-4 (Par-4) secretagogue.{27360} It binds to vimentin to displace Par-4 for secretion. Arylquin 1 induces Par-4 secretion from mouse embryonic fibroblasts (MEFs) and prostate cancer cells in vitro, effects that can be blocked by the inhibitor of vesicular transport brefeldin A (Item No. 11861). Arylquin 1 induces paracrine apoptosis of H1299, HOP92, and H460 cancer cells when co-cultured with Par-4+/+, but not Par-4-/-, MEFs.
Brand:CaymanSKU:-Out of stock
The phosphatidylinositol 3-kinases (PI3Ks) are lipid and protein kinases involved in diverse biological processes, including cell growth, migration, and metabolism.{17822} AS-041164 is a potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC50 = 70 nM), compared to PI3Kα (IC50 = 240 nM), PI3Kβ (IC50 = 1.45 μM), and PI3Kδ (IC50 =1.70 μM).{17823} When tested at 1.0 μM, it shows little or no activity against 38 other common kinases.{17823} When given orally to mice, AS-041164 shows a pharmacokinetic profile that is similar to the general PI3K inhibitor LY294002 but is three times more potent (ED50 = 27.4 mg/kg for AS-041164 versus 81.6 mg/kg for LY294002) in blocking neutrophil recruitment induced by RANTES.{17823}
Brand:CaymanSKU:- The phosphatidylinositol 3-kinases (PI3Ks) are lipid and protein kinases involved in diverse biological processes, including cell growth, migration, and metabolism.{17822} AS-041164 is a potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC50 = 70 nM), compared to PI3Kα (IC50 = 240 nM), PI3Kβ (IC50 = 1.45 μM), and PI3Kδ (IC50 =1.70 μM).{17823} When tested at 1.0 μM, it shows little or no activity against 38 other common kinases.{17823} When given orally to mice, AS-041164 shows a pharmacokinetic profile that is similar to the general PI3K inhibitor LY294002 but is three times more potent (ED50 = 27.4 mg/kg for AS-041164 versus 81.6 mg/kg for LY294002) in blocking neutrophil recruitment induced by RANTES.{17823}
Brand:CaymanSKU:- The phosphatidylinositol 3-kinases (PI3Ks) are lipid and protein kinases involved in diverse biological processes, including cell growth, migration, and metabolism.{17822} AS-041164 is a potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC50 = 70 nM), compared to PI3Kα (IC50 = 240 nM), PI3Kβ (IC50 = 1.45 μM), and PI3Kδ (IC50 =1.70 μM).{17823} When tested at 1.0 μM, it shows little or no activity against 38 other common kinases.{17823} When given orally to mice, AS-041164 shows a pharmacokinetic profile that is similar to the general PI3K inhibitor LY294002 but is three times more potent (ED50 = 27.4 mg/kg for AS-041164 versus 81.6 mg/kg for LY294002) in blocking neutrophil recruitment induced by RANTES.{17823}
Brand:CaymanSKU:- The phosphatidylinositol 3-kinases (PI3Ks) are lipid and protein kinases involved in diverse biological processes, including cell growth, migration, and metabolism.{17822} AS-041164 is a potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC50 = 70 nM), compared to PI3Kα (IC50 = 240 nM), PI3Kβ (IC50 = 1.45 μM), and PI3Kδ (IC50 =1.70 μM).{17823} When tested at 1.0 μM, it shows little or no activity against 38 other common kinases.{17823} When given orally to mice, AS-041164 shows a pharmacokinetic profile that is similar to the general PI3K inhibitor LY294002 but is three times more potent (ED50 = 27.4 mg/kg for AS-041164 versus 81.6 mg/kg for LY294002) in blocking neutrophil recruitment induced by RANTES.{17823}
Brand:CaymanSKU:-
AS-101 is an immunomodulator.{36943} It inhibits IL-10 secretion from and cell proliferation of IL-10-secreting human stomach adenocarcinoma and glioblastoma multiforme (GBM) cells when used at concentrations ranging from 0.5 to 2.5 µg/ml, an effect that can be blocked by the addition of recombinant IL-10. It reverses IL-10-induced increases in phosphorylated Stat3 and reduces the expression of Bcl-2 in B16 murine melanoma cells. AS-101 sensitizes GBM cells to paclitaxel (Item No. 10461), doxorubicin (Item No. 15007), and 5-fluorouracil (5-FU; Item No. 14416) in vitro and to paclitaxel in a GBM mouse xenograft model when administered at a dose of 0.5 mg/kg per day. AS-101 (1 mg/kg) also prevents infiltration of CD49d+ cells and decreases the expression of IL-6, TNF-α, IL-1β, and MCP-1 in the spinal cord, as well as delays onset and slows the progression of symptoms in a mouse model of experimental autoimmune encephalomyelitis (EAE).{36944}
Brand:CaymanSKU:21443 -Out of stock
AS-101 is an immunomodulator.{36943} It inhibits IL-10 secretion from and cell proliferation of IL-10-secreting human stomach adenocarcinoma and glioblastoma multiforme (GBM) cells when used at concentrations ranging from 0.5 to 2.5 µg/ml, an effect that can be blocked by the addition of recombinant IL-10. It reverses IL-10-induced increases in phosphorylated Stat3 and reduces the expression of Bcl-2 in B16 murine melanoma cells. AS-101 sensitizes GBM cells to paclitaxel (Item No. 10461), doxorubicin (Item No. 15007), and 5-fluorouracil (5-FU; Item No. 14416) in vitro and to paclitaxel in a GBM mouse xenograft model when administered at a dose of 0.5 mg/kg per day. AS-101 (1 mg/kg) also prevents infiltration of CD49d+ cells and decreases the expression of IL-6, TNF-α, IL-1β, and MCP-1 in the spinal cord, as well as delays onset and slows the progression of symptoms in a mouse model of experimental autoimmune encephalomyelitis (EAE).{36944}
Brand:CaymanSKU:21443 -Out of stock
AS-101 is an immunomodulator.{36943} It inhibits IL-10 secretion from and cell proliferation of IL-10-secreting human stomach adenocarcinoma and glioblastoma multiforme (GBM) cells when used at concentrations ranging from 0.5 to 2.5 µg/ml, an effect that can be blocked by the addition of recombinant IL-10. It reverses IL-10-induced increases in phosphorylated Stat3 and reduces the expression of Bcl-2 in B16 murine melanoma cells. AS-101 sensitizes GBM cells to paclitaxel (Item No. 10461), doxorubicin (Item No. 15007), and 5-fluorouracil (5-FU; Item No. 14416) in vitro and to paclitaxel in a GBM mouse xenograft model when administered at a dose of 0.5 mg/kg per day. AS-101 (1 mg/kg) also prevents infiltration of CD49d+ cells and decreases the expression of IL-6, TNF-α, IL-1β, and MCP-1 in the spinal cord, as well as delays onset and slows the progression of symptoms in a mouse model of experimental autoimmune encephalomyelitis (EAE).{36944}
Brand:CaymanSKU:21443 -Out of stock
GPR119, a glucose-dependent insulinotropic receptor, is a Gs protein-coupled receptor that is expressed in pancreas β-cells and intestinal L-cells.{14046} Activation of GPR119 by the endogenous ligands lyso-phosphatidylcholine and oleoyl ethanolamide increases intracellular cAMP levels and promotes glucose-stimulated insulin secretion.{14046,18880} AS-1269574 is an agonist of GPR119 that is effective both in isolated cells and in vivo.{18583} It increases cAMP levels in HEK293 cells transfected with human GPR119 (EC50 = 2.5 μM) and glucose-stimulated insulin secretion in mice (100 mg/kg).{18583}
Brand:CaymanSKU:10626 - 1 mgAvailable on backorder
GPR119, a glucose-dependent insulinotropic receptor, is a Gs protein-coupled receptor that is expressed in pancreas β-cells and intestinal L-cells.{14046} Activation of GPR119 by the endogenous ligands lyso-phosphatidylcholine and oleoyl ethanolamide increases intracellular cAMP levels and promotes glucose-stimulated insulin secretion.{14046,18880} AS-1269574 is an agonist of GPR119 that is effective both in isolated cells and in vivo.{18583} It increases cAMP levels in HEK293 cells transfected with human GPR119 (EC50 = 2.5 μM) and glucose-stimulated insulin secretion in mice (100 mg/kg).{18583}
Brand:CaymanSKU:10626 - 10 mgAvailable on backorder
GPR119, a glucose-dependent insulinotropic receptor, is a Gs protein-coupled receptor that is expressed in pancreas β-cells and intestinal L-cells.{14046} Activation of GPR119 by the endogenous ligands lyso-phosphatidylcholine and oleoyl ethanolamide increases intracellular cAMP levels and promotes glucose-stimulated insulin secretion.{14046,18880} AS-1269574 is an agonist of GPR119 that is effective both in isolated cells and in vivo.{18583} It increases cAMP levels in HEK293 cells transfected with human GPR119 (EC50 = 2.5 μM) and glucose-stimulated insulin secretion in mice (100 mg/kg).{18583}
Brand:CaymanSKU:10626 - 25 mgAvailable on backorder
GPR119, a glucose-dependent insulinotropic receptor, is a Gs protein-coupled receptor that is expressed in pancreas β-cells and intestinal L-cells.{14046} Activation of GPR119 by the endogenous ligands lyso-phosphatidylcholine and oleoyl ethanolamide increases intracellular cAMP levels and promotes glucose-stimulated insulin secretion.{14046,18880} AS-1269574 is an agonist of GPR119 that is effective both in isolated cells and in vivo.{18583} It increases cAMP levels in HEK293 cells transfected with human GPR119 (EC50 = 2.5 μM) and glucose-stimulated insulin secretion in mice (100 mg/kg).{18583}
Brand:CaymanSKU:10626 - 5 mgAvailable on backorder
AS-1842856 is a potent inhibitor of forkhead box class O transcription factor 1 (FoxO1; IC50 = 33 nM in HepG2 cells).{37141} Inhibition of FoxO1-mediated transactivation with AS-1842856 leads to a dose-dependent decrease in expression of glucose-6 phosphatase (G6Pase) and phosphoenolpyruvate carboxykinase (PEPCK) mRNA and inhibits glucogenesis in rat hepatoma Fao cells and a murine model of type 2 diabetes mellitus (T2DM). AS-1842856 also inhibits 3T3-L1 preadipocyte differentiation and reduces lipid droplet growth in adipocytes.{37142},{37143}
Brand:CaymanSKU:-Out of stock
AS-1842856 is a potent inhibitor of forkhead box class O transcription factor 1 (FoxO1; IC50 = 33 nM in HepG2 cells).{37141} Inhibition of FoxO1-mediated transactivation with AS-1842856 leads to a dose-dependent decrease in expression of glucose-6 phosphatase (G6Pase) and phosphoenolpyruvate carboxykinase (PEPCK) mRNA and inhibits glucogenesis in rat hepatoma Fao cells and a murine model of type 2 diabetes mellitus (T2DM). AS-1842856 also inhibits 3T3-L1 preadipocyte differentiation and reduces lipid droplet growth in adipocytes.{37142},{37143}
Brand:CaymanSKU:-Out of stock
AS-1842856 is a potent inhibitor of forkhead box class O transcription factor 1 (FoxO1; IC50 = 33 nM in HepG2 cells).{37141} Inhibition of FoxO1-mediated transactivation with AS-1842856 leads to a dose-dependent decrease in expression of glucose-6 phosphatase (G6Pase) and phosphoenolpyruvate carboxykinase (PEPCK) mRNA and inhibits glucogenesis in rat hepatoma Fao cells and a murine model of type 2 diabetes mellitus (T2DM). AS-1842856 also inhibits 3T3-L1 preadipocyte differentiation and reduces lipid droplet growth in adipocytes.{37142},{37143}
Brand:CaymanSKU:-Out of stock
AS-1892802 is a potent inhibitor of Rho-associated serine-threonine protein kinases (ROCKs; IC50s = 122, 52, and 57 nM for human ROCK1, ROCK2, and rat ROCK2, respectively).{40426} It is selective for ROCK1 and 2 over a panel of 167 kinases and a panel of 63 ion channels, receptors, and enzymes at a concentration of 10 μM. However, AS-1892802 inhibits protein kinase catalytic subunit (PKACα) and protein kinase X gene (PRKX) with IC50 values of 200 and 325 nM, respectively. AS-1892802 reduces weight imbalance deficits (ED50 = 0.15 mg/kg) in rats in a monoiodoacetate-induced model of non-inflammatory arthritis. It also has analgesic-like effects in a rat model of diabetic neuropathy induced by streptozotocin (Item No. 13104) and reduces cartilage damage and weight imbalance deficits in a rat model of osteoarthritis.{40427,40428}
Brand:CaymanSKU:- AS-1892802 is a potent inhibitor of Rho-associated serine-threonine protein kinases (ROCKs; IC50s = 122, 52, and 57 nM for human ROCK1, ROCK2, and rat ROCK2, respectively).{40426} It is selective for ROCK1 and 2 over a panel of 167 kinases and a panel of 63 ion channels, receptors, and enzymes at a concentration of 10 μM. However, AS-1892802 inhibits protein kinase catalytic subunit (PKACα) and protein kinase X gene (PRKX) with IC50 values of 200 and 325 nM, respectively. AS-1892802 reduces weight imbalance deficits (ED50 = 0.15 mg/kg) in rats in a monoiodoacetate-induced model of non-inflammatory arthritis. It also has analgesic-like effects in a rat model of diabetic neuropathy induced by streptozotocin (Item No. 13104) and reduces cartilage damage and weight imbalance deficits in a rat model of osteoarthritis.{40427,40428}
Brand:CaymanSKU:- AS-1892802 is a potent inhibitor of Rho-associated serine-threonine protein kinases (ROCKs; IC50s = 122, 52, and 57 nM for human ROCK1, ROCK2, and rat ROCK2, respectively).{40426} It is selective for ROCK1 and 2 over a panel of 167 kinases and a panel of 63 ion channels, receptors, and enzymes at a concentration of 10 μM. However, AS-1892802 inhibits protein kinase catalytic subunit (PKACα) and protein kinase X gene (PRKX) with IC50 values of 200 and 325 nM, respectively. AS-1892802 reduces weight imbalance deficits (ED50 = 0.15 mg/kg) in rats in a monoiodoacetate-induced model of non-inflammatory arthritis. It also has analgesic-like effects in a rat model of diabetic neuropathy induced by streptozotocin (Item No. 13104) and reduces cartilage damage and weight imbalance deficits in a rat model of osteoarthritis.{40427,40428}
Brand:CaymanSKU:- AS-1892802 is a potent inhibitor of Rho-associated serine-threonine protein kinases (ROCKs; IC50s = 122, 52, and 57 nM for human ROCK1, ROCK2, and rat ROCK2, respectively).{40426} It is selective for ROCK1 and 2 over a panel of 167 kinases and a panel of 63 ion channels, receptors, and enzymes at a concentration of 10 μM. However, AS-1892802 inhibits protein kinase catalytic subunit (PKACα) and protein kinase X gene (PRKX) with IC50 values of 200 and 325 nM, respectively. AS-1892802 reduces weight imbalance deficits (ED50 = 0.15 mg/kg) in rats in a monoiodoacetate-induced model of non-inflammatory arthritis. It also has analgesic-like effects in a rat model of diabetic neuropathy induced by streptozotocin (Item No. 13104) and reduces cartilage damage and weight imbalance deficits in a rat model of osteoarthritis.{40427,40428}
Brand:CaymanSKU:-
AS-19 is an agonist of the serotonin (5-HT) receptor subtype 5-HT7 (Ki = 0.6 nM).{48277} It is selective for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis = 89.7, 490, 6.6 and 98.5 nM, respectively), as well as sigma-1 and imidazoline I2 receptors (Kis = 657 and 282 nM, respectively). AS-19 increases conditioned responses and reverses amnesia induced by the muscarinic acetylcholine receptor antagonist scopolamine in rats in an autoshaping learning task when administered post-training at a dose of 5 mg/kg.{48278} It increases the paw withdrawal threshold in a mechanical pressure test in rats with chronic constriction injury when 0.3 µl of a 1.5 nM solution is injected into the ventrolateral periaqueductal gray area (vlPAG), an effect that can be blocked by the 5-HT7 receptor antagonist SB-269970 (Item No. 17081).{48279}
Brand:CaymanSKU:20642 -Available on backorder
AS-19 is an agonist of the serotonin (5-HT) receptor subtype 5-HT7 (Ki = 0.6 nM).{48277} It is selective for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis = 89.7, 490, 6.6 and 98.5 nM, respectively), as well as sigma-1 and imidazoline I2 receptors (Kis = 657 and 282 nM, respectively). AS-19 increases conditioned responses and reverses amnesia induced by the muscarinic acetylcholine receptor antagonist scopolamine in rats in an autoshaping learning task when administered post-training at a dose of 5 mg/kg.{48278} It increases the paw withdrawal threshold in a mechanical pressure test in rats with chronic constriction injury when 0.3 µl of a 1.5 nM solution is injected into the ventrolateral periaqueductal gray area (vlPAG), an effect that can be blocked by the 5-HT7 receptor antagonist SB-269970 (Item No. 17081).{48279}
Brand:CaymanSKU:20642 -Available on backorder
AS-19 is an agonist of the serotonin (5-HT) receptor subtype 5-HT7 (Ki = 0.6 nM).{48277} It is selective for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis = 89.7, 490, 6.6 and 98.5 nM, respectively), as well as sigma-1 and imidazoline I2 receptors (Kis = 657 and 282 nM, respectively). AS-19 increases conditioned responses and reverses amnesia induced by the muscarinic acetylcholine receptor antagonist scopolamine in rats in an autoshaping learning task when administered post-training at a dose of 5 mg/kg.{48278} It increases the paw withdrawal threshold in a mechanical pressure test in rats with chronic constriction injury when 0.3 µl of a 1.5 nM solution is injected into the ventrolateral periaqueductal gray area (vlPAG), an effect that can be blocked by the 5-HT7 receptor antagonist SB-269970 (Item No. 17081).{48279}
Brand:CaymanSKU:20642 -Available on backorder
SH2 domain-containing inositol 5’-phosphatase 2 (SHIP2) negatively regulates the insulin signaling pathway by hydrolyzing phosphatidylinositol-3,4,5-trisphosphate.{22158} Its activity has been implicated in the pathogenesis of insulin resistance and type 2 diabetes.{12707} AS-1949490 is a small molecule inhibitor of SHIP2 (IC50s = 0.62 and 0.34 µM for human and mouse, respectively; Ki = 0.44 µM for hSHIP2).{28682} It is not as potent an inhibitor of SHIP1, demonstrating inhibitory values 30-fold higher than that of SHIP2, and shows little effect against the phosphatases PTEN, synaptojanin, and myotubularin (IC50s >50 µM).{28682} AS-1949490 has been shown to dose-dependently increase insulin-induced phosphorylation of Akt and to activate glucose metabolism.{28682} It has also been shown to suppress gluconeogenesis through reduced expression of PEPCK and G6Pase mRNA in normal mice and to decrease plasma glucose in diabetic db/db mice.{28682}
Brand:CaymanSKU:-Available on backorder
SH2 domain-containing inositol 5’-phosphatase 2 (SHIP2) negatively regulates the insulin signaling pathway by hydrolyzing phosphatidylinositol-3,4,5-trisphosphate.{22158} Its activity has been implicated in the pathogenesis of insulin resistance and type 2 diabetes.{12707} AS-1949490 is a small molecule inhibitor of SHIP2 (IC50s = 0.62 and 0.34 µM for human and mouse, respectively; Ki = 0.44 µM for hSHIP2).{28682} It is not as potent an inhibitor of SHIP1, demonstrating inhibitory values 30-fold higher than that of SHIP2, and shows little effect against the phosphatases PTEN, synaptojanin, and myotubularin (IC50s >50 µM).{28682} AS-1949490 has been shown to dose-dependently increase insulin-induced phosphorylation of Akt and to activate glucose metabolism.{28682} It has also been shown to suppress gluconeogenesis through reduced expression of PEPCK and G6Pase mRNA in normal mice and to decrease plasma glucose in diabetic db/db mice.{28682}
Brand:CaymanSKU:-Available on backorder
SH2 domain-containing inositol 5’-phosphatase 2 (SHIP2) negatively regulates the insulin signaling pathway by hydrolyzing phosphatidylinositol-3,4,5-trisphosphate.{22158} Its activity has been implicated in the pathogenesis of insulin resistance and type 2 diabetes.{12707} AS-1949490 is a small molecule inhibitor of SHIP2 (IC50s = 0.62 and 0.34 µM for human and mouse, respectively; Ki = 0.44 µM for hSHIP2).{28682} It is not as potent an inhibitor of SHIP1, demonstrating inhibitory values 30-fold higher than that of SHIP2, and shows little effect against the phosphatases PTEN, synaptojanin, and myotubularin (IC50s >50 µM).{28682} AS-1949490 has been shown to dose-dependently increase insulin-induced phosphorylation of Akt and to activate glucose metabolism.{28682} It has also been shown to suppress gluconeogenesis through reduced expression of PEPCK and G6Pase mRNA in normal mice and to decrease plasma glucose in diabetic db/db mice.{28682}
Brand:CaymanSKU:-Available on backorder
SH2 domain-containing inositol 5’-phosphatase 2 (SHIP2) negatively regulates the insulin signaling pathway by hydrolyzing phosphatidylinositol-3,4,5-trisphosphate.{22158} Its activity has been implicated in the pathogenesis of insulin resistance and type 2 diabetes.{12707} AS-1949490 is a small molecule inhibitor of SHIP2 (IC50s = 0.62 and 0.34 µM for human and mouse, respectively; Ki = 0.44 µM for hSHIP2).{28682} It is not as potent an inhibitor of SHIP1, demonstrating inhibitory values 30-fold higher than that of SHIP2, and shows little effect against the phosphatases PTEN, synaptojanin, and myotubularin (IC50s >50 µM).{28682} AS-1949490 has been shown to dose-dependently increase insulin-induced phosphorylation of Akt and to activate glucose metabolism.{28682} It has also been shown to suppress gluconeogenesis through reduced expression of PEPCK and G6Pase mRNA in normal mice and to decrease plasma glucose in diabetic db/db mice.{28682}
Brand:CaymanSKU:-Available on backorder
AS-2077715 is a fungal metabolite and an inhibitor of fungal mitochondrial complex III (cytochrome bc1; IC50 = 80 ng/ml for T. mentagrophytes complex III).{52421} It is selective for fungal over mammalian complex III (IC50s = 480 and 860 ng/ml for murine EL-4 cell and human Jurkat cell complex III, respectively). AS-2077715 inhibits ATP production in (IC50 = 0.33 µg/ml) and is fungicidal against T. mentagrophytes when used at concentrations of 1 and 10 µg/ml. In vivo, AS-2077715 (10 and 20 mg/kg) reduces the number of foot pad skin colony forming units (CFUs) in a guinea pig model of T. mentagrophytes infection.{52422}
Brand:CaymanSKU:29775 - 1 mgAvailable on backorder
AS-2444697 is an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4; IC50 = 21 nM).{52225} It is greater than 30-fold selective for IRAK4 over a panel of 146 kinases, but is less than 10-fold selective over PDGFRα, PDGFRβ, TrkA, TrkC, CLK1, Itk, and FLT3. AS-2444697 inhibits IL-1β-induced IL-6 production and LPS-induced TNF-α production in cellular assays (IC50s = 250 and 47 nM, respectively). It is efficacious in rat models of adjuvant- and collagen-induced arthritis (ED50s = 2.7 and 1.6 mg/kg, respectively). AS-2444697 (0.3-3 mg/kg, twice daily) reduces urinary protein excretion, the development of interstitial fibrosis and glomerulosclerosis, and renal mRNA expression of genes encoding IL-1β, IL-6, TNF-α, and chemokine (C-C motif) ligand 2 (CCL2) without affecting blood pressure in the 5/6 nephrectomized rat model of chronic kidney disease.{52226}
Brand:CaymanSKU:29505 - 1 mgAvailable on backorder
AS-2444697 is an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4; IC50 = 21 nM).{52225} It is greater than 30-fold selective for IRAK4 over a panel of 146 kinases, but is less than 10-fold selective over PDGFRα, PDGFRβ, TrkA, TrkC, CLK1, Itk, and FLT3. AS-2444697 inhibits IL-1β-induced IL-6 production and LPS-induced TNF-α production in cellular assays (IC50s = 250 and 47 nM, respectively). It is efficacious in rat models of adjuvant- and collagen-induced arthritis (ED50s = 2.7 and 1.6 mg/kg, respectively). AS-2444697 (0.3-3 mg/kg, twice daily) reduces urinary protein excretion, the development of interstitial fibrosis and glomerulosclerosis, and renal mRNA expression of genes encoding IL-1β, IL-6, TNF-α, and chemokine (C-C motif) ligand 2 (CCL2) without affecting blood pressure in the 5/6 nephrectomized rat model of chronic kidney disease.{52226}
Brand:CaymanSKU:29505 - 10 mgAvailable on backorder
AS-2444697 is an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4; IC50 = 21 nM).{52225} It is greater than 30-fold selective for IRAK4 over a panel of 146 kinases, but is less than 10-fold selective over PDGFRα, PDGFRβ, TrkA, TrkC, CLK1, Itk, and FLT3. AS-2444697 inhibits IL-1β-induced IL-6 production and LPS-induced TNF-α production in cellular assays (IC50s = 250 and 47 nM, respectively). It is efficacious in rat models of adjuvant- and collagen-induced arthritis (ED50s = 2.7 and 1.6 mg/kg, respectively). AS-2444697 (0.3-3 mg/kg, twice daily) reduces urinary protein excretion, the development of interstitial fibrosis and glomerulosclerosis, and renal mRNA expression of genes encoding IL-1β, IL-6, TNF-α, and chemokine (C-C motif) ligand 2 (CCL2) without affecting blood pressure in the 5/6 nephrectomized rat model of chronic kidney disease.{52226}
Brand:CaymanSKU:29505 - 5 mgAvailable on backorder
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of Pl at the 3 position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. {8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits. {14518} AS-252424 is a potent inhibitor of phosphatidylinositol-3-kinase PI3K with selectivity for the γ isoform. It inhibits human recombinant PI3Kγ, α, β, and δ with IC50 values of 30, 940, 20,000 and 20,000 nM, respectively. {14230} AS-252424 also inhibits C5a-mediated phosphorylation of Akt in RAW 264.7 macrophages with an IC50 value of 0.23 µM. In a murine model of peritonitis, AS-252424 inhibited neutrophil recruitment 35% at a dose of 10 mg/kg. {14230}
Brand:CaymanSKU:10009052 - 1 mgAvailable on backorder
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of Pl at the 3 position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. {8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits. {14518} AS-252424 is a potent inhibitor of phosphatidylinositol-3-kinase PI3K with selectivity for the γ isoform. It inhibits human recombinant PI3Kγ, α, β, and δ with IC50 values of 30, 940, 20,000 and 20,000 nM, respectively. {14230} AS-252424 also inhibits C5a-mediated phosphorylation of Akt in RAW 264.7 macrophages with an IC50 value of 0.23 µM. In a murine model of peritonitis, AS-252424 inhibited neutrophil recruitment 35% at a dose of 10 mg/kg. {14230}
Brand:CaymanSKU:10009052 - 10 mgAvailable on backorder
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of Pl at the 3 position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. {8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits. {14518} AS-252424 is a potent inhibitor of phosphatidylinositol-3-kinase PI3K with selectivity for the γ isoform. It inhibits human recombinant PI3Kγ, α, β, and δ with IC50 values of 30, 940, 20,000 and 20,000 nM, respectively. {14230} AS-252424 also inhibits C5a-mediated phosphorylation of Akt in RAW 264.7 macrophages with an IC50 value of 0.23 µM. In a murine model of peritonitis, AS-252424 inhibited neutrophil recruitment 35% at a dose of 10 mg/kg. {14230}
Brand:CaymanSKU:10009052 - 25 mgAvailable on backorder
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of Pl at the 3 position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. {8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits. {14518} AS-252424 is a potent inhibitor of phosphatidylinositol-3-kinase PI3K with selectivity for the γ isoform. It inhibits human recombinant PI3Kγ, α, β, and δ with IC50 values of 30, 940, 20,000 and 20,000 nM, respectively. {14230} AS-252424 also inhibits C5a-mediated phosphorylation of Akt in RAW 264.7 macrophages with an IC50 value of 0.23 µM. In a murine model of peritonitis, AS-252424 inhibited neutrophil recruitment 35% at a dose of 10 mg/kg. {14230}
Brand:CaymanSKU:10009052 - 5 mgAvailable on backorder
AS-2863619 is a dual inhibitor of cyclin-dependent kinase 8 (Cdk8) and Cdk19 (IC50s = 0.6 and 4.3 nM, respectively).{58029} It induces Foxp3 expression in isolated mouse naïve T cells when used at a concentration of 1 µM alone or synergistically in combination with TGF-β. AS-2863619 (30 mg/kg) decreases ear edema and induces production of Foxp3+ regulatory T cells (Tregs) in mice. It also reduces disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE).
Brand:CaymanSKU:30976 - 1 mgAvailable on backorder
AS-2863619 is a dual inhibitor of cyclin-dependent kinase 8 (Cdk8) and Cdk19 (IC50s = 0.6 and 4.3 nM, respectively).{58029} It induces Foxp3 expression in isolated mouse naïve T cells when used at a concentration of 1 µM alone or synergistically in combination with TGF-β. AS-2863619 (30 mg/kg) decreases ear edema and induces production of Foxp3+ regulatory T cells (Tregs) in mice. It also reduces disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE).
Brand:CaymanSKU:30976 - 5 mgAvailable on backorder
AS-2863619 is a dual inhibitor of cyclin-dependent kinase 8 (Cdk8) and Cdk19 (IC50s = 0.6 and 4.3 nM, respectively).{58029} It induces Foxp3 expression in isolated mouse naïve T cells when used at a concentration of 1 µM alone or synergistically in combination with TGF-β. AS-2863619 (30 mg/kg) decreases ear edema and induces production of Foxp3+ regulatory T cells (Tregs) in mice. It also reduces disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE).
Brand:CaymanSKU:30976 - 500 µgAvailable on backorder
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of PI at the three position of the inositol ring to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits.{14518} AS-604850 is a selective, ATP-competitive inhibitor of PI3Kγ with IC50 values of 0.25, >20, >20, and 4.5 µM for the human recombinant γ, δ, β, and α isoforms, respectively.{13338} AS-604850 inhibited MCP-1-mediated monocyte chemotaxis with an IC50 value of 21 µM and reduced RANTES-induced peritoneal neutrophil recruitment in a murine model of leukocyte chemotaxis with an ED50 value of 42.4 mg/kg.{13338}
Brand:CaymanSKU:10010175 - 1 mgAvailable on backorder
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of PI at the three position of the inositol ring to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits.{14518} AS-604850 is a selective, ATP-competitive inhibitor of PI3Kγ with IC50 values of 0.25, >20, >20, and 4.5 µM for the human recombinant γ, δ, β, and α isoforms, respectively.{13338} AS-604850 inhibited MCP-1-mediated monocyte chemotaxis with an IC50 value of 21 µM and reduced RANTES-induced peritoneal neutrophil recruitment in a murine model of leukocyte chemotaxis with an ED50 value of 42.4 mg/kg.{13338}
Brand:CaymanSKU:10010175 - 10 mgAvailable on backorder
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of PI at the three position of the inositol ring to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits.{14518} AS-604850 is a selective, ATP-competitive inhibitor of PI3Kγ with IC50 values of 0.25, >20, >20, and 4.5 µM for the human recombinant γ, δ, β, and α isoforms, respectively.{13338} AS-604850 inhibited MCP-1-mediated monocyte chemotaxis with an IC50 value of 21 µM and reduced RANTES-induced peritoneal neutrophil recruitment in a murine model of leukocyte chemotaxis with an ED50 value of 42.4 mg/kg.{13338}
Brand:CaymanSKU:10010175 - 25 mgAvailable on backorder
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of PI at the three position of the inositol ring to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits.{14518} AS-604850 is a selective, ATP-competitive inhibitor of PI3Kγ with IC50 values of 0.25, >20, >20, and 4.5 µM for the human recombinant γ, δ, β, and α isoforms, respectively.{13338} AS-604850 inhibited MCP-1-mediated monocyte chemotaxis with an IC50 value of 21 µM and reduced RANTES-induced peritoneal neutrophil recruitment in a murine model of leukocyte chemotaxis with an ED50 value of 42.4 mg/kg.{13338}
Brand:CaymanSKU:10010175 - 5 mgAvailable on backorder
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the three position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits{14518} AS-605240 is an orally active inhibitor of PI3-kinase γ that suppresses joint inflammation in mouse models of rheumatoid arthritis.{13338} It inhibits human recombinant PI3Kγ, α, β, and δ in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.{13338} AS-605240 inhibits C5a-mediated phosphorylation of protein kinase B in RAW 264 cells with an IC50 value of 90 nM. In vivo, AS-605240 reduced RANTES-induced peritoneal neutrophil recruitment in a mouse model of leukocyte chemotaxis with an ED50 value of 9.1 mg/kg.
Brand:CaymanSKU:10007707 - 1 mgAvailable on backorder
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the three position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits{14518} AS-605240 is an orally active inhibitor of PI3-kinase γ that suppresses joint inflammation in mouse models of rheumatoid arthritis.{13338} It inhibits human recombinant PI3Kγ, α, β, and δ in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.{13338} AS-605240 inhibits C5a-mediated phosphorylation of protein kinase B in RAW 264 cells with an IC50 value of 90 nM. In vivo, AS-605240 reduced RANTES-induced peritoneal neutrophil recruitment in a mouse model of leukocyte chemotaxis with an ED50 value of 9.1 mg/kg.
Brand:CaymanSKU:10007707 - 10 mgAvailable on backorder
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the three position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits{14518} AS-605240 is an orally active inhibitor of PI3-kinase γ that suppresses joint inflammation in mouse models of rheumatoid arthritis.{13338} It inhibits human recombinant PI3Kγ, α, β, and δ in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.{13338} AS-605240 inhibits C5a-mediated phosphorylation of protein kinase B in RAW 264 cells with an IC50 value of 90 nM. In vivo, AS-605240 reduced RANTES-induced peritoneal neutrophil recruitment in a mouse model of leukocyte chemotaxis with an ED50 value of 9.1 mg/kg.
Brand:CaymanSKU:10007707 - 25 mgAvailable on backorder
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the three position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits{14518} AS-605240 is an orally active inhibitor of PI3-kinase γ that suppresses joint inflammation in mouse models of rheumatoid arthritis.{13338} It inhibits human recombinant PI3Kγ, α, β, and δ in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.{13338} AS-605240 inhibits C5a-mediated phosphorylation of protein kinase B in RAW 264 cells with an IC50 value of 90 nM. In vivo, AS-605240 reduced RANTES-induced peritoneal neutrophil recruitment in a mouse model of leukocyte chemotaxis with an ED50 value of 9.1 mg/kg.
Brand:CaymanSKU:10007707 - 5 mgAvailable on backorder
The mitogen-activated protein kinases, MEK1 and 2, are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the Ras-Raf-MEK-ERK pathway and are often upregulated in a variety of cancer cell types.{15629} AS-703026 is an orally bioavailable small molecule that selectively binds to and inhibits MEK1/2, preventing the activation of downstream effector proteins and transcription factors. It potently inhibits growth and survival of human INA-6 multiple myeloma cells and cytokine-induced osteoclast differentiation with IC50 values of 10 and 18.2 nM, respectively.{20674} In mice bearing H929 MM xenograft tumors, 30 mg/kg AS-703026 reduced tumor growth significantly, which correlated with downregulated ERK1/2 activity, induced PARP cleavage, and decreased microvessels in vivo.{20674} At 10 μM, AS-703026 supressed proliferation and transformation of K-Ras mutated colorectal cancer cells resistant to EGFR antibody therapy.{20673}
Brand:CaymanSKU:11226 - 1 mgAvailable on backorder
The mitogen-activated protein kinases, MEK1 and 2, are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the Ras-Raf-MEK-ERK pathway and are often upregulated in a variety of cancer cell types.{15629} AS-703026 is an orally bioavailable small molecule that selectively binds to and inhibits MEK1/2, preventing the activation of downstream effector proteins and transcription factors. It potently inhibits growth and survival of human INA-6 multiple myeloma cells and cytokine-induced osteoclast differentiation with IC50 values of 10 and 18.2 nM, respectively.{20674} In mice bearing H929 MM xenograft tumors, 30 mg/kg AS-703026 reduced tumor growth significantly, which correlated with downregulated ERK1/2 activity, induced PARP cleavage, and decreased microvessels in vivo.{20674} At 10 μM, AS-703026 supressed proliferation and transformation of K-Ras mutated colorectal cancer cells resistant to EGFR antibody therapy.{20673}
Brand:CaymanSKU:11226 - 10 mgAvailable on backorder
The mitogen-activated protein kinases, MEK1 and 2, are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the Ras-Raf-MEK-ERK pathway and are often upregulated in a variety of cancer cell types.{15629} AS-703026 is an orally bioavailable small molecule that selectively binds to and inhibits MEK1/2, preventing the activation of downstream effector proteins and transcription factors. It potently inhibits growth and survival of human INA-6 multiple myeloma cells and cytokine-induced osteoclast differentiation with IC50 values of 10 and 18.2 nM, respectively.{20674} In mice bearing H929 MM xenograft tumors, 30 mg/kg AS-703026 reduced tumor growth significantly, which correlated with downregulated ERK1/2 activity, induced PARP cleavage, and decreased microvessels in vivo.{20674} At 10 μM, AS-703026 supressed proliferation and transformation of K-Ras mutated colorectal cancer cells resistant to EGFR antibody therapy.{20673}
Brand:CaymanSKU:11226 - 25 mgAvailable on backorder
The mitogen-activated protein kinases, MEK1 and 2, are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the Ras-Raf-MEK-ERK pathway and are often upregulated in a variety of cancer cell types.{15629} AS-703026 is an orally bioavailable small molecule that selectively binds to and inhibits MEK1/2, preventing the activation of downstream effector proteins and transcription factors. It potently inhibits growth and survival of human INA-6 multiple myeloma cells and cytokine-induced osteoclast differentiation with IC50 values of 10 and 18.2 nM, respectively.{20674} In mice bearing H929 MM xenograft tumors, 30 mg/kg AS-703026 reduced tumor growth significantly, which correlated with downregulated ERK1/2 activity, induced PARP cleavage, and decreased microvessels in vivo.{20674} At 10 μM, AS-703026 supressed proliferation and transformation of K-Ras mutated colorectal cancer cells resistant to EGFR antibody therapy.{20673}
Brand:CaymanSKU:11226 - 5 mgAvailable on backorder
AS-8351 is a histone demethylase inhibitor. It has been used in combination with CHIR99021 (Item No. 13122), A 83-01 (Item No. 9001799), BIX01294 (Item No. 13124), SC-1 (Item No. 10009557), Y-27632 (Item No. 10005583), OAC2 (Item No. 14103), SU 16f (Item No. 19555), and JNJ-10198409 (Item No. 10008131) to induce reprogramming of human fetal lung fibroblasts into functional cardiomyocytes.{31142}
Brand:CaymanSKU:20811 -Available on backorder
AS-8351 is a histone demethylase inhibitor. It has been used in combination with CHIR99021 (Item No. 13122), A 83-01 (Item No. 9001799), BIX01294 (Item No. 13124), SC-1 (Item No. 10009557), Y-27632 (Item No. 10005583), OAC2 (Item No. 14103), SU 16f (Item No. 19555), and JNJ-10198409 (Item No. 10008131) to induce reprogramming of human fetal lung fibroblasts into functional cardiomyocytes.{31142}
Brand:CaymanSKU:20811 -Available on backorder
AS-8351 is a histone demethylase inhibitor. It has been used in combination with CHIR99021 (Item No. 13122), A 83-01 (Item No. 9001799), BIX01294 (Item No. 13124), SC-1 (Item No. 10009557), Y-27632 (Item No. 10005583), OAC2 (Item No. 14103), SU 16f (Item No. 19555), and JNJ-10198409 (Item No. 10008131) to induce reprogramming of human fetal lung fibroblasts into functional cardiomyocytes.{31142}
Brand:CaymanSKU:20811 -Available on backorder
AS1517499 is a STAT6 inhibitor (IC50 = 21 nM in a reporter assay).{52065} It inhibits IL-4-induced Th2 differentiation (IC50 = 2.3 nM), but not IL-12-induced Th1 differentiation, of mouse spleen T cells. AS1517499 (10 mg/kg) inhibits bronchial smooth muscle hyperresponsiveness and IL-13 production in ovalbumin-sensitized mice when administered one hour prior to antigen exposure.{52067} It inhibits STAT6 phosphorylation and thyroid epithelial cell (TEC) hyperplasia and decreases serum levels of 3,3′,5-triiodo-L-thyronine (T3; Item No. 16028) and thyroxine (T4) in a mouse model of Graves’ disease when administered at a dose of 10 mg/kg per day.{52068} AS1517499 (20 mg/kg twice weekly) also inhibits tumor growth and liver metastasis in a murine orthotopic 4T1 mammary carcinoma model.{52066}
Brand:CaymanSKU:29071 - 1 mgAvailable on backorder
AS1517499 is a STAT6 inhibitor (IC50 = 21 nM in a reporter assay).{52065} It inhibits IL-4-induced Th2 differentiation (IC50 = 2.3 nM), but not IL-12-induced Th1 differentiation, of mouse spleen T cells. AS1517499 (10 mg/kg) inhibits bronchial smooth muscle hyperresponsiveness and IL-13 production in ovalbumin-sensitized mice when administered one hour prior to antigen exposure.{52067} It inhibits STAT6 phosphorylation and thyroid epithelial cell (TEC) hyperplasia and decreases serum levels of 3,3′,5-triiodo-L-thyronine (T3; Item No. 16028) and thyroxine (T4) in a mouse model of Graves’ disease when administered at a dose of 10 mg/kg per day.{52068} AS1517499 (20 mg/kg twice weekly) also inhibits tumor growth and liver metastasis in a murine orthotopic 4T1 mammary carcinoma model.{52066}
Brand:CaymanSKU:29071 - 10 mgAvailable on backorder
AS1517499 is a STAT6 inhibitor (IC50 = 21 nM in a reporter assay).{52065} It inhibits IL-4-induced Th2 differentiation (IC50 = 2.3 nM), but not IL-12-induced Th1 differentiation, of mouse spleen T cells. AS1517499 (10 mg/kg) inhibits bronchial smooth muscle hyperresponsiveness and IL-13 production in ovalbumin-sensitized mice when administered one hour prior to antigen exposure.{52067} It inhibits STAT6 phosphorylation and thyroid epithelial cell (TEC) hyperplasia and decreases serum levels of 3,3′,5-triiodo-L-thyronine (T3; Item No. 16028) and thyroxine (T4) in a mouse model of Graves’ disease when administered at a dose of 10 mg/kg per day.{52068} AS1517499 (20 mg/kg twice weekly) also inhibits tumor growth and liver metastasis in a murine orthotopic 4T1 mammary carcinoma model.{52066}
Brand:CaymanSKU:29071 - 25 mgAvailable on backorder
AS1517499 is a STAT6 inhibitor (IC50 = 21 nM in a reporter assay).{52065} It inhibits IL-4-induced Th2 differentiation (IC50 = 2.3 nM), but not IL-12-induced Th1 differentiation, of mouse spleen T cells. AS1517499 (10 mg/kg) inhibits bronchial smooth muscle hyperresponsiveness and IL-13 production in ovalbumin-sensitized mice when administered one hour prior to antigen exposure.{52067} It inhibits STAT6 phosphorylation and thyroid epithelial cell (TEC) hyperplasia and decreases serum levels of 3,3′,5-triiodo-L-thyronine (T3; Item No. 16028) and thyroxine (T4) in a mouse model of Graves’ disease when administered at a dose of 10 mg/kg per day.{52068} AS1517499 (20 mg/kg twice weekly) also inhibits tumor growth and liver metastasis in a murine orthotopic 4T1 mammary carcinoma model.{52066}
Brand:CaymanSKU:29071 - 5 mgAvailable on backorder
Asapiprant is an antagonist of the prostaglandin D1 (PGD1) receptor (DP1; Ki = 0.44 nM).{50862} It is selective for DP1 over DP2, as well as the thromboxane A2 (TXA2), prostaglandin I2 (PGI2), and prostaglandin E1-4 (PGE1-4) receptors (Kis = >5,000, >4,800, >6,300, and 120->6,600 nM, respectively). Asapiprant (1 and 3 mg/kg) reduces PGD2-induced increases in nasal resistance in a guinea model of allergic rhinitis. It reduces nasal secretion, when administered at doses of 3 and 30 mg/kg, and antigen-induced cell infiltration in nasal lavage fluids, when administered at 3 and 10 mg/kg, in a guinea pig model of allergic rhinitis induced by ovalbumin. Asapiprant (10 mg/kg) also decreases airway hyperresponsiveness, inflammatory cell infiltration in bronchoalveolar lavage fluid (BALF), and mucin production in a rat model of ovalbumin-induced asthma.
Brand:CaymanSKU:30008 - 1 mgAvailable on backorder
Asapiprant is an antagonist of the prostaglandin D1 (PGD1) receptor (DP1; Ki = 0.44 nM).{50862} It is selective for DP1 over DP2, as well as the thromboxane A2 (TXA2), prostaglandin I2 (PGI2), and prostaglandin E1-4 (PGE1-4) receptors (Kis = >5,000, >4,800, >6,300, and 120->6,600 nM, respectively). Asapiprant (1 and 3 mg/kg) reduces PGD2-induced increases in nasal resistance in a guinea model of allergic rhinitis. It reduces nasal secretion, when administered at doses of 3 and 30 mg/kg, and antigen-induced cell infiltration in nasal lavage fluids, when administered at 3 and 10 mg/kg, in a guinea pig model of allergic rhinitis induced by ovalbumin. Asapiprant (10 mg/kg) also decreases airway hyperresponsiveness, inflammatory cell infiltration in bronchoalveolar lavage fluid (BALF), and mucin production in a rat model of ovalbumin-induced asthma.
Brand:CaymanSKU:30008 - 10 mgAvailable on backorder
Asapiprant is an antagonist of the prostaglandin D1 (PGD1) receptor (DP1; Ki = 0.44 nM).{50862} It is selective for DP1 over DP2, as well as the thromboxane A2 (TXA2), prostaglandin I2 (PGI2), and prostaglandin E1-4 (PGE1-4) receptors (Kis = >5,000, >4,800, >6,300, and 120->6,600 nM, respectively). Asapiprant (1 and 3 mg/kg) reduces PGD2-induced increases in nasal resistance in a guinea model of allergic rhinitis. It reduces nasal secretion, when administered at doses of 3 and 30 mg/kg, and antigen-induced cell infiltration in nasal lavage fluids, when administered at 3 and 10 mg/kg, in a guinea pig model of allergic rhinitis induced by ovalbumin. Asapiprant (10 mg/kg) also decreases airway hyperresponsiveness, inflammatory cell infiltration in bronchoalveolar lavage fluid (BALF), and mucin production in a rat model of ovalbumin-induced asthma.
Brand:CaymanSKU:30008 - 25 mgAvailable on backorder
Asapiprant is an antagonist of the prostaglandin D1 (PGD1) receptor (DP1; Ki = 0.44 nM).{50862} It is selective for DP1 over DP2, as well as the thromboxane A2 (TXA2), prostaglandin I2 (PGI2), and prostaglandin E1-4 (PGE1-4) receptors (Kis = >5,000, >4,800, >6,300, and 120->6,600 nM, respectively). Asapiprant (1 and 3 mg/kg) reduces PGD2-induced increases in nasal resistance in a guinea model of allergic rhinitis. It reduces nasal secretion, when administered at doses of 3 and 30 mg/kg, and antigen-induced cell infiltration in nasal lavage fluids, when administered at 3 and 10 mg/kg, in a guinea pig model of allergic rhinitis induced by ovalbumin. Asapiprant (10 mg/kg) also decreases airway hyperresponsiveness, inflammatory cell infiltration in bronchoalveolar lavage fluid (BALF), and mucin production in a rat model of ovalbumin-induced asthma.
Brand:CaymanSKU:30008 - 5 mgAvailable on backorder
Asarinin is a lignan that has been found in A. sieboldii.{51057} It is an epimer of sesamin (Item No. 70310) and a noncompetitive inhibitor of Δ5-desaturase (Ki = 0.28 mM).{51058} It is selective for Δ5-desaturase over Δ6- and Δ9-desaturase. Asarinin is cytotoxic to A2780 and SKOV3 ovarian cancer cells (IC50s = 38.45 and 60.87 µM, respectively) but not immortalized ovarian surface epithelial cells (IC50 = >200 µM).{51057} It induces apoptosis and activates caspase-3, -8, and -9 in A2780 and SKOV3 cells.
Brand:CaymanSKU:27456 - 1 mgAvailable on backorder
Asarinin is a lignan that has been found in A. sieboldii.{51057} It is an epimer of sesamin (Item No. 70310) and a noncompetitive inhibitor of Δ5-desaturase (Ki = 0.28 mM).{51058} It is selective for Δ5-desaturase over Δ6- and Δ9-desaturase. Asarinin is cytotoxic to A2780 and SKOV3 ovarian cancer cells (IC50s = 38.45 and 60.87 µM, respectively) but not immortalized ovarian surface epithelial cells (IC50 = >200 µM).{51057} It induces apoptosis and activates caspase-3, -8, and -9 in A2780 and SKOV3 cells.
Brand:CaymanSKU:27456 - 10 mgAvailable on backorder
Asarinin is a lignan that has been found in A. sieboldii.{51057} It is an epimer of sesamin (Item No. 70310) and a noncompetitive inhibitor of Δ5-desaturase (Ki = 0.28 mM).{51058} It is selective for Δ5-desaturase over Δ6- and Δ9-desaturase. Asarinin is cytotoxic to A2780 and SKOV3 ovarian cancer cells (IC50s = 38.45 and 60.87 µM, respectively) but not immortalized ovarian surface epithelial cells (IC50 = >200 µM).{51057} It induces apoptosis and activates caspase-3, -8, and -9 in A2780 and SKOV3 cells.
Brand:CaymanSKU:27456 - 25 mgAvailable on backorder