Cayman
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2-oxoglutarate (2OG) and other Fe(II)-dependent oxygenases are an important family of enzymes with roles in collagen biosynthesis, lipid metabolism, nucleic acid repair and modification, histone demethylation, and hypoxic sensing.{18346,20944,18060} Impaired 2OG oxygenase activity is linked to the cellular hypoxic response and various diseases including cancer.{20945} Iron-chelators, Co(II) ions, and 2OG analogues such as pyridine-2,4-dicarboxylate and N-oxalylglycine have been used as non-selective inhibitors of 2OG oxygenases.{18060,20945,20943} However, they require administration as pro-drug diester derivatives. IOX1 is a broad-spectrum inhibitor of 2OG oxygenases that does not require application in a pro-drug formulation. IOX1 inhibits JMJD2A, JMJD2E and the 2OG oxygenases PHF8, PHD2, and FIH with IC50 values of 1.7, 2.4, 13.3, 14.3, and 20.5 μM, respectively.{20945} IOX1 inhibits H3K9me3 demethylation by JMJD2A in HeLa cells with an IC50 value of 87 μM.{20945} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:11572 - 5 mgAvailable on backorder
2-oxoglutarate (2OG) and other Fe(II)-dependent oxygenases are an important family of enzymes with roles in collagen biosynthesis, lipid metabolism, nucleic acid repair and modification, histone demethylation, and hypoxic sensing.{18346,20944,18060} Impaired 2OG oxygenase activity is linked to the cellular hypoxic response and various diseases including cancer.{20945} Iron-chelators, Co(II) ions, and 2OG analogues such as pyridine-2,4-dicarboxylate and N-oxalylglycine have been used as non-selective inhibitors of 2OG oxygenases.{18060,20945,20943} However, they require administration as pro-drug diester derivatives. IOX1 is a broad-spectrum inhibitor of 2OG oxygenases that does not require application in a pro-drug formulation. IOX1 inhibits JMJD2A, JMJD2E and the 2OG oxygenases PHF8, PHD2, and FIH with IC50 values of 1.7, 2.4, 13.3, 14.3, and 20.5 μM, respectively.{20945} IOX1 inhibits H3K9me3 demethylation by JMJD2A in HeLa cells with an IC50 value of 87 μM.{20945} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:11572 - 50 mgAvailable on backorder
Hypoxia-inducible factor (HIF) is regulated by the hydroxylation of prolyl residues in oxygen-dependent degradation domains in the HIF-1α subunit, which mark it for degradation by the proteasome.{21056,21057} HIF prolyl hydroxylation is catalyzed by prolyl hydroxylase domain enzymes (PHD1, 2, and 3), members of the Fe(II) and 2-oxoglutarate (2OG) oxygenase family. They require dioxygen as a cosubstrate, thus acting as the hypoxia-sensing component of the HIF system. The activity of PHD is suppressed by hypoxia, increasing both the abundance and activity of the HIF transcriptional complex.{21056,21057} IOX2 potently inhibits PHD2 (IC50 = 21 nM) with over 100-fold selectivity compared to inhibition of JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH (IC50s > 100 μM).{21058} IOX2 is active in cells, inhibiting HIF-1α hydroxylation in RCC4 cells at 50 μM.{21058} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:11573 - 10 mgAvailable on backorder
Hypoxia-inducible factor (HIF) is regulated by the hydroxylation of prolyl residues in oxygen-dependent degradation domains in the HIF-1α subunit, which mark it for degradation by the proteasome.{21056,21057} HIF prolyl hydroxylation is catalyzed by prolyl hydroxylase domain enzymes (PHD1, 2, and 3), members of the Fe(II) and 2-oxoglutarate (2OG) oxygenase family. They require dioxygen as a cosubstrate, thus acting as the hypoxia-sensing component of the HIF system. The activity of PHD is suppressed by hypoxia, increasing both the abundance and activity of the HIF transcriptional complex.{21056,21057} IOX2 potently inhibits PHD2 (IC50 = 21 nM) with over 100-fold selectivity compared to inhibition of JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH (IC50s > 100 μM).{21058} IOX2 is active in cells, inhibiting HIF-1α hydroxylation in RCC4 cells at 50 μM.{21058} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:11573 - 25 mgAvailable on backorder
Hypoxia-inducible factor (HIF) is regulated by the hydroxylation of prolyl residues in oxygen-dependent degradation domains in the HIF-1α subunit, which mark it for degradation by the proteasome.{21056,21057} HIF prolyl hydroxylation is catalyzed by prolyl hydroxylase domain enzymes (PHD1, 2, and 3), members of the Fe(II) and 2-oxoglutarate (2OG) oxygenase family. They require dioxygen as a cosubstrate, thus acting as the hypoxia-sensing component of the HIF system. The activity of PHD is suppressed by hypoxia, increasing both the abundance and activity of the HIF transcriptional complex.{21056,21057} IOX2 potently inhibits PHD2 (IC50 = 21 nM) with over 100-fold selectivity compared to inhibition of JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH (IC50s > 100 μM).{21058} IOX2 is active in cells, inhibiting HIF-1α hydroxylation in RCC4 cells at 50 μM.{21058} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:11573 - 5 mgAvailable on backorder
Hypoxia-inducible factor (HIF) is regulated by the hydroxylation of prolyl residues in oxygen-dependent degradation domains in the HIF-1α subunit, which mark it for degradation by the proteasome.{21056,21057} HIF prolyl hydroxylation is catalyzed by prolyl hydroxylase domain enzymes (PHD1, 2, and 3), members of the Fe(II) and 2-oxoglutarate (2OG) oxygenase family. They require dioxygen as a cosubstrate, thus acting as the hypoxia-sensing component of the HIF system. The activity of PHD is suppressed by hypoxia, increasing both the abundance and activity of the HIF transcriptional complex.{21056,21057} IOX2 potently inhibits PHD2 (IC50 = 21 nM) with over 100-fold selectivity compared to inhibition of JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH (IC50s > 100 μM).{21058} IOX2 is active in cells, inhibiting HIF-1α hydroxylation in RCC4 cells at 50 μM.{21058} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:11573 - 50 mgAvailable on backorder
Hypoxia-inducible factors (HIFs) are regulated by the hydroxylation of prolyl residues in oxygen-dependent degradation domains, which leads to degradation by the proteasome.{21056,21057} HIF prolyl hydroxylation is catalyzed by prolyl hydroxylase domain enzymes (PHD1, 2, and 3), members of the Fe(II) and 2-oxoglutarate (2OG) oxygenase family. They require dioxygen as a co-substrate, thus acting as the hypoxia-sensing component of the HIF system. IOX4 is a potent inhibitor of PHD2 (IC50 = 1.6 nM).{29178} It displays >1,000-fold selectivity for PHD2 over other 2OG-dependent dioxygenases, including JMJD isoforms, FBXL11, JARID1C, BBOX1, FIH, and FTO. IOX4 is active in vivo, inhibiting prolyl hydroxylation and increasing HIF-1α levels in cells (IC50 values range from 5.6 to 11.7 µM) and inducing HIF-1α and HIF-2α expression in mice.{29178} The induction of HIF expression in mice occurs in the brain as well as in the liver, kidney, and heart, indicating that IOX4 penetrates the blood-brain barrier.{29178}
Brand:CaymanSKU:-Available on backorder
Hypoxia-inducible factors (HIFs) are regulated by the hydroxylation of prolyl residues in oxygen-dependent degradation domains, which leads to degradation by the proteasome.{21056,21057} HIF prolyl hydroxylation is catalyzed by prolyl hydroxylase domain enzymes (PHD1, 2, and 3), members of the Fe(II) and 2-oxoglutarate (2OG) oxygenase family. They require dioxygen as a co-substrate, thus acting as the hypoxia-sensing component of the HIF system. IOX4 is a potent inhibitor of PHD2 (IC50 = 1.6 nM).{29178} It displays >1,000-fold selectivity for PHD2 over other 2OG-dependent dioxygenases, including JMJD isoforms, FBXL11, JARID1C, BBOX1, FIH, and FTO. IOX4 is active in vivo, inhibiting prolyl hydroxylation and increasing HIF-1α levels in cells (IC50 values range from 5.6 to 11.7 µM) and inducing HIF-1α and HIF-2α expression in mice.{29178} The induction of HIF expression in mice occurs in the brain as well as in the liver, kidney, and heart, indicating that IOX4 penetrates the blood-brain barrier.{29178}
Brand:CaymanSKU:-Available on backorder
Hypoxia-inducible factors (HIFs) are regulated by the hydroxylation of prolyl residues in oxygen-dependent degradation domains, which leads to degradation by the proteasome.{21056,21057} HIF prolyl hydroxylation is catalyzed by prolyl hydroxylase domain enzymes (PHD1, 2, and 3), members of the Fe(II) and 2-oxoglutarate (2OG) oxygenase family. They require dioxygen as a co-substrate, thus acting as the hypoxia-sensing component of the HIF system. IOX4 is a potent inhibitor of PHD2 (IC50 = 1.6 nM).{29178} It displays >1,000-fold selectivity for PHD2 over other 2OG-dependent dioxygenases, including JMJD isoforms, FBXL11, JARID1C, BBOX1, FIH, and FTO. IOX4 is active in vivo, inhibiting prolyl hydroxylation and increasing HIF-1α levels in cells (IC50 values range from 5.6 to 11.7 µM) and inducing HIF-1α and HIF-2α expression in mice.{29178} The induction of HIF expression in mice occurs in the brain as well as in the liver, kidney, and heart, indicating that IOX4 penetrates the blood-brain barrier.{29178}
Brand:CaymanSKU:-Available on backorder
Hypoxia-inducible factors (HIFs) are regulated by the hydroxylation of prolyl residues in oxygen-dependent degradation domains, which leads to degradation by the proteasome.{21056,21057} HIF prolyl hydroxylation is catalyzed by prolyl hydroxylase domain enzymes (PHD1, 2, and 3), members of the Fe(II) and 2-oxoglutarate (2OG) oxygenase family. They require dioxygen as a co-substrate, thus acting as the hypoxia-sensing component of the HIF system. IOX4 is a potent inhibitor of PHD2 (IC50 = 1.6 nM).{29178} It displays >1,000-fold selectivity for PHD2 over other 2OG-dependent dioxygenases, including JMJD isoforms, FBXL11, JARID1C, BBOX1, FIH, and FTO. IOX4 is active in vivo, inhibiting prolyl hydroxylation and increasing HIF-1α levels in cells (IC50 values range from 5.6 to 11.7 µM) and inducing HIF-1α and HIF-2α expression in mice.{29178} The induction of HIF expression in mice occurs in the brain as well as in the liver, kidney, and heart, indicating that IOX4 penetrates the blood-brain barrier.{29178}
Brand:CaymanSKU:-Available on backorder
Immunogen: Synthetic peptide from the N-terminal region of human IP receptor • Host: Rabbit • Species Reactivity: (+) Human and mouse; other species not tested • Application: WB • The IP receptor is a GPCR that mediates the action of PGI2. It participates in signal transduction of the pain response, cardioprotection, and inflammation.
Brand:CaymanSKU:10005518- 1 eaAvailable on backorder
Immunogen: Synthetic peptide from the N-terminal region of human IP receptor • Host: Rabbit • Species Reactivity: (+) Human and mouse; other species not tested • Application: WB • The IP receptor is a GPCR that mediates the action of PGI2. It participates in signal transduction of the pain response, cardioprotection, and inflammation.
Brand:CaymanSKU:10005518- 1 ea Prostaglandin I2 (PGI2) is a potent vasorelaxant and inhibitor of human platelet aggregation.{4375} The PGI2 receptor (IP receptor) also participates in signal transduction of the pain response, cardioprotection, and inflammation.{9050,5018,9805,8508,5466} Cloning of the murine and human IP receptors revealed a significant amino-terminal truncation of the human IP receptor compared to the murine receptor.{3173,1614} Cayman Chemical’s IP receptor antibody detects a 67 kDa band on immunoblot. The predicted migration of the deglycosylated protein is 40 kDa and bands at either 67 or 40 kDa may be detected depending on the degree of post-translational modification of the sample.{11563}
Brand:CaymanSKU:10005518 - 1 eaAvailable on backorder
Immunogen: Peptide from the N-terminal region of mouse IP receptor • Host: Rabbit • Species Reactivity: (+) Human and Mouse; other species not tested • Application: WB
Brand:CaymanSKU:160070- 1 ea Prostaglandin I2 (PGI2) is a potent vasorelaxant and inhibitor of human platelet aggregation.{4375} Research of the PGI2 receptor (IP receptor) also demonstrates its participation in signal transduction of the pain response, cardioprotection, and inflammation.{9050,5018,9805,8508,5466} Cloning of the mouse and human IP receptors reveals a significant amino-terminal truncation of the human IP receptor compared to the mouse receptor.{3173,1614} Accordingly, this antibody is useful only for immunochemical analysis of mouse and rat samples. The IP receptor (mouse) polyclonal antibody detects a ~45 kDa band from several human cell lines. Additionally, a 67 kDa band may be observed from mouse neural tissues and platelets. The calculated molecular weight of the IP receptor (mouse) is 44 kDa based on the amino acid sequence.
Brand:CaymanSKU:160070 - 1 eaAvailable on backorder
Immunogen: Peptide from the N-terminal region of mouse IP receptor • Host: Rabbit • Species Reactivity: (+) Human and Mouse; other species not tested • Application: WB
Brand:CaymanSKU:160070- 1 eaAvailable on backorder
Immunogen: Human IP6K2 protein • Host: Mouse • Clone: 4F10 • Isotype: IgG2b • Species Reactivity: (+) Human • Applications: ICC and WB
Brand:CaymanSKU:10239- 1 ea Inositol hexakisphosphate kinase 2 (IP6K2) is a cytoplasmic kinase that catalyzes the conversion of IP6 to diphosphoinositol pentakisphosphate in the presence of ATP.{22131} IP6K2 functions as a proapoptotic protein kinase.{22130} IP6K2 binds to tumor necrosis factor receptor-associated factor 2 and inhibits NF-κB signaling.{22139} Heat Shock Protein 90 regulates apoptosis through a normal physiological interaction with IP6K2 by inhibiting its catalytic activity.{22128} Thus, IP6K2 is a potential target for cancer therapeutics development.{22128}
Brand:CaymanSKU:10239 - 1 eaAvailable on backorder
Immunogen: Human IP6K2 protein • Host: Mouse • Clone: 4F10 • Isotype: IgG2b • Species Reactivity: (+) Human • Applications: ICC and WB
Brand:CaymanSKU:10239- 1 eaAvailable on backorder
IP7e is a brain-penetrant activator of nuclear receptor related protein 1 (Nurr1/NR4A2) signaling (EC50 = 3.9 nM in a reporter assay).{46629} In vivo, IP7e (10 mg/kg) prevents spinal cord axonal loss and demyelination and decreases spinal cord macrophage and T cell infiltration in a mouse model of experimental autoimmune encephalomyelitis (EAE).{46630}
Brand:CaymanSKU:29726 - 1 mgAvailable on backorder
IP7e is a brain-penetrant activator of nuclear receptor related protein 1 (Nurr1/NR4A2) signaling (EC50 = 3.9 nM in a reporter assay).{46629} In vivo, IP7e (10 mg/kg) prevents spinal cord axonal loss and demyelination and decreases spinal cord macrophage and T cell infiltration in a mouse model of experimental autoimmune encephalomyelitis (EAE).{46630}
Brand:CaymanSKU:29726 - 5 mgAvailable on backorder
p21-activated kinase 1 (PAK1) is a member of a family non-receptor serine/threonine kinases that are vital to normal cell function. Binding of various upstream partners to PAK1 results in release of an autoinhibitory domain that blocks activity of the kinase domain.{23498} PAK1 expression and activity is upregulated in several human cancers and is a potential therapeutic target for cancer intervention.{23498} IPA-3 is a cell-permeable allosteric inhibitor of PAK1 that is non-competitive with respect to ATP binding (IC50 = 2.5 µM).{23497} It does not, however, inhibit the activity of PAK1 that has been pre-activated with Cdc42. IPA-3 binds covalently to the PAK1 regulatory domain (apparent Kd = 1.9 uM) and prevents binding to the upstream activator Cdc42.{23499}
Brand:CaymanSKU:- p21-activated kinase 1 (PAK1) is a member of a family non-receptor serine/threonine kinases that are vital to normal cell function. Binding of various upstream partners to PAK1 results in release of an autoinhibitory domain that blocks activity of the kinase domain.{23498} PAK1 expression and activity is upregulated in several human cancers and is a potential therapeutic target for cancer intervention.{23498} IPA-3 is a cell-permeable allosteric inhibitor of PAK1 that is non-competitive with respect to ATP binding (IC50 = 2.5 µM).{23497} It does not, however, inhibit the activity of PAK1 that has been pre-activated with Cdc42. IPA-3 binds covalently to the PAK1 regulatory domain (apparent Kd = 1.9 uM) and prevents binding to the upstream activator Cdc42.{23499}
Brand:CaymanSKU:- p21-activated kinase 1 (PAK1) is a member of a family non-receptor serine/threonine kinases that are vital to normal cell function. Binding of various upstream partners to PAK1 results in release of an autoinhibitory domain that blocks activity of the kinase domain.{23498} PAK1 expression and activity is upregulated in several human cancers and is a potential therapeutic target for cancer intervention.{23498} IPA-3 is a cell-permeable allosteric inhibitor of PAK1 that is non-competitive with respect to ATP binding (IC50 = 2.5 µM).{23497} It does not, however, inhibit the activity of PAK1 that has been pre-activated with Cdc42. IPA-3 binds covalently to the PAK1 regulatory domain (apparent Kd = 1.9 uM) and prevents binding to the upstream activator Cdc42.{23499}
Brand:CaymanSKU:- p21-activated kinase 1 (PAK1) is a member of a family non-receptor serine/threonine kinases that are vital to normal cell function. Binding of various upstream partners to PAK1 results in release of an autoinhibitory domain that blocks activity of the kinase domain.{23498} PAK1 expression and activity is upregulated in several human cancers and is a potential therapeutic target for cancer intervention.{23498} IPA-3 is a cell-permeable allosteric inhibitor of PAK1 that is non-competitive with respect to ATP binding (IC50 = 2.5 µM).{23497} It does not, however, inhibit the activity of PAK1 that has been pre-activated with Cdc42. IPA-3 binds covalently to the PAK1 regulatory domain (apparent Kd = 1.9 uM) and prevents binding to the upstream activator Cdc42.{23499}
Brand:CaymanSKU:-
The G protein-coupled receptors GPR109A and GPR109B are recognized to be receptors for hydroxy-carboxylic acid (HCA) metabolites, are abundant in adipocytes, and are relevant to atherosclerosis and dyslipidemia.{24565,24562} IPBT-5CA is a selective agonist of GPR109B (HCA3; EC50 = 400 nM).{24563} It displays no activity at GPR109A (HCA2).{24563} IBC-293 inhibits forskolin-stimulated cAMP release in Chinese hamster ovary cells stably expressing GPR109B (EC50 = 54 nM) but not in cells expressing GPR109A.{24564} This is accompanied by a rapid and transient increase in intracellular calcium and activation of ERK1/2 through a pertussis toxin-sensitive Gi signaling pathway.{24564}
Brand:CaymanSKU:- The G protein-coupled receptors GPR109A and GPR109B are recognized to be receptors for hydroxy-carboxylic acid (HCA) metabolites, are abundant in adipocytes, and are relevant to atherosclerosis and dyslipidemia.{24565,24562} IPBT-5CA is a selective agonist of GPR109B (HCA3; EC50 = 400 nM).{24563} It displays no activity at GPR109A (HCA2).{24563} IBC-293 inhibits forskolin-stimulated cAMP release in Chinese hamster ovary cells stably expressing GPR109B (EC50 = 54 nM) but not in cells expressing GPR109A.{24564} This is accompanied by a rapid and transient increase in intracellular calcium and activation of ERK1/2 through a pertussis toxin-sensitive Gi signaling pathway.{24564}
Brand:CaymanSKU:- The G protein-coupled receptors GPR109A and GPR109B are recognized to be receptors for hydroxy-carboxylic acid (HCA) metabolites, are abundant in adipocytes, and are relevant to atherosclerosis and dyslipidemia.{24565,24562} IPBT-5CA is a selective agonist of GPR109B (HCA3; EC50 = 400 nM).{24563} It displays no activity at GPR109A (HCA2).{24563} IBC-293 inhibits forskolin-stimulated cAMP release in Chinese hamster ovary cells stably expressing GPR109B (EC50 = 54 nM) but not in cells expressing GPR109A.{24564} This is accompanied by a rapid and transient increase in intracellular calcium and activation of ERK1/2 through a pertussis toxin-sensitive Gi signaling pathway.{24564}
Brand:CaymanSKU:- The G protein-coupled receptors GPR109A and GPR109B are recognized to be receptors for hydroxy-carboxylic acid (HCA) metabolites, are abundant in adipocytes, and are relevant to atherosclerosis and dyslipidemia.{24565,24562} IPBT-5CA is a selective agonist of GPR109B (HCA3; EC50 = 400 nM).{24563} It displays no activity at GPR109A (HCA2).{24563} IBC-293 inhibits forskolin-stimulated cAMP release in Chinese hamster ovary cells stably expressing GPR109B (EC50 = 54 nM) but not in cells expressing GPR109A.{24564} This is accompanied by a rapid and transient increase in intracellular calcium and activation of ERK1/2 through a pertussis toxin-sensitive Gi signaling pathway.{24564}
Brand:CaymanSKU:-![An agonist of muscarinic acetylcholine receptors; stimulates [35S]GTPγS binding CHO cell membranes expressing human M2 muscarinic receptors and cell membranes expressing M4 muscarinic receptors (EC50s = 2.12 and 8.47 nM](https://interpriseusa.com/wp-content/uploads/2021/06/27235.png)
Iperoxo is an agonist of muscarinic acetylcholine receptors.{48128,42728} It stimulates [35S]GTPγS binding to CHO cell membranes expressing human M2 muscarinic receptors and cell membranes expressing M4 muscarinic receptors (EC50s = 2.12 and 8.47 nM, respectively).{48128} Iperoxo induces M1-dependent inhibition of the twitch response in electrically-stimulated isolated rabbit vas deferens (pD2 = 9.87) and M3-mediated contraction of isolated guinea pig ileum (pD2 = 9.78).{42728} In vivo, iperoxo reduces formalin-induced paw licking and acetic acid-induced writhing in mice (ED50s = 0.004 and 0.001 mg/kg, respectively).{42729}
Brand:CaymanSKU:27235 - 1 mgAvailable on backorder
Iperoxo is an agonist of muscarinic acetylcholine receptors.{48128,42728} It stimulates [35S]GTPγS binding to CHO cell membranes expressing human M2 muscarinic receptors and cell membranes expressing M4 muscarinic receptors (EC50s = 2.12 and 8.47 nM, respectively).{48128} Iperoxo induces M1-dependent inhibition of the twitch response in electrically-stimulated isolated rabbit vas deferens (pD2 = 9.87) and M3-mediated contraction of isolated guinea pig ileum (pD2 = 9.78).{42728} In vivo, iperoxo reduces formalin-induced paw licking and acetic acid-induced writhing in mice (ED50s = 0.004 and 0.001 mg/kg, respectively).{42729}
Brand:CaymanSKU:27235 - 10 mgAvailable on backorder
Iperoxo is an agonist of muscarinic acetylcholine receptors.{48128,42728} It stimulates [35S]GTPγS binding to CHO cell membranes expressing human M2 muscarinic receptors and cell membranes expressing M4 muscarinic receptors (EC50s = 2.12 and 8.47 nM, respectively).{48128} Iperoxo induces M1-dependent inhibition of the twitch response in electrically-stimulated isolated rabbit vas deferens (pD2 = 9.87) and M3-mediated contraction of isolated guinea pig ileum (pD2 = 9.78).{42728} In vivo, iperoxo reduces formalin-induced paw licking and acetic acid-induced writhing in mice (ED50s = 0.004 and 0.001 mg/kg, respectively).{42729}
Brand:CaymanSKU:27235 - 5 mgAvailable on backorder
IPI-145 is a potent inhibitor of the phosphoinositide 3-kinase (PI3K) isoforms PI3Kγ and PI3Kδ (IC50s = 0.24 and 50 nM, respectively).{27763} It is orally bioavailable and selective.{27763} As PI3Kγ and PI3Kδ are preferentially expressed in immune cells, IPI-145 has profound effects in collagen-induced and adjuvant-induced arthritis, ovalbumin-induced asthma, and systemic lupus erythematosus animal models.{27763,27764} It also has potential applications in immunotherapy and in certain cancers.{27762,27761}
Brand:CaymanSKU:-Out of stock
IPI-145 is a potent inhibitor of the phosphoinositide 3-kinase (PI3K) isoforms PI3Kγ and PI3Kδ (IC50s = 0.24 and 50 nM, respectively).{27763} It is orally bioavailable and selective.{27763} As PI3Kγ and PI3Kδ are preferentially expressed in immune cells, IPI-145 has profound effects in collagen-induced and adjuvant-induced arthritis, ovalbumin-induced asthma, and systemic lupus erythematosus animal models.{27763,27764} It also has potential applications in immunotherapy and in certain cancers.{27762,27761}
Brand:CaymanSKU:-Out of stock
IPI-145 is a potent inhibitor of the phosphoinositide 3-kinase (PI3K) isoforms PI3Kγ and PI3Kδ (IC50s = 0.24 and 50 nM, respectively).{27763} It is orally bioavailable and selective.{27763} As PI3Kγ and PI3Kδ are preferentially expressed in immune cells, IPI-145 has profound effects in collagen-induced and adjuvant-induced arthritis, ovalbumin-induced asthma, and systemic lupus erythematosus animal models.{27763,27764} It also has potential applications in immunotherapy and in certain cancers.{27762,27761}
Brand:CaymanSKU:-Out of stock
IPI-145 is a potent inhibitor of the phosphoinositide 3-kinase (PI3K) isoforms PI3Kγ and PI3Kδ (IC50s = 0.24 and 50 nM, respectively).{27763} It is orally bioavailable and selective.{27763} As PI3Kγ and PI3Kδ are preferentially expressed in immune cells, IPI-145 has profound effects in collagen-induced and adjuvant-induced arthritis, ovalbumin-induced asthma, and systemic lupus erythematosus animal models.{27763,27764} It also has potential applications in immunotherapy and in certain cancers.{27762,27761}
Brand:CaymanSKU:-Out of stock
IPI-549 is an inhibitor of PI3Kγ (IC50s = 16, 3,200, 3,500, and >8,400 nM for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively).{42626} It is greater than 100-fold selective for PI3Kγ over a panel of 468 mutant and nonmutant protein and lipid kinases, including Class II PI3K isoforms, and a panel of 80 G protein-coupled receptors, ion channels, and transporters at 10 µM. It inhibits phosphorylation of AKT S473 in SKOV3, 786-0, RAW 264.7, and RAJI cells and inhibits migration of bone marrow-derived macrophages (BMDMs) (IC50 = 85 nM). IPI-549 sensitizes doxorubicin-resistant SW620/Ad300 cells to P-glycoprotein (P-gp) substrates, such as paclitaxel (IC50s = 710 and 6.7 nM for paclitaxel alone and in combination with IPI-549, respectively), and increases the level of intracellular paclitaxel in SW620/Ad300 cells.{42627} It also enhances the tumor growth reduction of paclitaxel (Item No. 10461) in an SW620/Ad300 mouse xenograft model when administered at a dose of 3 mg/kg in combination with paclitaxel.
Brand:CaymanSKU:26416 - 1 mgAvailable on backorder
IPI-549 is an inhibitor of PI3Kγ (IC50s = 16, 3,200, 3,500, and >8,400 nM for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively).{42626} It is greater than 100-fold selective for PI3Kγ over a panel of 468 mutant and nonmutant protein and lipid kinases, including Class II PI3K isoforms, and a panel of 80 G protein-coupled receptors, ion channels, and transporters at 10 µM. It inhibits phosphorylation of AKT S473 in SKOV3, 786-0, RAW 264.7, and RAJI cells and inhibits migration of bone marrow-derived macrophages (BMDMs) (IC50 = 85 nM). IPI-549 sensitizes doxorubicin-resistant SW620/Ad300 cells to P-glycoprotein (P-gp) substrates, such as paclitaxel (IC50s = 710 and 6.7 nM for paclitaxel alone and in combination with IPI-549, respectively), and increases the level of intracellular paclitaxel in SW620/Ad300 cells.{42627} It also enhances the tumor growth reduction of paclitaxel (Item No. 10461) in an SW620/Ad300 mouse xenograft model when administered at a dose of 3 mg/kg in combination with paclitaxel.
Brand:CaymanSKU:26416 - 10 mgAvailable on backorder
IPI-549 is an inhibitor of PI3Kγ (IC50s = 16, 3,200, 3,500, and >8,400 nM for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively).{42626} It is greater than 100-fold selective for PI3Kγ over a panel of 468 mutant and nonmutant protein and lipid kinases, including Class II PI3K isoforms, and a panel of 80 G protein-coupled receptors, ion channels, and transporters at 10 µM. It inhibits phosphorylation of AKT S473 in SKOV3, 786-0, RAW 264.7, and RAJI cells and inhibits migration of bone marrow-derived macrophages (BMDMs) (IC50 = 85 nM). IPI-549 sensitizes doxorubicin-resistant SW620/Ad300 cells to P-glycoprotein (P-gp) substrates, such as paclitaxel (IC50s = 710 and 6.7 nM for paclitaxel alone and in combination with IPI-549, respectively), and increases the level of intracellular paclitaxel in SW620/Ad300 cells.{42627} It also enhances the tumor growth reduction of paclitaxel (Item No. 10461) in an SW620/Ad300 mouse xenograft model when administered at a dose of 3 mg/kg in combination with paclitaxel.
Brand:CaymanSKU:26416 - 25 mgAvailable on backorder
IPI-549 is an inhibitor of PI3Kγ (IC50s = 16, 3,200, 3,500, and >8,400 nM for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively).{42626} It is greater than 100-fold selective for PI3Kγ over a panel of 468 mutant and nonmutant protein and lipid kinases, including Class II PI3K isoforms, and a panel of 80 G protein-coupled receptors, ion channels, and transporters at 10 µM. It inhibits phosphorylation of AKT S473 in SKOV3, 786-0, RAW 264.7, and RAJI cells and inhibits migration of bone marrow-derived macrophages (BMDMs) (IC50 = 85 nM). IPI-549 sensitizes doxorubicin-resistant SW620/Ad300 cells to P-glycoprotein (P-gp) substrates, such as paclitaxel (IC50s = 710 and 6.7 nM for paclitaxel alone and in combination with IPI-549, respectively), and increases the level of intracellular paclitaxel in SW620/Ad300 cells.{42627} It also enhances the tumor growth reduction of paclitaxel (Item No. 10461) in an SW620/Ad300 mouse xenograft model when administered at a dose of 3 mg/kg in combination with paclitaxel.
Brand:CaymanSKU:26416 - 5 mgAvailable on backorder
Immunogen: Synthetic peptide from an internal region of human iPLA2 (Type VI) • Host: Rabbit • Species Reactivity : (+) Human, bovine, hamster, mouse, and rat • Cross Reactivity: (+) Human, mouse, hamster, and rat iPLA2 • Application: WB
Brand:CaymanSKU:160507- 1 ea Calcium-independent phospholipase A2 (iPLA2) is one of the most recently characterized isoforms in the growing list of the phospholipase A2 enzyme family.{3941} iPLA2 has been purified or cloned from CHO cells and mouse P388D1 macrophage-like cells and is the major isoform of phospholipase A2 found in A-10 smooth muscle cells.{4234,4233,3508,1960,3924,2993} The enzyme has a molecular weight of about 80-85 kDa and is classified as a type VI PLA2.1-5 The enzyme from CHO cells is approximately 95% and 90% homologous to mouse and human iPLA2, respectively.{4234,4233}
Brand:CaymanSKU:160507 - 1 eaAvailable on backorder
Immunogen: Synthetic peptide from an internal region of human iPLA2 (Type VI) • Host: Rabbit • Species Reactivity : (+) Human, bovine, hamster, mouse, and rat • Cross Reactivity: (+) Human, mouse, hamster, and rat iPLA2 • Application: WB
Brand:CaymanSKU:160507- 1 eaAvailable on backorder
Ipragliflozin is a sodium-glucose cotransporter 2 (SGLT2) inhibitor (IC50 = 7.4 nM in CHO cells expressing the human cotransporter).{49504} It is selective for SGLT2 over SGLT1, SGLT3, SGLT4, SGLT5, and SGLT6 (IC50s = 1.9, 30.4, 15.9, 0.46, and 10.4 µM, respectively). Ipragliflozin (0.1-3 mg/kg) decreases plasma levels of insulin and glucose in an oral glucose tolerance test in a mouse model of diabetes induced by high-fat diet, streptozotocin (STZ; Item No. 13104), and nicotinamide (Item No. 11127).{49505} It decreases plasma and hepatic IL-6, TNF-α, chemokine (C-C motif) ligand 2 (CCL2), and C-reactive protein (CRP) levels in the same model when administered at a dose of 3 mg/kg per day for 28 days.
Brand:CaymanSKU:22287 -Out of stock
Ipragliflozin is a sodium-glucose cotransporter 2 (SGLT2) inhibitor (IC50 = 7.4 nM in CHO cells expressing the human cotransporter).{49504} It is selective for SGLT2 over SGLT1, SGLT3, SGLT4, SGLT5, and SGLT6 (IC50s = 1.9, 30.4, 15.9, 0.46, and 10.4 µM, respectively). Ipragliflozin (0.1-3 mg/kg) decreases plasma levels of insulin and glucose in an oral glucose tolerance test in a mouse model of diabetes induced by high-fat diet, streptozotocin (STZ; Item No. 13104), and nicotinamide (Item No. 11127).{49505} It decreases plasma and hepatic IL-6, TNF-α, chemokine (C-C motif) ligand 2 (CCL2), and C-reactive protein (CRP) levels in the same model when administered at a dose of 3 mg/kg per day for 28 days.
Brand:CaymanSKU:22287 -Out of stock
Ipragliflozin is a sodium-glucose cotransporter 2 (SGLT2) inhibitor (IC50 = 7.4 nM in CHO cells expressing the human cotransporter).{49504} It is selective for SGLT2 over SGLT1, SGLT3, SGLT4, SGLT5, and SGLT6 (IC50s = 1.9, 30.4, 15.9, 0.46, and 10.4 µM, respectively). Ipragliflozin (0.1-3 mg/kg) decreases plasma levels of insulin and glucose in an oral glucose tolerance test in a mouse model of diabetes induced by high-fat diet, streptozotocin (STZ; Item No. 13104), and nicotinamide (Item No. 11127).{49505} It decreases plasma and hepatic IL-6, TNF-α, chemokine (C-C motif) ligand 2 (CCL2), and C-reactive protein (CRP) levels in the same model when administered at a dose of 3 mg/kg per day for 28 days.
Brand:CaymanSKU:22287 -Out of stock
Ipragliflozin is a sodium-glucose cotransporter 2 (SGLT2) inhibitor (IC50 = 7.4 nM in CHO cells expressing the human cotransporter).{49504} It is selective for SGLT2 over SGLT1, SGLT3, SGLT4, SGLT5, and SGLT6 (IC50s = 1.9, 30.4, 15.9, 0.46, and 10.4 µM, respectively). Ipragliflozin (0.1-3 mg/kg) decreases plasma levels of insulin and glucose in an oral glucose tolerance test in a mouse model of diabetes induced by high-fat diet, streptozotocin (STZ; Item No. 13104), and nicotinamide (Item No. 11127).{49505} It decreases plasma and hepatic IL-6, TNF-α, chemokine (C-C motif) ligand 2 (CCL2), and C-reactive protein (CRP) levels in the same model when administered at a dose of 3 mg/kg per day for 28 days.
Brand:CaymanSKU:22287 -Out of stock
Ipratropium is a muscarinic receptor antagonist (IC50s = 2.9, 2, and 1.7 nM for M1, M2, and M3 receptors, respectively).{47807} It inhibits acetylcholine-induced bronchospasm in anesthetized guinea pigs (EC50 = 68 μg/ml). Aerosolized ipratropium (0.2 mg/20 ml) prevents increases in airway resistance in a rat model of cadmium inhalation-induced chronic pulmonary inflammation with airspace enlargement and reduces neutrophil counts and total cell numbers in bronchoalveolar lavage fluid (BALF) and airspace enlargement in lungs when administered in combination with formoterol (Item No. 15584).{47808} Formulations containing ipratropium have been used in the treatment of bronchospasm associated with chronic obstructive pulmonary disease.
Brand:CaymanSKU:29423 - 100 mgAvailable on backorder
Ipratropium is a muscarinic receptor antagonist (IC50s = 2.9, 2, and 1.7 nM for M1, M2, and M3 receptors, respectively).{47807} It inhibits acetylcholine-induced bronchospasm in anesthetized guinea pigs (EC50 = 68 μg/ml). Aerosolized ipratropium (0.2 mg/20 ml) prevents increases in airway resistance in a rat model of cadmium inhalation-induced chronic pulmonary inflammation with airspace enlargement and reduces neutrophil counts and total cell numbers in bronchoalveolar lavage fluid (BALF) and airspace enlargement in lungs when administered in combination with formoterol (Item No. 15584).{47808} Formulations containing ipratropium have been used in the treatment of bronchospasm associated with chronic obstructive pulmonary disease.
Brand:CaymanSKU:29423 - 50 mgAvailable on backorder
Ipriflavone (Item No. 26319) is an analytical reference standard categorized as an aromatase inhibitor and synthetic isoflavone.{46133} This product is intended for research and forensic applications.
Brand:CaymanSKU:26319 - 1 mgAvailable on backorder
Ipriflavone (Item No. 26319) is an analytical reference standard categorized as an aromatase inhibitor and synthetic isoflavone.{46133} This product is intended for research and forensic applications.
Brand:CaymanSKU:26319 - 5 mgAvailable on backorder
Ipsapirone is a partial agonist of the serotonin (5-HT) receptor 5-HT1A (Ki = 10 nM in hippocampal membranes).{35118} It reduces 5-HT release in rat ventral hippocampus in vivo.{35119} Low doses of ipsapirone decrease, while high doses increase, extracellular dopamine release in murine nucleus accumbens.{35120} Extracellular dopamine levels in murine striatum increase following administration of ipsapirone at concentrations >0.1 mg/kg. Ipsapirone has anxiolytic effects in vivo, inhibiting foot shock-induced aggression and passive avoidance behavior in rats (ED50s = 2.2 and 0.5 mg/kg, respectively).{35121} Formulations containing ipsapirone have been used to treat depression and borderline personality disorder.{35122}
Brand:CaymanSKU:22075 -Out of stock
Ipsapirone is a partial agonist of the serotonin (5-HT) receptor 5-HT1A (Ki = 10 nM in hippocampal membranes).{35118} It reduces 5-HT release in rat ventral hippocampus in vivo.{35119} Low doses of ipsapirone decrease, while high doses increase, extracellular dopamine release in murine nucleus accumbens.{35120} Extracellular dopamine levels in murine striatum increase following administration of ipsapirone at concentrations >0.1 mg/kg. Ipsapirone has anxiolytic effects in vivo, inhibiting foot shock-induced aggression and passive avoidance behavior in rats (ED50s = 2.2 and 0.5 mg/kg, respectively).{35121} Formulations containing ipsapirone have been used to treat depression and borderline personality disorder.{35122}
Brand:CaymanSKU:22075 -Out of stock
Ipsapirone is a partial agonist of the serotonin (5-HT) receptor 5-HT1A (Ki = 10 nM in hippocampal membranes).{35118} It reduces 5-HT release in rat ventral hippocampus in vivo.{35119} Low doses of ipsapirone decrease, while high doses increase, extracellular dopamine release in murine nucleus accumbens.{35120} Extracellular dopamine levels in murine striatum increase following administration of ipsapirone at concentrations >0.1 mg/kg. Ipsapirone has anxiolytic effects in vivo, inhibiting foot shock-induced aggression and passive avoidance behavior in rats (ED50s = 2.2 and 0.5 mg/kg, respectively).{35121} Formulations containing ipsapirone have been used to treat depression and borderline personality disorder.{35122}
Brand:CaymanSKU:22075 -Out of stock
Ipsapirone is a partial agonist of the serotonin (5-HT) receptor 5-HT1A (Ki = 10 nM in hippocampal membranes).{35118} It reduces 5-HT release in rat ventral hippocampus in vivo.{35119} Low doses of ipsapirone decrease, while high doses increase, extracellular dopamine release in murine nucleus accumbens.{35120} Extracellular dopamine levels in murine striatum increase following administration of ipsapirone at concentrations >0.1 mg/kg. Ipsapirone has anxiolytic effects in vivo, inhibiting foot shock-induced aggression and passive avoidance behavior in rats (ED50s = 2.2 and 0.5 mg/kg, respectively).{35121} Formulations containing ipsapirone have been used to treat depression and borderline personality disorder.{35122}
Brand:CaymanSKU:22075 -Out of stock
IPSU is a potent orexin receptor 2 (OX2R) antagonist (Ki = 14.13 nM).{46765} It is selective for OX2R over OX1R (Ki = 512.8 nM). IPSU (50 mg/kg) increases non-rapid eye movement (NREM) sleep in mice.
Brand:CaymanSKU:30007 - 1 mgAvailable on backorder
IPSU is a potent orexin receptor 2 (OX2R) antagonist (Ki = 14.13 nM).{46765} It is selective for OX2R over OX1R (Ki = 512.8 nM). IPSU (50 mg/kg) increases non-rapid eye movement (NREM) sleep in mice.
Brand:CaymanSKU:30007 - 10 mgAvailable on backorder
IPSU is a potent orexin receptor 2 (OX2R) antagonist (Ki = 14.13 nM).{46765} It is selective for OX2R over OX1R (Ki = 512.8 nM). IPSU (50 mg/kg) increases non-rapid eye movement (NREM) sleep in mice.
Brand:CaymanSKU:30007 - 25 mgAvailable on backorder
IPSU is a potent orexin receptor 2 (OX2R) antagonist (Ki = 14.13 nM).{46765} It is selective for OX2R over OX1R (Ki = 512.8 nM). IPSU (50 mg/kg) increases non-rapid eye movement (NREM) sleep in mice.
Brand:CaymanSKU:30007 - 5 mgAvailable on backorder
IPTG is a molecular mimic of allolactose, a lactose metabolite that triggers transcription of the lac operon.{22697} It is used in the concentration range of 100 μM – 1.5 mM to induce protein expression where the gene is under the control of the lac operator and is suitable for use with X-gal or bluo-gal to detect lac gene activity in cloning procedures.{24874}
Brand:CaymanSKU:- IPTG is a molecular mimic of allolactose, a lactose metabolite that triggers transcription of the lac operon.{22697} It is used in the concentration range of 100 μM – 1.5 mM to induce protein expression where the gene is under the control of the lac operator and is suitable for use with X-gal or bluo-gal to detect lac gene activity in cloning procedures.{24874}
Brand:CaymanSKU:- IPTG is a molecular mimic of allolactose, a lactose metabolite that triggers transcription of the lac operon.{22697} It is used in the concentration range of 100 μM – 1.5 mM to induce protein expression where the gene is under the control of the lac operator and is suitable for use with X-gal or bluo-gal to detect lac gene activity in cloning procedures.{24874}
Brand:CaymanSKU:- IPTG is a molecular mimic of allolactose, a lactose metabolite that triggers transcription of the lac operon.{22697} It is used in the concentration range of 100 μM – 1.5 mM to induce protein expression where the gene is under the control of the lac operator and is suitable for use with X-gal or bluo-gal to detect lac gene activity in cloning procedures.{24874}
Brand:CaymanSKU:-
IQ-1 is a cell-permeable tetrahydroisoquinolinylidene compound that maintains long-term mouse embryonic stem cell (ESC) pluripotency.{26541} When used at 4 µg/ml with Wnt3a, it allows ESCs to form embryoid bodies that continue to express markers of pluripotency, including α-fetoprotein and β-III tubulin.{26541} IQ-1 blocks the interaction of the protein Naked cuticle with a subunit of the protein phosphatase PP2A, altering signaling through Wnt/β-catenin and maintaining the expression of stem cell markers Oct4, Nanog, and Rex1 in ESCs.{26541}
Brand:CaymanSKU:- IQ-1 is a cell-permeable tetrahydroisoquinolinylidene compound that maintains long-term mouse embryonic stem cell (ESC) pluripotency.{26541} When used at 4 µg/ml with Wnt3a, it allows ESCs to form embryoid bodies that continue to express markers of pluripotency, including α-fetoprotein and β-III tubulin.{26541} IQ-1 blocks the interaction of the protein Naked cuticle with a subunit of the protein phosphatase PP2A, altering signaling through Wnt/β-catenin and maintaining the expression of stem cell markers Oct4, Nanog, and Rex1 in ESCs.{26541}
Brand:CaymanSKU:- IQ-1 is a cell-permeable tetrahydroisoquinolinylidene compound that maintains long-term mouse embryonic stem cell (ESC) pluripotency.{26541} When used at 4 µg/ml with Wnt3a, it allows ESCs to form embryoid bodies that continue to express markers of pluripotency, including α-fetoprotein and β-III tubulin.{26541} IQ-1 blocks the interaction of the protein Naked cuticle with a subunit of the protein phosphatase PP2A, altering signaling through Wnt/β-catenin and maintaining the expression of stem cell markers Oct4, Nanog, and Rex1 in ESCs.{26541}
Brand:CaymanSKU:- IQ-1 is a cell-permeable tetrahydroisoquinolinylidene compound that maintains long-term mouse embryonic stem cell (ESC) pluripotency.{26541} When used at 4 µg/ml with Wnt3a, it allows ESCs to form embryoid bodies that continue to express markers of pluripotency, including α-fetoprotein and β-III tubulin.{26541} IQ-1 blocks the interaction of the protein Naked cuticle with a subunit of the protein phosphatase PP2A, altering signaling through Wnt/β-catenin and maintaining the expression of stem cell markers Oct4, Nanog, and Rex1 in ESCs.{26541}
Brand:CaymanSKU:-
IQ-1S (free acid) is an inhibitor of NF-κB/AP-1 (IC50 = 2.3 µM in a reporter assay).{52381} It inhibits TNF-α and IL-6 production in human Mono-Mac-6 cells (IC50s = 1.3 and 3.8 µM, respectively) and isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 2.6 and 5.6 µM, respectively), as well as nitric oxide (NO) production in murine J774-A.1 macrophages (IC50 = 3.1 µM). IQ-1S (free acid) binds to JNKs (Kd = 0.24, 0.36, and 0.1µM for JNK1-3), as well as casein kinase 1δ (CK1δ), PI3Kγ, and MAPK-interacting serine/threonine kinase 2 (MKNK2; Kds = 0.38, 0.47, and 0.92 µM, respectively).
Brand:CaymanSKU:29851 - 10 mgAvailable on backorder
IQ-1S (free acid) is an inhibitor of NF-κB/AP-1 (IC50 = 2.3 µM in a reporter assay).{52381} It inhibits TNF-α and IL-6 production in human Mono-Mac-6 cells (IC50s = 1.3 and 3.8 µM, respectively) and isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 2.6 and 5.6 µM, respectively), as well as nitric oxide (NO) production in murine J774-A.1 macrophages (IC50 = 3.1 µM). IQ-1S (free acid) binds to JNKs (Kd = 0.24, 0.36, and 0.1µM for JNK1-3), as well as casein kinase 1δ (CK1δ), PI3Kγ, and MAPK-interacting serine/threonine kinase 2 (MKNK2; Kds = 0.38, 0.47, and 0.92 µM, respectively).
Brand:CaymanSKU:29851 - 25 mgAvailable on backorder
IQ-1S (free acid) is an inhibitor of NF-κB/AP-1 (IC50 = 2.3 µM in a reporter assay).{52381} It inhibits TNF-α and IL-6 production in human Mono-Mac-6 cells (IC50s = 1.3 and 3.8 µM, respectively) and isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 2.6 and 5.6 µM, respectively), as well as nitric oxide (NO) production in murine J774-A.1 macrophages (IC50 = 3.1 µM). IQ-1S (free acid) binds to JNKs (Kd = 0.24, 0.36, and 0.1µM for JNK1-3), as well as casein kinase 1δ (CK1δ), PI3Kγ, and MAPK-interacting serine/threonine kinase 2 (MKNK2; Kds = 0.38, 0.47, and 0.92 µM, respectively).
Brand:CaymanSKU:29851 - 5 mgAvailable on backorder
Nuclear factor-κB (NF-κB) is a ubiquitous transcription factor and an essential mediator of gene expression during activation of immune and inflammatory responses. NF-κB mediates the expression of a great variety of genes in response to extracellular stimuli including IL-1, TNF-α, and LPS. A serine/threonine protein kinase associated with interleukin-1 receptor-associated kinase 1 (IRAK-1) and its homologue murine pelle-like protein kinase (mPLK) has been identified.{10659,18740} IRAK-1 is associated with the IL-1 receptor subunits IL-1RI and IL-1RAcP after IL-1 binding and serves as a signaling molecule to mediate IL-1 response.{18739} IRAK-1 mediates a signaling cascade leading to NF-κB activation by members of the IL-1 family including IL-1 and IL-18 (also known as IGIF).{2150,18740}
Brand:CaymanSKU:13843 - 1 eaAvailable on backorder
Antigen: synthetic peptide corresponding to human IRAK-1 amino acids 700-712 • Host: rabbit • Cross Reactivity: (+) human and mouse IRAK-1; (−) IRAK-2 • Application(s): IP and WB • IRAK-1 is associated with the IL-1 receptor subunits IL-1RI and IL-1RAcP after IL-1 binding and serves as a signaling molecule to mediate IL-1 response. It mediates a signaling cascade leading to NF-κB activation by members of the IL-1 family including IL-1 and IL-18.
Brand:CaymanSKU:13843- 1 eaAvailable on backorder
Antigen: synthetic peptide corresponding to human IRAK-1 amino acids 700-712 • Host: rabbit • Cross Reactivity: (+) human and mouse IRAK-1; (−) IRAK-2 • Application(s): IP and WB • IRAK-1 is associated with the IL-1 receptor subunits IL-1RI and IL-1RAcP after IL-1 binding and serves as a signaling molecule to mediate IL-1 response. It mediates a signaling cascade leading to NF-κB activation by members of the IL-1 family including IL-1 and IL-18.
Brand:CaymanSKU:13843- 1 ea
Interleukin-1 receptor-associated kinases (IRAKs) are important mediators in the signal transduction of Toll/IL-1 receptor (TIR) family members. Dysregulation of TIR signaling, typified by increased NF-κB activity, results in the development of some cancers and other diseases, making the development of IRAK inhibitors a potential therapeutic strategy. IRAK-1/4 inhibitor is a benzimidazole that disrupts the activity of IRAK-1 and -4 with IC50 values of 0.3 and 0.2 µM, respectively.{29157} It demonstrates IC50 values >10 µM in a panel of 27 other kinases tested.{29157} This compound has been used to inhibit a pro-inflammatory response in microglia isolated from clinically diagnosed Alzheimer’s disease patients.{29158}
Brand:CaymanSKU:-Available on backorder
Interleukin-1 receptor-associated kinases (IRAKs) are important mediators in the signal transduction of Toll/IL-1 receptor (TIR) family members. Dysregulation of TIR signaling, typified by increased NF-κB activity, results in the development of some cancers and other diseases, making the development of IRAK inhibitors a potential therapeutic strategy. IRAK-1/4 inhibitor is a benzimidazole that disrupts the activity of IRAK-1 and -4 with IC50 values of 0.3 and 0.2 µM, respectively.{29157} It demonstrates IC50 values >10 µM in a panel of 27 other kinases tested.{29157} This compound has been used to inhibit a pro-inflammatory response in microglia isolated from clinically diagnosed Alzheimer’s disease patients.{29158}
Brand:CaymanSKU:-Available on backorder
Interleukin-1 receptor-associated kinases (IRAKs) are important mediators in the signal transduction of Toll/IL-1 receptor (TIR) family members. Dysregulation of TIR signaling, typified by increased NF-κB activity, results in the development of some cancers and other diseases, making the development of IRAK inhibitors a potential therapeutic strategy. IRAK-1/4 inhibitor is a benzimidazole that disrupts the activity of IRAK-1 and -4 with IC50 values of 0.3 and 0.2 µM, respectively.{29157} It demonstrates IC50 values >10 µM in a panel of 27 other kinases tested.{29157} This compound has been used to inhibit a pro-inflammatory response in microglia isolated from clinically diagnosed Alzheimer’s disease patients.{29158}
Brand:CaymanSKU:-Available on backorder
Interleukin-1 receptor-associated kinases (IRAKs) are important mediators in the signal transduction of Toll/IL-1 receptor (TIR) family members. Dysregulation of TIR signaling, typified by increased NF-κB activity, results in the development of some cancers and other diseases, making the development of IRAK inhibitors a potential therapeutic strategy. IRAK-1/4 inhibitor is a benzimidazole that disrupts the activity of IRAK-1 and -4 with IC50 values of 0.3 and 0.2 µM, respectively.{29157} It demonstrates IC50 values >10 µM in a panel of 27 other kinases tested.{29157} This compound has been used to inhibit a pro-inflammatory response in microglia isolated from clinically diagnosed Alzheimer’s disease patients.{29158}
Brand:CaymanSKU:-Available on backorder
The toll-like receptor (TLR) family in mammals comprises a family of transmembrane proteins characterized by multiple copies of leucine rich repeats in the extracellular domain and an interleukin-1 (IL-1) receptor motif in the cytoplasmic domain. Like its counterparts in Drosophila, TLRs signal through adaptor molecules.{17503} Interleukin-1 receptor-associated kinases (IRAKs) are important mediators in the signal transduction of Toll/IL-1 receptor (TIR) family members.{18761} The cytoplasmic domains of TIR proteins interact with the adapter protein, MyD88. MyD88 then recruits IRAKs (IRAK-1-4), which in turn interact with other adapter molecules, such as TRAF6 to activate NF-κB and MAPK pathways. A member of this family, IRAK-4 has been identified.{18762} IRAK-4 may act as an upstream activator of IRAK-1. IRAK-4 is important for LPS activation of TLRs. Mice lacking IRAK4 are resistant to lethal doses of LPS and are also severely impaired in their responses to viral and bacterial challenges.{18763,18764}
Brand:CaymanSKU:13845 - 1 eaAvailable on backorder
Antigen: synthetic peptide corresponding to a mixture of mouse IRAK-4 amino acids 38-54 and 120-136 • Host: rabbit • Cross Reactivity: (+) human and mouse IRAK-4 • Application(s): IP and WB • IRAK-4 may act as an upstream activator of IRAK-1 and is important for LPS activation of TLRs. Mice lacking IRAK4 are resistant to lethal doses of LPS and are also severely impaired in their responses to viral and bacterial challenges.
Brand:CaymanSKU:13845- 1 eaAvailable on backorder
Antigen: synthetic peptide corresponding to a mixture of mouse IRAK-4 amino acids 38-54 and 120-136 • Host: rabbit • Cross Reactivity: (+) human and mouse IRAK-4 • Application(s): IP and WB • IRAK-4 may act as an upstream activator of IRAK-1 and is important for LPS activation of TLRs. Mice lacking IRAK4 are resistant to lethal doses of LPS and are also severely impaired in their responses to viral and bacterial challenges.
Brand:CaymanSKU:13845- 1 ea
Irbesartan is an antagonist of the angiotensin II type 1 (AT1) receptor (Ki = 1.3 nM).{21001} It is an insurmountable antagonist of AT1, as its antagonism cannot be overcome by increasing concentrations of angiotensin II.{21393} Irbesartan (3, 10, and 30 mg/kg) reduces blood pressure in stroke-prone spontaneously hypertensive rats and increases survival of SPSH rats fed a high-salt low-protein diet.{43281} It also reduces plaque formation, collagen content, as well as the increased expression of the AT1 receptor, PDGF-b, MCP-1, and VCAM-1 in a model of diabetes-induced atherosclerosis using apolipoprotein E (ApoE) knockout mice with diabetes induced by streptozotocin (STZ; Item No. 13104).{43280} Formulations containing irbesartan have been used, alone and in combination with diuretics, in the treatment of hypertension.
Brand:CaymanSKU:11952 - 10 mgAvailable on backorder