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GSK591 is a chemical probe for protein arginine methyltransferase 5 (PRMT5) that potently inhibits the PRMT5/MEP50 complex from methylating histone H4 (IC50 = 11 nM) in vitro. GSK591 is selective for PRMT5 (up to 50 µM) relative to a panel of other methyltransferases. In Z-138 cells, GSK591 inhibits the symmetric arginine methylation of SmD3 with an EC50 value of 56 nM. For more information on GSK591 please visit the Structural Genomics Consortium (SGC). The negative control, SGC2096, for GSK591 is also available exclusively through the SGC. You can submit a request to receive the negative control here.
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GSK591 is a chemical probe for protein arginine methyltransferase 5 (PRMT5) that potently inhibits the PRMT5/MEP50 complex from methylating histone H4 (IC50 = 11 nM) in vitro. GSK591 is selective for PRMT5 (up to 50 µM) relative to a panel of other methyltransferases. In Z-138 cells, GSK591 inhibits the symmetric arginine methylation of SmD3 with an EC50 value of 56 nM. For more information on GSK591 please visit the Structural Genomics Consortium (SGC). The negative control, SGC2096, for GSK591 is also available exclusively through the SGC. You can submit a request to receive the negative control here.
Brand:CaymanSKU:-Available on backorder
The bromodomain and PHD finger-containing (BRPF) proteins are scaffolding components of chromatin-binding MOZ/MORF histone acetyltransferase complexes, which have activity as transcriptional regulators.{21051,29177} BRPF1 (BR140 or Peregrin) is important for maintaining Hox gene expression and the development of multiple tissues, axial skeleton, and the hematopoietic system.{29177} GSK5959 is a potent, cell-permeable inhibitor of the BRPF1 bromodomain (IC50 = 80 nM).{29176} It exhibits greater than 100-fold selectivity for the BRPF1 bromodomain over a panel of 35 other bromodomains. GSK5959 disrupts chromatin binding of BRPF1 in a cellular assay by blocking the interaction of BRPF1 with histone H3.3.{29176}
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The bromodomain and PHD finger-containing (BRPF) proteins are scaffolding components of chromatin-binding MOZ/MORF histone acetyltransferase complexes, which have activity as transcriptional regulators.{21051,29177} BRPF1 (BR140 or Peregrin) is important for maintaining Hox gene expression and the development of multiple tissues, axial skeleton, and the hematopoietic system.{29177} GSK5959 is a potent, cell-permeable inhibitor of the BRPF1 bromodomain (IC50 = 80 nM).{29176} It exhibits greater than 100-fold selectivity for the BRPF1 bromodomain over a panel of 35 other bromodomains. GSK5959 disrupts chromatin binding of BRPF1 in a cellular assay by blocking the interaction of BRPF1 with histone H3.3.{29176}
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The bromodomain and PHD finger-containing (BRPF) proteins are scaffolding components of chromatin-binding MOZ/MORF histone acetyltransferase complexes, which have activity as transcriptional regulators.{21051,29177} BRPF1 (BR140 or Peregrin) is important for maintaining Hox gene expression and the development of multiple tissues, axial skeleton, and the hematopoietic system.{29177} GSK5959 is a potent, cell-permeable inhibitor of the BRPF1 bromodomain (IC50 = 80 nM).{29176} It exhibits greater than 100-fold selectivity for the BRPF1 bromodomain over a panel of 35 other bromodomains. GSK5959 disrupts chromatin binding of BRPF1 in a cellular assay by blocking the interaction of BRPF1 with histone H3.3.{29176}
Brand:CaymanSKU:-Available on backorder
The bromodomain and PHD finger-containing (BRPF) proteins are scaffolding components of chromatin-binding MOZ/MORF histone acetyltransferase complexes, which have activity as transcriptional regulators.{21051,29177} BRPF1 (BR140 or Peregrin) is important for maintaining Hox gene expression and the development of multiple tissues, axial skeleton, and the hematopoietic system.{29177} GSK5959 is a potent, cell-permeable inhibitor of the BRPF1 bromodomain (IC50 = 80 nM).{29176} It exhibits greater than 100-fold selectivity for the BRPF1 bromodomain over a panel of 35 other bromodomains. GSK5959 disrupts chromatin binding of BRPF1 in a cellular assay by blocking the interaction of BRPF1 with histone H3.3.{29176}
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GSK621 is an activator of AMP-activated protein kinase (AMPK). It has been shown to increase phosphorylation at AMPKα T172, a marker of AMPK activation, in both acute myeloid leukemia (AML) cell lines and primary AML samples.{31816} GSK621 is reported to reduce the proliferation of AML cell lines (IC50s = 13-30 μM), triggering autophagy via the eIF2α/ATF4 signaling pathway.{31816}
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GSK621 is an activator of AMP-activated protein kinase (AMPK). It has been shown to increase phosphorylation at AMPKα T172, a marker of AMPK activation, in both acute myeloid leukemia (AML) cell lines and primary AML samples.{31816} GSK621 is reported to reduce the proliferation of AML cell lines (IC50s = 13-30 μM), triggering autophagy via the eIF2α/ATF4 signaling pathway.{31816}
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GSK621 is an activator of AMP-activated protein kinase (AMPK). It has been shown to increase phosphorylation at AMPKα T172, a marker of AMPK activation, in both acute myeloid leukemia (AML) cell lines and primary AML samples.{31816} GSK621 is reported to reduce the proliferation of AML cell lines (IC50s = 13-30 μM), triggering autophagy via the eIF2α/ATF4 signaling pathway.{31816}
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GSK621 is an activator of AMP-activated protein kinase (AMPK). It has been shown to increase phosphorylation at AMPKα T172, a marker of AMPK activation, in both acute myeloid leukemia (AML) cell lines and primary AML samples.{31816} GSK621 is reported to reduce the proliferation of AML cell lines (IC50s = 13-30 μM), triggering autophagy via the eIF2α/ATF4 signaling pathway.{31816}
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GSK650394 is an inhibitor of serum- and glucocorticoid-regulated kinase (IC50s = 62 and 103 nM for SGK1 and SGK2, respectively).{28036} It demonstrates greater than 30-fold selectivity for SGK1 over Akt and other related kinases.{28036} GSK650394 can inhibit the androgen-stimulated growth of human prostate carcinoma LNCaP cells with an IC50 value of ~ 1 μM.{28036}
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GSK650394 is an inhibitor of serum- and glucocorticoid-regulated kinase (IC50s = 62 and 103 nM for SGK1 and SGK2, respectively).{28036} It demonstrates greater than 30-fold selectivity for SGK1 over Akt and other related kinases.{28036} GSK650394 can inhibit the androgen-stimulated growth of human prostate carcinoma LNCaP cells with an IC50 value of ~ 1 μM.{28036}
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GSK650394 is an inhibitor of serum- and glucocorticoid-regulated kinase (IC50s = 62 and 103 nM for SGK1 and SGK2, respectively).{28036} It demonstrates greater than 30-fold selectivity for SGK1 over Akt and other related kinases.{28036} GSK650394 can inhibit the androgen-stimulated growth of human prostate carcinoma LNCaP cells with an IC50 value of ~ 1 μM.{28036}
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GSK650394 is an inhibitor of serum- and glucocorticoid-regulated kinase (IC50s = 62 and 103 nM for SGK1 and SGK2, respectively).{28036} It demonstrates greater than 30-fold selectivity for SGK1 over Akt and other related kinases.{28036} GSK650394 can inhibit the androgen-stimulated growth of human prostate carcinoma LNCaP cells with an IC50 value of ~ 1 μM.{28036}
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GSK6853 is a chemical probe for the bromodomain of BRPF1 that displays a TR-FRET pIC50 value of 8.1 and a BROMOscan pKd value of 9.5.{33511} It exhibits >1,600-fold selectivity for BRPF1 over all other bromodomains in a BROMOscan assay and shows cellular target engagement with a pIC50 value of 7.7 in a NanoBRET assay evaluating the interaction of the NanoLuc-BRPF1 bromodomain with histone H3.3-HaloTag in HEK293 cells.{33511} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:20985 -Out of stock
GSK6853 is a chemical probe for the bromodomain of BRPF1 that displays a TR-FRET pIC50 value of 8.1 and a BROMOscan pKd value of 9.5.{33511} It exhibits >1,600-fold selectivity for BRPF1 over all other bromodomains in a BROMOscan assay and shows cellular target engagement with a pIC50 value of 7.7 in a NanoBRET assay evaluating the interaction of the NanoLuc-BRPF1 bromodomain with histone H3.3-HaloTag in HEK293 cells.{33511} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:20985 -Out of stock
GSK6853 is a chemical probe for the bromodomain of BRPF1 that displays a TR-FRET pIC50 value of 8.1 and a BROMOscan pKd value of 9.5.{33511} It exhibits >1,600-fold selectivity for BRPF1 over all other bromodomains in a BROMOscan assay and shows cellular target engagement with a pIC50 value of 7.7 in a NanoBRET assay evaluating the interaction of the NanoLuc-BRPF1 bromodomain with histone H3.3-HaloTag in HEK293 cells.{33511} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:20985 -Out of stock
GSK6853 is a chemical probe for the bromodomain of BRPF1 that displays a TR-FRET pIC50 value of 8.1 and a BROMOscan pKd value of 9.5.{33511} It exhibits >1,600-fold selectivity for BRPF1 over all other bromodomains in a BROMOscan assay and shows cellular target engagement with a pIC50 value of 7.7 in a NanoBRET assay evaluating the interaction of the NanoLuc-BRPF1 bromodomain with histone H3.3-HaloTag in HEK293 cells.{33511} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:20985 -Out of stock
GSK690693 is an ATP-competitive, pan-Akt kinase inhibitor with IC50 values of 2, 13, and 9 nM for Akt1, 2, and 3, respectively.{27556} It also inhibits other members of the AGC kinase family, including AMPK, DAPK3, PAKs, PKA, PKC, PKG, and PrkX (IC50 values range from 2-81 nM).{27556} By preventing the phosphorylation of downstream Akt substrates, GSK690693 has been shown to inhibit proliferation and to induce apoptosis in various human tumor cells in vitro and in xenografts in immunocompromised mice.{27556}
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GSK690693 is an ATP-competitive, pan-Akt kinase inhibitor with IC50 values of 2, 13, and 9 nM for Akt1, 2, and 3, respectively.{27556} It also inhibits other members of the AGC kinase family, including AMPK, DAPK3, PAKs, PKA, PKC, PKG, and PrkX (IC50 values range from 2-81 nM).{27556} By preventing the phosphorylation of downstream Akt substrates, GSK690693 has been shown to inhibit proliferation and to induce apoptosis in various human tumor cells in vitro and in xenografts in immunocompromised mice.{27556}
Brand:CaymanSKU:-Out of stock
GSK690693 is an ATP-competitive, pan-Akt kinase inhibitor with IC50 values of 2, 13, and 9 nM for Akt1, 2, and 3, respectively.{27556} It also inhibits other members of the AGC kinase family, including AMPK, DAPK3, PAKs, PKA, PKC, PKG, and PrkX (IC50 values range from 2-81 nM).{27556} By preventing the phosphorylation of downstream Akt substrates, GSK690693 has been shown to inhibit proliferation and to induce apoptosis in various human tumor cells in vitro and in xenografts in immunocompromised mice.{27556}
Brand:CaymanSKU:-Out of stock
GSK690693 is an ATP-competitive, pan-Akt kinase inhibitor with IC50 values of 2, 13, and 9 nM for Akt1, 2, and 3, respectively.{27556} It also inhibits other members of the AGC kinase family, including AMPK, DAPK3, PAKs, PKA, PKC, PKG, and PrkX (IC50 values range from 2-81 nM).{27556} By preventing the phosphorylation of downstream Akt substrates, GSK690693 has been shown to inhibit proliferation and to induce apoptosis in various human tumor cells in vitro and in xenografts in immunocompromised mice.{27556}
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GSK805 is a potent, orally bioavailable retinoid-related orphan receptor gamma t (RORγt) inverse agonist that interacts with the receptor’s putative ligand binding domain without exerting significant effects on DNA binding.{34690} It inhibits the expression of IL-17 (at 0.5 µM) in naïve CD4+ T cells activated under Th17-cell-polarizing conditions and affects the broader RORγt-dependent gene network, inhibiting the development and pathogenic function of Th17 cells. GSK805 significantly reduces the severity of experimental autoimmune encephalomyelitis (EAE), a mouse model of multiple sclerosis, when given orally to the hosts at 10 mg/kg daily beginning at the time of disease induction.
Brand:CaymanSKU:9002444 - 1 mgAvailable on backorder
GSK805 is a potent, orally bioavailable retinoid-related orphan receptor gamma t (RORγt) inverse agonist that interacts with the receptor’s putative ligand binding domain without exerting significant effects on DNA binding.{34690} It inhibits the expression of IL-17 (at 0.5 µM) in naïve CD4+ T cells activated under Th17-cell-polarizing conditions and affects the broader RORγt-dependent gene network, inhibiting the development and pathogenic function of Th17 cells. GSK805 significantly reduces the severity of experimental autoimmune encephalomyelitis (EAE), a mouse model of multiple sclerosis, when given orally to the hosts at 10 mg/kg daily beginning at the time of disease induction.
Brand:CaymanSKU:9002444 - 10 mgAvailable on backorder
GSK805 is a potent, orally bioavailable retinoid-related orphan receptor gamma t (RORγt) inverse agonist that interacts with the receptor’s putative ligand binding domain without exerting significant effects on DNA binding.{34690} It inhibits the expression of IL-17 (at 0.5 µM) in naïve CD4+ T cells activated under Th17-cell-polarizing conditions and affects the broader RORγt-dependent gene network, inhibiting the development and pathogenic function of Th17 cells. GSK805 significantly reduces the severity of experimental autoimmune encephalomyelitis (EAE), a mouse model of multiple sclerosis, when given orally to the hosts at 10 mg/kg daily beginning at the time of disease induction.
Brand:CaymanSKU:9002444 - 5 mgAvailable on backorder
A number of tumor cells and cell lines have been observed to have highly upregulated expression and activity of fatty acid synthase (FASN). GSK837149A is a selective, reversible inhibitor of FASN (pIC50 = 7.8).{30981} It acts by inhibiting the β-ketoacyl reductase activity of FASN.
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A number of tumor cells and cell lines have been observed to have highly upregulated expression and activity of fatty acid synthase (FASN). GSK837149A is a selective, reversible inhibitor of FASN (pIC50 = 7.8).{30981} It acts by inhibiting the β-ketoacyl reductase activity of FASN.
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A number of tumor cells and cell lines have been observed to have highly upregulated expression and activity of fatty acid synthase (FASN). GSK837149A is a selective, reversible inhibitor of FASN (pIC50 = 7.8).{30981} It acts by inhibiting the β-ketoacyl reductase activity of FASN.
Brand:CaymanSKU:-Available on backorder
A number of tumor cells and cell lines have been observed to have highly upregulated expression and activity of fatty acid synthase (FASN). GSK837149A is a selective, reversible inhibitor of FASN (pIC50 = 7.8).{30981} It acts by inhibiting the β-ketoacyl reductase activity of FASN.
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GSK864 is an allosteric inhibitor of mutant isocitrate dehydrogenase 1 (IDH1; IC50s = 9, 15, and 17 nM for IDH1 mutants R132C, R132H, and R132G, respectively).{29821} It is moderately selective for mutant IDH1 over wild-type IDH1 and IDH2 mutants/wild-type. GSK864 causes a dose-dependent reduction in 2-hydroxyglutarate and overcomes the block of differentiation in acute myeloid leukemia (AML) cells expressing mutant IDH1.{29821} It reduces the number of leukemic blasts in mice with AML xenografts.{29821} See the Structural Genomics Consortium (SGC) website for more information.
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GSK864 is an allosteric inhibitor of mutant isocitrate dehydrogenase 1 (IDH1; IC50s = 9, 15, and 17 nM for IDH1 mutants R132C, R132H, and R132G, respectively).{29821} It is moderately selective for mutant IDH1 over wild-type IDH1 and IDH2 mutants/wild-type. GSK864 causes a dose-dependent reduction in 2-hydroxyglutarate and overcomes the block of differentiation in acute myeloid leukemia (AML) cells expressing mutant IDH1.{29821} It reduces the number of leukemic blasts in mice with AML xenografts.{29821} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-Available on backorder
GSK864 is an allosteric inhibitor of mutant isocitrate dehydrogenase 1 (IDH1; IC50s = 9, 15, and 17 nM for IDH1 mutants R132C, R132H, and R132G, respectively).{29821} It is moderately selective for mutant IDH1 over wild-type IDH1 and IDH2 mutants/wild-type. GSK864 causes a dose-dependent reduction in 2-hydroxyglutarate and overcomes the block of differentiation in acute myeloid leukemia (AML) cells expressing mutant IDH1.{29821} It reduces the number of leukemic blasts in mice with AML xenografts.{29821} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-Available on backorder
GSK864 is an allosteric inhibitor of mutant isocitrate dehydrogenase 1 (IDH1; IC50s = 9, 15, and 17 nM for IDH1 mutants R132C, R132H, and R132G, respectively).{29821} It is moderately selective for mutant IDH1 over wild-type IDH1 and IDH2 mutants/wild-type. GSK864 causes a dose-dependent reduction in 2-hydroxyglutarate and overcomes the block of differentiation in acute myeloid leukemia (AML) cells expressing mutant IDH1.{29821} It reduces the number of leukemic blasts in mice with AML xenografts.{29821} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-Available on backorder
GSK872 is an inhibitor of receptor-interacting protein kinase 3 (RIPK3).{37147} It is selective for RIPK3, having >1,000-fold selectivity over 300 kinases in a fluorescence polarization assay at a concentration of 1 μM. GSK872 inhibits TNF- and virus-induced necrosis in 3T3-SA fibroblasts. It also inhibits necrosis induced by toll-like receptor 3 (TLR3).
Brand:CaymanSKU:23300 - 1 mgAvailable on backorder
GSK872 is an inhibitor of receptor-interacting protein kinase 3 (RIPK3).{37147} It is selective for RIPK3, having >1,000-fold selectivity over 300 kinases in a fluorescence polarization assay at a concentration of 1 μM. GSK872 inhibits TNF- and virus-induced necrosis in 3T3-SA fibroblasts. It also inhibits necrosis induced by toll-like receptor 3 (TLR3).
Brand:CaymanSKU:23300 - 10 mgAvailable on backorder
GSK872 is an inhibitor of receptor-interacting protein kinase 3 (RIPK3).{37147} It is selective for RIPK3, having >1,000-fold selectivity over 300 kinases in a fluorescence polarization assay at a concentration of 1 μM. GSK872 inhibits TNF- and virus-induced necrosis in 3T3-SA fibroblasts. It also inhibits necrosis induced by toll-like receptor 3 (TLR3).
Brand:CaymanSKU:23300 - 5 mgAvailable on backorder
GSK923295 is a potent inhibitor of centromere-associated protein E (CENP-E; Ki = 3.2 nM), a kinesin motor protein involved in mitotic checkpoint signaling.{31966,31965} GSK923295 causes mitotic cell cycle delay, leading to apoptosis in various cancer cell lines.{31966} It induces apoptosis in cancer cells in mice bearing xenografts of COLO 205 cells.{31966,31965} GSK923295 can be used with AZ3146, an inhibitor of the spindle checkpoint kinase Mps1, to generate aneuploidy in cells.{31964}
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GSK923295 is a potent inhibitor of centromere-associated protein E (CENP-E; Ki = 3.2 nM), a kinesin motor protein involved in mitotic checkpoint signaling.{31966,31965} GSK923295 causes mitotic cell cycle delay, leading to apoptosis in various cancer cell lines.{31966} It induces apoptosis in cancer cells in mice bearing xenografts of COLO 205 cells.{31966,31965} GSK923295 can be used with AZ3146, an inhibitor of the spindle checkpoint kinase Mps1, to generate aneuploidy in cells.{31964}
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GSK923295 is a potent inhibitor of centromere-associated protein E (CENP-E; Ki = 3.2 nM), a kinesin motor protein involved in mitotic checkpoint signaling.{31966,31965} GSK923295 causes mitotic cell cycle delay, leading to apoptosis in various cancer cell lines.{31966} It induces apoptosis in cancer cells in mice bearing xenografts of COLO 205 cells.{31966,31965} GSK923295 can be used with AZ3146, an inhibitor of the spindle checkpoint kinase Mps1, to generate aneuploidy in cells.{31964}
Brand:CaymanSKU:-Available on backorder
GSK923295 is a potent inhibitor of centromere-associated protein E (CENP-E; Ki = 3.2 nM), a kinesin motor protein involved in mitotic checkpoint signaling.{31966,31965} GSK923295 causes mitotic cell cycle delay, leading to apoptosis in various cancer cell lines.{31966} It induces apoptosis in cancer cells in mice bearing xenografts of COLO 205 cells.{31966,31965} GSK923295 can be used with AZ3146, an inhibitor of the spindle checkpoint kinase Mps1, to generate aneuploidy in cells.{31964}
Brand:CaymanSKU:-Available on backorder
Brand:CaymanSKU:703310 - 1 eaAvailable on backorder
GT 2016 is an antagonist of histamine H3 receptors (Ki = 43.8 nM).{51179} It is selective for H3 over H1 and H2 receptors (IC50 = >10,000 nM for both) and lacks activity against kidney and brain histamine methyltransferase at concentrations up to 3 μM. In vivo, GT 2016 (10 and 30 mg/kg) increases histamine release in the rat parietal cortex.
Brand:CaymanSKU:11996 - 1 mgAvailable on backorder
GT 2016 is an antagonist of histamine H3 receptors (Ki = 43.8 nM).{51179} It is selective for H3 over H1 and H2 receptors (IC50 = >10,000 nM for both) and lacks activity against kidney and brain histamine methyltransferase at concentrations up to 3 μM. In vivo, GT 2016 (10 and 30 mg/kg) increases histamine release in the rat parietal cortex.
Brand:CaymanSKU:11996 - 10 mgAvailable on backorder
GT 2016 is an antagonist of histamine H3 receptors (Ki = 43.8 nM).{51179} It is selective for H3 over H1 and H2 receptors (IC50 = >10,000 nM for both) and lacks activity against kidney and brain histamine methyltransferase at concentrations up to 3 μM. In vivo, GT 2016 (10 and 30 mg/kg) increases histamine release in the rat parietal cortex.
Brand:CaymanSKU:11996 - 25 mgAvailable on backorder
GT 2016 is an antagonist of histamine H3 receptors (Ki = 43.8 nM).{51179} It is selective for H3 over H1 and H2 receptors (IC50 = >10,000 nM for both) and lacks activity against kidney and brain histamine methyltransferase at concentrations up to 3 μM. In vivo, GT 2016 (10 and 30 mg/kg) increases histamine release in the rat parietal cortex.
Brand:CaymanSKU:11996 - 5 mgAvailable on backorder
GTP 14564 is an inhibitor of class III receptor tyrosine kinases (IC50s = 0.3 µM for c-Fms, c-Kit, ITD-FLT3 and 1 µM for PDGFRβ).{28667} It is without effect against a panel of non-receptor tyrosine and serine/threonine kinases.{28667} GTP 14564 blocks the proliferation of leukemia cells stimulated with FLT3 ligand by preventing the activation of STAT5.{28667,28668}
Brand:CaymanSKU:-Available on backorder
GTP 14564 is an inhibitor of class III receptor tyrosine kinases (IC50s = 0.3 µM for c-Fms, c-Kit, ITD-FLT3 and 1 µM for PDGFRβ).{28667} It is without effect against a panel of non-receptor tyrosine and serine/threonine kinases.{28667} GTP 14564 blocks the proliferation of leukemia cells stimulated with FLT3 ligand by preventing the activation of STAT5.{28667,28668}
Brand:CaymanSKU:-Available on backorder
GTP 14564 is an inhibitor of class III receptor tyrosine kinases (IC50s = 0.3 µM for c-Fms, c-Kit, ITD-FLT3 and 1 µM for PDGFRβ).{28667} It is without effect against a panel of non-receptor tyrosine and serine/threonine kinases.{28667} GTP 14564 blocks the proliferation of leukemia cells stimulated with FLT3 ligand by preventing the activation of STAT5.{28667,28668}
Brand:CaymanSKU:-Available on backorder
Brand:CaymanSKU:32753 - 200 µgAvailable on backorder
Brand:CaymanSKU:32753- 200 µgAvailable on backorder
Brand:CaymanSKU:32753- 200 µg
GTS-21 is an agonist of α7-containing nicotinic acetylcholine receptors (nAChRs) that, at a concentration of 100 μM, activates human α7-containing nAChRs expressed in Xenopus oocytes to 60% of the levels generated by endogenous ligand acetylcholine.{36257} It is selective for α7-containing nAChRs, having no activity at α2-, α3-, and α4-containing nAChRs at a concentration of 100 μM. GTS-21 stimulates dopamine release from rat striatal slices (EC50 = 10 μM).{36258} In vivo, GTS-21 decreases delay in the delayed matching-to-sample task in monkeys. It also suppresses amnesia and neuronal cell death in a gerbil model of ischemia-reperfusion injury.{36259}
Brand:CaymanSKU:21570 -Out of stock
GTS-21 is an agonist of α7-containing nicotinic acetylcholine receptors (nAChRs) that, at a concentration of 100 μM, activates human α7-containing nAChRs expressed in Xenopus oocytes to 60% of the levels generated by endogenous ligand acetylcholine.{36257} It is selective for α7-containing nAChRs, having no activity at α2-, α3-, and α4-containing nAChRs at a concentration of 100 μM. GTS-21 stimulates dopamine release from rat striatal slices (EC50 = 10 μM).{36258} In vivo, GTS-21 decreases delay in the delayed matching-to-sample task in monkeys. It also suppresses amnesia and neuronal cell death in a gerbil model of ischemia-reperfusion injury.{36259}
Brand:CaymanSKU:21570 -Out of stock
GTS-21 is an agonist of α7-containing nicotinic acetylcholine receptors (nAChRs) that, at a concentration of 100 μM, activates human α7-containing nAChRs expressed in Xenopus oocytes to 60% of the levels generated by endogenous ligand acetylcholine.{36257} It is selective for α7-containing nAChRs, having no activity at α2-, α3-, and α4-containing nAChRs at a concentration of 100 μM. GTS-21 stimulates dopamine release from rat striatal slices (EC50 = 10 μM).{36258} In vivo, GTS-21 decreases delay in the delayed matching-to-sample task in monkeys. It also suppresses amnesia and neuronal cell death in a gerbil model of ischemia-reperfusion injury.{36259}
Brand:CaymanSKU:21570 -Out of stock
GTS-21 is an agonist of α7-containing nicotinic acetylcholine receptors (nAChRs) that, at a concentration of 100 μM, activates human α7-containing nAChRs expressed in Xenopus oocytes to 60% of the levels generated by endogenous ligand acetylcholine.{36257} It is selective for α7-containing nAChRs, having no activity at α2-, α3-, and α4-containing nAChRs at a concentration of 100 μM. GTS-21 stimulates dopamine release from rat striatal slices (EC50 = 10 μM).{36258} In vivo, GTS-21 decreases delay in the delayed matching-to-sample task in monkeys. It also suppresses amnesia and neuronal cell death in a gerbil model of ischemia-reperfusion injury.{36259}
Brand:CaymanSKU:21570 -Out of stock
Guaiacol is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. Guaiacol is readily oxidized by the heme iron of peroxidases including the peroxidase of cyclooxygenase (COX) enzymes. It therefore serves as a reducing co-substrate for COX reactions.{4208} The color yield per peroxide at 470 nm is 6,650 (M peroxide reduced)-1 cm-1.{5037,8582,8109} Two moles of guaiacol are oxidized for each mole of hydroperoxide reduced by the peroxidase. The resulting guaiacol chromophore can be used for the colorimetric determination of hydroperoxidase activity.
Brand:CaymanSKU:70430 - 100 gAvailable on backorder
Guaiacol is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. Guaiacol is readily oxidized by the heme iron of peroxidases including the peroxidase of cyclooxygenase (COX) enzymes. It therefore serves as a reducing co-substrate for COX reactions.{4208} The color yield per peroxide at 470 nm is 6,650 (M peroxide reduced)-1 cm-1.{5037,8582,8109} Two moles of guaiacol are oxidized for each mole of hydroperoxide reduced by the peroxidase. The resulting guaiacol chromophore can be used for the colorimetric determination of hydroperoxidase activity.
Brand:CaymanSKU:70430 - 25 gAvailable on backorder
Guaiacol is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. Guaiacol is readily oxidized by the heme iron of peroxidases including the peroxidase of cyclooxygenase (COX) enzymes. It therefore serves as a reducing co-substrate for COX reactions.{4208} The color yield per peroxide at 470 nm is 6,650 (M peroxide reduced)-1 cm-1.{5037,8582,8109} Two moles of guaiacol are oxidized for each mole of hydroperoxide reduced by the peroxidase. The resulting guaiacol chromophore can be used for the colorimetric determination of hydroperoxidase activity.
Brand:CaymanSKU:70430 - 50 gAvailable on backorder
Guaiacol is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. Guaiacol is readily oxidized by the heme iron of peroxidases including the peroxidase of cyclooxygenase (COX) enzymes. It therefore serves as a reducing co-substrate for COX reactions.{4208} The color yield per peroxide at 470 nm is 6,650 (M peroxide reduced)-1 cm-1.{5037,8582,8109} Two moles of guaiacol are oxidized for each mole of hydroperoxide reduced by the peroxidase. The resulting guaiacol chromophore can be used for the colorimetric determination of hydroperoxidase activity.
Brand:CaymanSKU:70430 - 500 gAvailable on backorder
Guaiazulene is a sesquiterpene that has been found in M. chamomilla and has diverse biological activities.{59011,59012,59013} It inhibits lipid peroxidation in rat hepatic microsomes (IC50 = 9.8 μM), as well as scavenges hydroxyl and 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals in cell-free assays.{59011} It inhibits LPS-induced nitric oxide production in RAW 264.7 cells (EC50 = 10.1 μM) but is cytotoxic to RAW 264.7 cells at higher concentrations with cytotoxic concentration (CC50) values of 29.8 and 30.8 μM in the presence and absence, respectively, of LPS.{59012} Guaiazulene is cytotoxic to N2a neuroblastoma cells and primary rat neurons in a concentration-dependent manner.{59013} It inhibits decreases in hepatic glutathione (GSH) levels induced by paracetamol (acetaminophen; Item No. 10024) in rats when administered at a dose of 250 mg/kg.{59011}
Brand:CaymanSKU:31506 - 10 gAvailable on backorder
Guaiazulene is a sesquiterpene that has been found in M. chamomilla and has diverse biological activities.{59011,59012,59013} It inhibits lipid peroxidation in rat hepatic microsomes (IC50 = 9.8 μM), as well as scavenges hydroxyl and 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals in cell-free assays.{59011} It inhibits LPS-induced nitric oxide production in RAW 264.7 cells (EC50 = 10.1 μM) but is cytotoxic to RAW 264.7 cells at higher concentrations with cytotoxic concentration (CC50) values of 29.8 and 30.8 μM in the presence and absence, respectively, of LPS.{59012} Guaiazulene is cytotoxic to N2a neuroblastoma cells and primary rat neurons in a concentration-dependent manner.{59013} It inhibits decreases in hepatic glutathione (GSH) levels induced by paracetamol (acetaminophen; Item No. 10024) in rats when administered at a dose of 250 mg/kg.{59011}
Brand:CaymanSKU:31506 - 25 gAvailable on backorder
Guaiazulene is a sesquiterpene that has been found in M. chamomilla and has diverse biological activities.{59011,59012,59013} It inhibits lipid peroxidation in rat hepatic microsomes (IC50 = 9.8 μM), as well as scavenges hydroxyl and 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals in cell-free assays.{59011} It inhibits LPS-induced nitric oxide production in RAW 264.7 cells (EC50 = 10.1 μM) but is cytotoxic to RAW 264.7 cells at higher concentrations with cytotoxic concentration (CC50) values of 29.8 and 30.8 μM in the presence and absence, respectively, of LPS.{59012} Guaiazulene is cytotoxic to N2a neuroblastoma cells and primary rat neurons in a concentration-dependent manner.{59013} It inhibits decreases in hepatic glutathione (GSH) levels induced by paracetamol (acetaminophen; Item No. 10024) in rats when administered at a dose of 250 mg/kg.{59011}
Brand:CaymanSKU:31506 - 50 gAvailable on backorder
Guaifenesin is an expectorant that is reported to inhibit the secretion of the mucin MUC5AC in the IL-13-treated human airway epithelial cells with an IC50 value of ~100 μM.{33409}
Brand:CaymanSKU:21250 -Out of stock
Guaifenesin is an expectorant that is reported to inhibit the secretion of the mucin MUC5AC in the IL-13-treated human airway epithelial cells with an IC50 value of ~100 μM.{33409}
Brand:CaymanSKU:21250 -Out of stock
Guaifenesin is an expectorant that is reported to inhibit the secretion of the mucin MUC5AC in the IL-13-treated human airway epithelial cells with an IC50 value of ~100 μM.{33409}
Brand:CaymanSKU:21250 -Out of stock
Guaifenesin is an expectorant that is reported to inhibit the secretion of the mucin MUC5AC in the IL-13-treated human airway epithelial cells with an IC50 value of ~100 μM.{33409}
Brand:CaymanSKU:21250 -Out of stock
Guanabenz is an α2-adrenergic receptor agonist (effective concentrations 10-100 nM) with hypotensive effects.{20036}{20037} It also competes for imidazoline I2-binding sites in brown adipose tissue (Ki = 97 nM).{20035}
Brand:CaymanSKU:10851 - 100 mgAvailable on backorder
Guanabenz is an α2-adrenergic receptor agonist (effective concentrations 10-100 nM) with hypotensive effects.{20036}{20037} It also competes for imidazoline I2-binding sites in brown adipose tissue (Ki = 97 nM).{20035}
Brand:CaymanSKU:10851 - 25 mgAvailable on backorder
Guanabenz is an α2-adrenergic receptor agonist (effective concentrations 10-100 nM) with hypotensive effects.{20036}{20037} It also competes for imidazoline I2-binding sites in brown adipose tissue (Ki = 97 nM).{20035}
Brand:CaymanSKU:10851 - 50 mgAvailable on backorder
Guanethidine is an antihypertensive compound that competes with norepinephrine for transport into presynaptic terminals of adrenergic neurons by the norepinephrine transporter.{26665} Once guanethidine has entered the nerve, it becomes concentrated in synaptic vesicles, depleting endogenous norepinephrine, and thus, reducing the release of norepinephrine in response to action potentials.{26665} Guanethidine’s actions are restricted to peripheral nerve terminals because its basic guanidine group does not allow passage through the blood brain barrier.{26665} Its use has been explored in the relief of chronic pain caused by complex regional pain syndrome.{26666}
Brand:CaymanSKU:- Guanethidine is an antihypertensive compound that competes with norepinephrine for transport into presynaptic terminals of adrenergic neurons by the norepinephrine transporter.{26665} Once guanethidine has entered the nerve, it becomes concentrated in synaptic vesicles, depleting endogenous norepinephrine, and thus, reducing the release of norepinephrine in response to action potentials.{26665} Guanethidine’s actions are restricted to peripheral nerve terminals because its basic guanidine group does not allow passage through the blood brain barrier.{26665} Its use has been explored in the relief of chronic pain caused by complex regional pain syndrome.{26666}
Brand:CaymanSKU:- Guanethidine is an antihypertensive compound that competes with norepinephrine for transport into presynaptic terminals of adrenergic neurons by the norepinephrine transporter.{26665} Once guanethidine has entered the nerve, it becomes concentrated in synaptic vesicles, depleting endogenous norepinephrine, and thus, reducing the release of norepinephrine in response to action potentials.{26665} Guanethidine’s actions are restricted to peripheral nerve terminals because its basic guanidine group does not allow passage through the blood brain barrier.{26665} Its use has been explored in the relief of chronic pain caused by complex regional pain syndrome.{26666}
Brand:CaymanSKU:-
Guanfacine is an α2-adrenergic receptor (α2-AR) agonist with Ki values of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.{40326} It has EC50 values of 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively, for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki = 19 nM in a radioligand binding assay).{40341} Guanfacine (0.3-5 mg/kg) binds to adrenergic receptors in the central nervous system and lowers blood pressure in hypertensive rats in a dose-dependent manner.{40342} It also improves spatial working memory deficits induced by hypobaric hypoxia in rats.{40340} Formulations containing guanfacine are used in the treatment of high blood pressure and attention deficit hyperactivity disorder (ADHD).
Brand:CaymanSKU:22907 - 10 mgAvailable on backorder
Guanfacine is an α2-adrenergic receptor (α2-AR) agonist with Ki values of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.{40326} It has EC50 values of 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively, for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki = 19 nM in a radioligand binding assay).{40341} Guanfacine (0.3-5 mg/kg) binds to adrenergic receptors in the central nervous system and lowers blood pressure in hypertensive rats in a dose-dependent manner.{40342} It also improves spatial working memory deficits induced by hypobaric hypoxia in rats.{40340} Formulations containing guanfacine are used in the treatment of high blood pressure and attention deficit hyperactivity disorder (ADHD).
Brand:CaymanSKU:22907 - 25 mgAvailable on backorder
Guanfacine is an α2-adrenergic receptor (α2-AR) agonist with Ki values of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.{40326} It has EC50 values of 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively, for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki = 19 nM in a radioligand binding assay).{40341} Guanfacine (0.3-5 mg/kg) binds to adrenergic receptors in the central nervous system and lowers blood pressure in hypertensive rats in a dose-dependent manner.{40342} It also improves spatial working memory deficits induced by hypobaric hypoxia in rats.{40340} Formulations containing guanfacine are used in the treatment of high blood pressure and attention deficit hyperactivity disorder (ADHD).
Brand:CaymanSKU:22907 - 50 mgAvailable on backorder
Guanfacine-13C,15N3 is intended for us as an internal standard for the quantification of guanfacine (Item No. 22907) by GC- or LC-MS. Guanfacine is an α2-adrenergic receptor (α2-AR) agonist with Ki values of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.{40326} It has EC50 values of 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively, for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki = 19 nM in a radioligand binding assay).{40341} Guanfacine (0.3-5 mg/kg) binds to adrenergic receptors in the central nervous system and lowers blood pressure in hypertensive rats in a dose-dependent manner.{40342} It also improves spatial working memory deficits induced by hypobaric hypoxia in rats.{40340} Formulations containing guanfacine are used in the treatment of high blood pressure and attention deficit hyperactivity disorder (ADHD).
Brand:CaymanSKU:30143 - 1 mgAvailable on backorder
Guanidinoethyl sulfonate, also known as taurocyamine, is a natural guanidine-taurine analog derived from taurine. It is an intermediate of taurine and hypotaurine metabolism and is phosphorylated by taurocyamine kinase.{28666} Guanidinoethyl sulfonate competitively inhibits taurine uptake by sodium-dependent taurine transporters in rat hepatocytes (Ki = 1.75 mM).{28663} It also acts as a competitive glycine receptor antagonist in mouse striatal neurons.{28664} Plasma levels of guanidinoethyl sulfonate are significantly increased in patients with chronic renal failure.{28665}
Brand:CaymanSKU:-Available on backorder
Guanidinoethyl sulfonate, also known as taurocyamine, is a natural guanidine-taurine analog derived from taurine. It is an intermediate of taurine and hypotaurine metabolism and is phosphorylated by taurocyamine kinase.{28666} Guanidinoethyl sulfonate competitively inhibits taurine uptake by sodium-dependent taurine transporters in rat hepatocytes (Ki = 1.75 mM).{28663} It also acts as a competitive glycine receptor antagonist in mouse striatal neurons.{28664} Plasma levels of guanidinoethyl sulfonate are significantly increased in patients with chronic renal failure.{28665}
Brand:CaymanSKU:-Available on backorder
Guanidinoethyl sulfonate, also known as taurocyamine, is a natural guanidine-taurine analog derived from taurine. It is an intermediate of taurine and hypotaurine metabolism and is phosphorylated by taurocyamine kinase.{28666} Guanidinoethyl sulfonate competitively inhibits taurine uptake by sodium-dependent taurine transporters in rat hepatocytes (Ki = 1.75 mM).{28663} It also acts as a competitive glycine receptor antagonist in mouse striatal neurons.{28664} Plasma levels of guanidinoethyl sulfonate are significantly increased in patients with chronic renal failure.{28665}
Brand:CaymanSKU:-Available on backorder
Guanoclor is an antihypertensive agent that binds to non-adrenergic sites in pig kidney membranes (IC50 = 10 nM).{45588,45589} It inhibits the Na+/H+ exchanger in pig kidney membranes (IC50 = 1 μM) and cell-free bovine dopamine β-hydroxylase (IC50 = 90 μM). Guanoclor inhibits electrically stimulated norepinephrine release from spleen.{45588} It decreases norepinephrine levels in dog heart, spleen, hypothalamus, and adrenal gland when administered at a dose of 10 mg/kg per day for six weeks. It decreases adrenal catecholamine levels in rats when administered at a dose of 20 mg/kg per day for six weeks. Guanoclor (20 mg/kg) decreases experimentally induced hypertension and the tyramine-induced pressor response and increases the norepinephrine-induced pressor response in non-anesthetized dogs.
Brand:CaymanSKU:27659 - 10 mgAvailable on backorder
Guanoclor is an antihypertensive agent that binds to non-adrenergic sites in pig kidney membranes (IC50 = 10 nM).{45588,45589} It inhibits the Na+/H+ exchanger in pig kidney membranes (IC50 = 1 μM) and cell-free bovine dopamine β-hydroxylase (IC50 = 90 μM). Guanoclor inhibits electrically stimulated norepinephrine release from spleen.{45588} It decreases norepinephrine levels in dog heart, spleen, hypothalamus, and adrenal gland when administered at a dose of 10 mg/kg per day for six weeks. It decreases adrenal catecholamine levels in rats when administered at a dose of 20 mg/kg per day for six weeks. Guanoclor (20 mg/kg) decreases experimentally induced hypertension and the tyramine-induced pressor response and increases the norepinephrine-induced pressor response in non-anesthetized dogs.
Brand:CaymanSKU:27659 - 25 mgAvailable on backorder