Chemicals
Showing 9151–9300 of 41137 results
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AMG 232 is an inhibitor of the murine double minute 2 (MDM2) interaction with the tumor suppressor p53 (KD = 0.045 nM; IC50 = 0.6 nM in a cell-free binding assay).{48262} It inhibits proliferation of HCT116 p53 wild-type, but not p53-/-, cells (IC50s = 10 nM and >25 µM, respectively).{48263} It reduces tumor growth in an SJSA-1 osteosarcoma mouse xenograft model (ED50 = 9.1 mg/kg) and induces complete regression of tumors in the same model when administered at a dose of 75 mg/kg per day for 10 days.{48263,48262} It induces apoptosis of SJSA-1 mouse xenograft tumor cells, decreasing BrdU-labeled cells, increasing cleaved caspase-3, and halting the cell cycle.{48262}
Brand:CaymanSKU:25667 - 5 mgAvailable on backorder
AMG 319 is a potent inhibitor of phosphatidylinositol 3-kinase (PI3K) isoform δ (PI3Kδ; IC50 = 18 nM) that less effectively targets the α, β, and γ isoforms (IC50s = 33, 2.7, and 0.85 µM, respectively).{32332} It blocks anti-IgM/CD40L-induced proliferation (IC50 = 8.6 nM) and reduces Akt phosphorylation (IC50 = 1.5 nM) in B cells.{32332} AMG 319 is orally bioavailable and reduces inflammation in two animal models.{32332}
Brand:CaymanSKU:-Available on backorder
AMG 319 is a potent inhibitor of phosphatidylinositol 3-kinase (PI3K) isoform δ (PI3Kδ; IC50 = 18 nM) that less effectively targets the α, β, and γ isoforms (IC50s = 33, 2.7, and 0.85 µM, respectively).{32332} It blocks anti-IgM/CD40L-induced proliferation (IC50 = 8.6 nM) and reduces Akt phosphorylation (IC50 = 1.5 nM) in B cells.{32332} AMG 319 is orally bioavailable and reduces inflammation in two animal models.{32332}
Brand:CaymanSKU:-Available on backorder
AMG 319 is a potent inhibitor of phosphatidylinositol 3-kinase (PI3K) isoform δ (PI3Kδ; IC50 = 18 nM) that less effectively targets the α, β, and γ isoforms (IC50s = 33, 2.7, and 0.85 µM, respectively).{32332} It blocks anti-IgM/CD40L-induced proliferation (IC50 = 8.6 nM) and reduces Akt phosphorylation (IC50 = 1.5 nM) in B cells.{32332} AMG 319 is orally bioavailable and reduces inflammation in two animal models.{32332}
Brand:CaymanSKU:-Available on backorder
AMG 319 is a potent inhibitor of phosphatidylinositol 3-kinase (PI3K) isoform δ (PI3Kδ; IC50 = 18 nM) that less effectively targets the α, β, and γ isoforms (IC50s = 33, 2.7, and 0.85 µM, respectively).{32332} It blocks anti-IgM/CD40L-induced proliferation (IC50 = 8.6 nM) and reduces Akt phosphorylation (IC50 = 1.5 nM) in B cells.{32332} AMG 319 is orally bioavailable and reduces inflammation in two animal models.{32332}
Brand:CaymanSKU:-Available on backorder
AMG 337 is an orally active and selective inhibitor of c-Met kinase activity (IC50 = 1 nM) and adaptor protein Gab-1 phosphorylation, which subsequently blocks downstream PI3K and MAPK pathways.{33506} It has been shown to inhibit hepatocyte growth factor-mediated c-Met phosphorylation in PC3 cells (IC50 = 5 nM) and to block tumor growth in a c-Met-dependent xenograft model in mice (ED50 = 0.3 mg/kg).{33506} AMG 337 has been used to inhibit cell proliferation in various c-Met-dependent tumor models.{33508,33507}
Brand:CaymanSKU:21333 -Out of stock
AMG 337 is an orally active and selective inhibitor of c-Met kinase activity (IC50 = 1 nM) and adaptor protein Gab-1 phosphorylation, which subsequently blocks downstream PI3K and MAPK pathways.{33506} It has been shown to inhibit hepatocyte growth factor-mediated c-Met phosphorylation in PC3 cells (IC50 = 5 nM) and to block tumor growth in a c-Met-dependent xenograft model in mice (ED50 = 0.3 mg/kg).{33506} AMG 337 has been used to inhibit cell proliferation in various c-Met-dependent tumor models.{33508,33507}
Brand:CaymanSKU:21333 -Out of stock
AMG 337 is an orally active and selective inhibitor of c-Met kinase activity (IC50 = 1 nM) and adaptor protein Gab-1 phosphorylation, which subsequently blocks downstream PI3K and MAPK pathways.{33506} It has been shown to inhibit hepatocyte growth factor-mediated c-Met phosphorylation in PC3 cells (IC50 = 5 nM) and to block tumor growth in a c-Met-dependent xenograft model in mice (ED50 = 0.3 mg/kg).{33506} AMG 337 has been used to inhibit cell proliferation in various c-Met-dependent tumor models.{33508,33507}
Brand:CaymanSKU:21333 -Out of stock
AMG 337 is an orally active and selective inhibitor of c-Met kinase activity (IC50 = 1 nM) and adaptor protein Gab-1 phosphorylation, which subsequently blocks downstream PI3K and MAPK pathways.{33506} It has been shown to inhibit hepatocyte growth factor-mediated c-Met phosphorylation in PC3 cells (IC50 = 5 nM) and to block tumor growth in a c-Met-dependent xenograft model in mice (ED50 = 0.3 mg/kg).{33506} AMG 337 has been used to inhibit cell proliferation in various c-Met-dependent tumor models.{33508,33507}
Brand:CaymanSKU:21333 -Out of stock
AMG 47a is an orally bioavailable inhibitor of Lck, VEGF receptor 2 (VEGFR2/KDR), p38α, and JAK3 (IC50s = 0.2, 1, 3, and 72 nM, respectively).{39861} It is selective for these kinases over a panel of additional kinases including SYK, JNK1, and PKAβ (IC50s = 292 to >25,000 nM) but does inhibit Src (IC50 = 2 nM). It decreases IL-2, but not TNF-α, production induced by an anti-CD3 antibody in 50% whole blood and inhibits T cell proliferation in vitro in a mixed lymphocyte reaction assay (IC50 = 30 nM). AMG 47a (10, 30, and 100 mg/kg) has anti-inflammatory activity, decreasing production of IL-2 induced by an anti-CD3 antibody in mice. It also decreases levels of mutant oncogene KRASG12V in HeLa cells in a reporter assay when used at a concentration of 1 µM.{39862}
Brand:CaymanSKU:25339 - 10 mgAvailable on backorder
AMG 47a is an orally bioavailable inhibitor of Lck, VEGF receptor 2 (VEGFR2/KDR), p38α, and JAK3 (IC50s = 0.2, 1, 3, and 72 nM, respectively).{39861} It is selective for these kinases over a panel of additional kinases including SYK, JNK1, and PKAβ (IC50s = 292 to >25,000 nM) but does inhibit Src (IC50 = 2 nM). It decreases IL-2, but not TNF-α, production induced by an anti-CD3 antibody in 50% whole blood and inhibits T cell proliferation in vitro in a mixed lymphocyte reaction assay (IC50 = 30 nM). AMG 47a (10, 30, and 100 mg/kg) has anti-inflammatory activity, decreasing production of IL-2 induced by an anti-CD3 antibody in mice. It also decreases levels of mutant oncogene KRASG12V in HeLa cells in a reporter assay when used at a concentration of 1 µM.{39862}
Brand:CaymanSKU:25339 - 25 mgAvailable on backorder
AMG 47a is an orally bioavailable inhibitor of Lck, VEGF receptor 2 (VEGFR2/KDR), p38α, and JAK3 (IC50s = 0.2, 1, 3, and 72 nM, respectively).{39861} It is selective for these kinases over a panel of additional kinases including SYK, JNK1, and PKAβ (IC50s = 292 to >25,000 nM) but does inhibit Src (IC50 = 2 nM). It decreases IL-2, but not TNF-α, production induced by an anti-CD3 antibody in 50% whole blood and inhibits T cell proliferation in vitro in a mixed lymphocyte reaction assay (IC50 = 30 nM). AMG 47a (10, 30, and 100 mg/kg) has anti-inflammatory activity, decreasing production of IL-2 induced by an anti-CD3 antibody in mice. It also decreases levels of mutant oncogene KRASG12V in HeLa cells in a reporter assay when used at a concentration of 1 µM.{39862}
Brand:CaymanSKU:25339 - 5 mgAvailable on backorder
AMG 47a is an orally bioavailable inhibitor of Lck, VEGF receptor 2 (VEGFR2/KDR), p38α, and JAK3 (IC50s = 0.2, 1, 3, and 72 nM, respectively).{39861} It is selective for these kinases over a panel of additional kinases including SYK, JNK1, and PKAβ (IC50s = 292 to >25,000 nM) but does inhibit Src (IC50 = 2 nM). It decreases IL-2, but not TNF-α, production induced by an anti-CD3 antibody in 50% whole blood and inhibits T cell proliferation in vitro in a mixed lymphocyte reaction assay (IC50 = 30 nM). AMG 47a (10, 30, and 100 mg/kg) has anti-inflammatory activity, decreasing production of IL-2 induced by an anti-CD3 antibody in mice. It also decreases levels of mutant oncogene KRASG12V in HeLa cells in a reporter assay when used at a concentration of 1 µM.{39862}
Brand:CaymanSKU:25339 - 50 mgAvailable on backorder
AMG 487 is a chemokine (C-X-C motif) receptor 3 (CXCR3) antagonist (IC50 = 8.2 nM in a radioligand binding assay).{50088} It inhibits cell migration induced by chemokine (C-X-C motif) ligand 10 (CXCL10), CXCL11, and CXCL9 (IC50s = 8, 15, and 36 nM, respectively). In vivo, AMG 487 (3 mg/kg) inhibits bronchoalveolar lavage fluid (BALF) cell infiltration in a mouse model of bleomycin-induced cellular recruitment. It reduces the number of lung metastases in the K7M2 and Saos-LM7 osteosarcoma mouse xenograft models.{47785} AMG 487 (5 mg/kg) also restores mitochondrial function and inhibits mitochondrial-dependent hepatocellular apoptosis in a mouse model of non-alcoholic steatohepatitis (NASH).{47786}
Brand:CaymanSKU:28416 - 1 mgAvailable on backorder
AMG 487 is a chemokine (C-X-C motif) receptor 3 (CXCR3) antagonist (IC50 = 8.2 nM in a radioligand binding assay).{50088} It inhibits cell migration induced by chemokine (C-X-C motif) ligand 10 (CXCL10), CXCL11, and CXCL9 (IC50s = 8, 15, and 36 nM, respectively). In vivo, AMG 487 (3 mg/kg) inhibits bronchoalveolar lavage fluid (BALF) cell infiltration in a mouse model of bleomycin-induced cellular recruitment. It reduces the number of lung metastases in the K7M2 and Saos-LM7 osteosarcoma mouse xenograft models.{47785} AMG 487 (5 mg/kg) also restores mitochondrial function and inhibits mitochondrial-dependent hepatocellular apoptosis in a mouse model of non-alcoholic steatohepatitis (NASH).{47786}
Brand:CaymanSKU:28416 - 10 mgAvailable on backorder
AMG 487 is a chemokine (C-X-C motif) receptor 3 (CXCR3) antagonist (IC50 = 8.2 nM in a radioligand binding assay).{50088} It inhibits cell migration induced by chemokine (C-X-C motif) ligand 10 (CXCL10), CXCL11, and CXCL9 (IC50s = 8, 15, and 36 nM, respectively). In vivo, AMG 487 (3 mg/kg) inhibits bronchoalveolar lavage fluid (BALF) cell infiltration in a mouse model of bleomycin-induced cellular recruitment. It reduces the number of lung metastases in the K7M2 and Saos-LM7 osteosarcoma mouse xenograft models.{47785} AMG 487 (5 mg/kg) also restores mitochondrial function and inhibits mitochondrial-dependent hepatocellular apoptosis in a mouse model of non-alcoholic steatohepatitis (NASH).{47786}
Brand:CaymanSKU:28416 - 25 mgAvailable on backorder
AMG 487 is a chemokine (C-X-C motif) receptor 3 (CXCR3) antagonist (IC50 = 8.2 nM in a radioligand binding assay).{50088} It inhibits cell migration induced by chemokine (C-X-C motif) ligand 10 (CXCL10), CXCL11, and CXCL9 (IC50s = 8, 15, and 36 nM, respectively). In vivo, AMG 487 (3 mg/kg) inhibits bronchoalveolar lavage fluid (BALF) cell infiltration in a mouse model of bleomycin-induced cellular recruitment. It reduces the number of lung metastases in the K7M2 and Saos-LM7 osteosarcoma mouse xenograft models.{47785} AMG 487 (5 mg/kg) also restores mitochondrial function and inhibits mitochondrial-dependent hepatocellular apoptosis in a mouse model of non-alcoholic steatohepatitis (NASH).{47786}
Brand:CaymanSKU:28416 - 5 mgAvailable on backorder
AMG 517 is an antagonist of transient receptor potential vanilloid 1 (TRPV1; IC50 = 0.9 nM).{45105} It inhibits mechanical and thermal allodynia in a rat model of burn injury when administered intrathecally at a dose of 165 µg.{35412} AMG 517 (150 and 300 µg/kg) also reverses increases in the level of calcitonin gene-related peptide (CGRP) and increases expression of GFAP and GAP-43 in the dorsal horn of the spinal cord, as well as enhances axonal regeneration in a rat model of sciatic nerve transection injury.{45106}
Brand:CaymanSKU:26191 - 10 mgAvailable on backorder
AMG 517 is an antagonist of transient receptor potential vanilloid 1 (TRPV1; IC50 = 0.9 nM).{45105} It inhibits mechanical and thermal allodynia in a rat model of burn injury when administered intrathecally at a dose of 165 µg.{35412} AMG 517 (150 and 300 µg/kg) also reverses increases in the level of calcitonin gene-related peptide (CGRP) and increases expression of GFAP and GAP-43 in the dorsal horn of the spinal cord, as well as enhances axonal regeneration in a rat model of sciatic nerve transection injury.{45106}
Brand:CaymanSKU:26191 - 25 mgAvailable on backorder
AMG 517 is an antagonist of transient receptor potential vanilloid 1 (TRPV1; IC50 = 0.9 nM).{45105} It inhibits mechanical and thermal allodynia in a rat model of burn injury when administered intrathecally at a dose of 165 µg.{35412} AMG 517 (150 and 300 µg/kg) also reverses increases in the level of calcitonin gene-related peptide (CGRP) and increases expression of GFAP and GAP-43 in the dorsal horn of the spinal cord, as well as enhances axonal regeneration in a rat model of sciatic nerve transection injury.{45106}
Brand:CaymanSKU:26191 - 5 mgAvailable on backorder
AMG 517 is an antagonist of transient receptor potential vanilloid 1 (TRPV1; IC50 = 0.9 nM).{45105} It inhibits mechanical and thermal allodynia in a rat model of burn injury when administered intrathecally at a dose of 165 µg.{35412} AMG 517 (150 and 300 µg/kg) also reverses increases in the level of calcitonin gene-related peptide (CGRP) and increases expression of GFAP and GAP-43 in the dorsal horn of the spinal cord, as well as enhances axonal regeneration in a rat model of sciatic nerve transection injury.{45106}
Brand:CaymanSKU:26191 - 50 mgAvailable on backorder
AMG 706 is a multikinase inhibitor that predominantly targets receptor tyrosine kinases, including VEGFR1, VEGFR2, VEGFR3, c-Kit, PDGFR, and RET (IC50s = 2, 3, 6, 8, 84, and 59 nM, respectively).{30951} It also potently inhibits CSF1R and ZAK (IC50s = 5.6 and 8 nM, respectively), as well as several mutants of c-Kit.{24156} AMG 706 inhibits the proliferation of human endothelial cells induced by VEGF but not FGF.{30951} Oral administration of AMG 706 blocks VEGF-induced angiogenesis in the rat corneal model and induces regression of established A431 xenografts in mice.{30951}
Brand:CaymanSKU:-Available on backorder
AMG 706 is a multikinase inhibitor that predominantly targets receptor tyrosine kinases, including VEGFR1, VEGFR2, VEGFR3, c-Kit, PDGFR, and RET (IC50s = 2, 3, 6, 8, 84, and 59 nM, respectively).{30951} It also potently inhibits CSF1R and ZAK (IC50s = 5.6 and 8 nM, respectively), as well as several mutants of c-Kit.{24156} AMG 706 inhibits the proliferation of human endothelial cells induced by VEGF but not FGF.{30951} Oral administration of AMG 706 blocks VEGF-induced angiogenesis in the rat corneal model and induces regression of established A431 xenografts in mice.{30951}
Brand:CaymanSKU:-Available on backorder
AMG 706 is a multikinase inhibitor that predominantly targets receptor tyrosine kinases, including VEGFR1, VEGFR2, VEGFR3, c-Kit, PDGFR, and RET (IC50s = 2, 3, 6, 8, 84, and 59 nM, respectively).{30951} It also potently inhibits CSF1R and ZAK (IC50s = 5.6 and 8 nM, respectively), as well as several mutants of c-Kit.{24156} AMG 706 inhibits the proliferation of human endothelial cells induced by VEGF but not FGF.{30951} Oral administration of AMG 706 blocks VEGF-induced angiogenesis in the rat corneal model and induces regression of established A431 xenografts in mice.{30951}
Brand:CaymanSKU:-Available on backorder
AMG 706 is a multikinase inhibitor that predominantly targets receptor tyrosine kinases, including VEGFR1, VEGFR2, VEGFR3, c-Kit, PDGFR, and RET (IC50s = 2, 3, 6, 8, 84, and 59 nM, respectively).{30951} It also potently inhibits CSF1R and ZAK (IC50s = 5.6 and 8 nM, respectively), as well as several mutants of c-Kit.{24156} AMG 706 inhibits the proliferation of human endothelial cells induced by VEGF but not FGF.{30951} Oral administration of AMG 706 blocks VEGF-induced angiogenesis in the rat corneal model and induces regression of established A431 xenografts in mice.{30951}
Brand:CaymanSKU:-Available on backorder
AMG 837 is a potent, orally bioavailable partial agonist at GPR40 (FFAR1; EC50 = 13 nM) that is highly selective over GPR41, GPR43, and GPR120 (EC50 > 10,000 nM) in a calcium flux assay using CHO cells transfected with the human receptor.{34388,34389} GPR40 is a G protein-coupled free fatty acid receptor localized mainly on pancreatic islet cells that activates the Gq signaling pathway. In rats, AMG 837 increases insulin release when glucose levels are elevated, but it failed to do so in healthy volunteers during Phase I clinical trials.{34389,34390}
Brand:CaymanSKU:21815 -Out of stock
AMG 837 is a potent, orally bioavailable partial agonist at GPR40 (FFAR1; EC50 = 13 nM) that is highly selective over GPR41, GPR43, and GPR120 (EC50 > 10,000 nM) in a calcium flux assay using CHO cells transfected with the human receptor.{34388,34389} GPR40 is a G protein-coupled free fatty acid receptor localized mainly on pancreatic islet cells that activates the Gq signaling pathway. In rats, AMG 837 increases insulin release when glucose levels are elevated, but it failed to do so in healthy volunteers during Phase I clinical trials.{34389,34390}
Brand:CaymanSKU:21815 -Out of stock
AMG 837 is a potent, orally bioavailable partial agonist at GPR40 (FFAR1; EC50 = 13 nM) that is highly selective over GPR41, GPR43, and GPR120 (EC50 > 10,000 nM) in a calcium flux assay using CHO cells transfected with the human receptor.{34388,34389} GPR40 is a G protein-coupled free fatty acid receptor localized mainly on pancreatic islet cells that activates the Gq signaling pathway. In rats, AMG 837 increases insulin release when glucose levels are elevated, but it failed to do so in healthy volunteers during Phase I clinical trials.{34389,34390}
Brand:CaymanSKU:21815 -Out of stock
AMG 837 is a potent, orally bioavailable partial agonist at GPR40 (FFAR1; EC50 = 13 nM) that is highly selective over GPR41, GPR43, and GPR120 (EC50 > 10,000 nM) in a calcium flux assay using CHO cells transfected with the human receptor.{34388,34389} GPR40 is a G protein-coupled free fatty acid receptor localized mainly on pancreatic islet cells that activates the Gq signaling pathway. In rats, AMG 837 increases insulin release when glucose levels are elevated, but it failed to do so in healthy volunteers during Phase I clinical trials.{34389,34390}
Brand:CaymanSKU:21815 -Out of stock
Three Aurora kinases, A-C, are involved in phosphorylation events that are critical for the completion of mitosis. Their expression is elevated in a variety of human cancers. AMG 900 is an orally bioavailable, selective Aurora kinase inhibitor with IC50 values of 5, 4, and 1 nM for Aurora A, B, and C, respectively.{31008} It is greater than 10-fold selective for Aurora kinases over p38α, TYK2, JNK2, Met, and Tie2 (IC50s = 53, 220, 520, 550, and 650 nM, respectively).{31008} At 2-3 nM, AMG 900 has been shown to inhibit the proliferation of 26 different tumor cell lines in vitro, including cell lines resistant to either the antimitotic agent paclitaxel (Item No. 10461) or to other Aurora kinase inhibitors.{31008} Furthermore, AMG 900 is reported to be broadly active in multiple xenograft models, including three multidrug-resistant xenograft models, representing five tumor types.{31008}
Brand:CaymanSKU:-Available on backorder
Three Aurora kinases, A-C, are involved in phosphorylation events that are critical for the completion of mitosis. Their expression is elevated in a variety of human cancers. AMG 900 is an orally bioavailable, selective Aurora kinase inhibitor with IC50 values of 5, 4, and 1 nM for Aurora A, B, and C, respectively.{31008} It is greater than 10-fold selective for Aurora kinases over p38α, TYK2, JNK2, Met, and Tie2 (IC50s = 53, 220, 520, 550, and 650 nM, respectively).{31008} At 2-3 nM, AMG 900 has been shown to inhibit the proliferation of 26 different tumor cell lines in vitro, including cell lines resistant to either the antimitotic agent paclitaxel (Item No. 10461) or to other Aurora kinase inhibitors.{31008} Furthermore, AMG 900 is reported to be broadly active in multiple xenograft models, including three multidrug-resistant xenograft models, representing five tumor types.{31008}
Brand:CaymanSKU:-Available on backorder
Three Aurora kinases, A-C, are involved in phosphorylation events that are critical for the completion of mitosis. Their expression is elevated in a variety of human cancers. AMG 900 is an orally bioavailable, selective Aurora kinase inhibitor with IC50 values of 5, 4, and 1 nM for Aurora A, B, and C, respectively.{31008} It is greater than 10-fold selective for Aurora kinases over p38α, TYK2, JNK2, Met, and Tie2 (IC50s = 53, 220, 520, 550, and 650 nM, respectively).{31008} At 2-3 nM, AMG 900 has been shown to inhibit the proliferation of 26 different tumor cell lines in vitro, including cell lines resistant to either the antimitotic agent paclitaxel (Item No. 10461) or to other Aurora kinase inhibitors.{31008} Furthermore, AMG 900 is reported to be broadly active in multiple xenograft models, including three multidrug-resistant xenograft models, representing five tumor types.{31008}
Brand:CaymanSKU:-Available on backorder
Three Aurora kinases, A-C, are involved in phosphorylation events that are critical for the completion of mitosis. Their expression is elevated in a variety of human cancers. AMG 900 is an orally bioavailable, selective Aurora kinase inhibitor with IC50 values of 5, 4, and 1 nM for Aurora A, B, and C, respectively.{31008} It is greater than 10-fold selective for Aurora kinases over p38α, TYK2, JNK2, Met, and Tie2 (IC50s = 53, 220, 520, 550, and 650 nM, respectively).{31008} At 2-3 nM, AMG 900 has been shown to inhibit the proliferation of 26 different tumor cell lines in vitro, including cell lines resistant to either the antimitotic agent paclitaxel (Item No. 10461) or to other Aurora kinase inhibitors.{31008} Furthermore, AMG 900 is reported to be broadly active in multiple xenograft models, including three multidrug-resistant xenograft models, representing five tumor types.{31008}
Brand:CaymanSKU:-Available on backorder
AMG 925 is a dual inhibitor of FMS-related tyrosine kinase 3 (FLT3) and cyclin-dependent kinase 4 (Cdk4; IC50s = 1 and 3 nM, respectively).{48702} It is selective for FLT3 and Cdk4 over Cdk1 (IC50 = 2.22 μM). AMG 925 also binds to FLT3ITD, FLT3D835Y, FLT3D835H, FLT3K663Q, and FLT3N841I (Kds = 1-4 nM). It inhibits proliferation of MOLM-13, COLO 205, and U937 cancer cells (IC50s = 19, 55, and 52 nM, respectively). AMG 925 (50, 75, and 150 mg/kg) reduces intratumor levels of pSTAT5 and pRb and inhibits tumor growth in a MOLM-13 acute myeloid leukemia (AML) mouse xenograft model.
Brand:CaymanSKU:29245 - 1 mgAvailable on backorder
AMG 925 is a dual inhibitor of FMS-related tyrosine kinase 3 (FLT3) and cyclin-dependent kinase 4 (Cdk4; IC50s = 1 and 3 nM, respectively).{48702} It is selective for FLT3 and Cdk4 over Cdk1 (IC50 = 2.22 μM). AMG 925 also binds to FLT3ITD, FLT3D835Y, FLT3D835H, FLT3K663Q, and FLT3N841I (Kds = 1-4 nM). It inhibits proliferation of MOLM-13, COLO 205, and U937 cancer cells (IC50s = 19, 55, and 52 nM, respectively). AMG 925 (50, 75, and 150 mg/kg) reduces intratumor levels of pSTAT5 and pRb and inhibits tumor growth in a MOLM-13 acute myeloid leukemia (AML) mouse xenograft model.
Brand:CaymanSKU:29245 - 10 mgAvailable on backorder
AMG 925 is a dual inhibitor of FMS-related tyrosine kinase 3 (FLT3) and cyclin-dependent kinase 4 (Cdk4; IC50s = 1 and 3 nM, respectively).{48702} It is selective for FLT3 and Cdk4 over Cdk1 (IC50 = 2.22 μM). AMG 925 also binds to FLT3ITD, FLT3D835Y, FLT3D835H, FLT3K663Q, and FLT3N841I (Kds = 1-4 nM). It inhibits proliferation of MOLM-13, COLO 205, and U937 cancer cells (IC50s = 19, 55, and 52 nM, respectively). AMG 925 (50, 75, and 150 mg/kg) reduces intratumor levels of pSTAT5 and pRb and inhibits tumor growth in a MOLM-13 acute myeloid leukemia (AML) mouse xenograft model.
Brand:CaymanSKU:29245 - 25 mgAvailable on backorder
AMG 925 is a dual inhibitor of FMS-related tyrosine kinase 3 (FLT3) and cyclin-dependent kinase 4 (Cdk4; IC50s = 1 and 3 nM, respectively).{48702} It is selective for FLT3 and Cdk4 over Cdk1 (IC50 = 2.22 μM). AMG 925 also binds to FLT3ITD, FLT3D835Y, FLT3D835H, FLT3K663Q, and FLT3N841I (Kds = 1-4 nM). It inhibits proliferation of MOLM-13, COLO 205, and U937 cancer cells (IC50s = 19, 55, and 52 nM, respectively). AMG 925 (50, 75, and 150 mg/kg) reduces intratumor levels of pSTAT5 and pRb and inhibits tumor growth in a MOLM-13 acute myeloid leukemia (AML) mouse xenograft model.
Brand:CaymanSKU:29245 - 5 mgAvailable on backorder
AMG 9810 is a competitive antagonist of capsaicin activation of the vanilloid receptor 1 (TRPV1) (IC50s = 24.5 and 85.6 nM for human and rat, respectively).{23388} Additionally, it has been shown to compete with other modes of TRPV1 activation, including protons (IC50s = 92.7 and 294 nM for human and rat, respectively), heat (IC50s = 15.8 and 21 nM for human and rat, respectively), and the endogenous ligands: anandamide, N-arachidonyl dopamine (IC50s = 8.5 and 260 nM for human and rat, respectively), and oleoyldopamine.{23388} In a rat model of inflammatory pain induced by intraplantar injection of complete Freund’s adjuvant, 30-100 mg/kg AMG 9810 reverses thermal and mechanical hyperalgesia.{23388}
Brand:CaymanSKU:-AMG 9810 is a competitive antagonist of capsaicin activation of the vanilloid receptor 1 (TRPV1) (IC50s = 24.5 and 85.6 nM for human and rat, respectively).{23388} Additionally, it has been shown to compete with other modes of TRPV1 activation, including protons (IC50s = 92.7 and 294 nM for human and rat, respectively), heat (IC50s = 15.8 and 21 nM for human and rat, respectively), and the endogenous ligands: anandamide, N-arachidonyl dopamine (IC50s = 8.5 and 260 nM for human and rat, respectively), and oleoyldopamine.{23388} In a rat model of inflammatory pain induced by intraplantar injection of complete Freund’s adjuvant, 30-100 mg/kg AMG 9810 reverses thermal and mechanical hyperalgesia.{23388}
Brand:CaymanSKU:-AMG 9810 is a competitive antagonist of capsaicin activation of the vanilloid receptor 1 (TRPV1) (IC50s = 24.5 and 85.6 nM for human and rat, respectively).{23388} Additionally, it has been shown to compete with other modes of TRPV1 activation, including protons (IC50s = 92.7 and 294 nM for human and rat, respectively), heat (IC50s = 15.8 and 21 nM for human and rat, respectively), and the endogenous ligands: anandamide, N-arachidonyl dopamine (IC50s = 8.5 and 260 nM for human and rat, respectively), and oleoyldopamine.{23388} In a rat model of inflammatory pain induced by intraplantar injection of complete Freund’s adjuvant, 30-100 mg/kg AMG 9810 reverses thermal and mechanical hyperalgesia.{23388}
Brand:CaymanSKU:-AMG 9810 is a competitive antagonist of capsaicin activation of the vanilloid receptor 1 (TRPV1) (IC50s = 24.5 and 85.6 nM for human and rat, respectively).{23388} Additionally, it has been shown to compete with other modes of TRPV1 activation, including protons (IC50s = 92.7 and 294 nM for human and rat, respectively), heat (IC50s = 15.8 and 21 nM for human and rat, respectively), and the endogenous ligands: anandamide, N-arachidonyl dopamine (IC50s = 8.5 and 260 nM for human and rat, respectively), and oleoyldopamine.{23388} In a rat model of inflammatory pain induced by intraplantar injection of complete Freund’s adjuvant, 30-100 mg/kg AMG 9810 reverses thermal and mechanical hyperalgesia.{23388}
Brand:CaymanSKU:-AMG-Tie2-1 is an inhibitor of tunica interna endothelial cell kinase 2 (Tie2) and VEGF receptor 2 (VEGFR2) with IC50 values of 1 and 3 nM, respectively, in a homogenous time-resolved fluorescence (HTRF) assay.{46498} It inhibits angiopoietin 1-induced Tie2 autophosphorylation in EA.hy926 human endothelial cells (IC50 = 10 nM).
Brand:CaymanSKU:28850 - 1 mgAvailable on backorder
AMG-Tie2-1 is an inhibitor of tunica interna endothelial cell kinase 2 (Tie2) and VEGF receptor 2 (VEGFR2) with IC50 values of 1 and 3 nM, respectively, in a homogenous time-resolved fluorescence (HTRF) assay.{46498} It inhibits angiopoietin 1-induced Tie2 autophosphorylation in EA.hy926 human endothelial cells (IC50 = 10 nM).
Brand:CaymanSKU:28850 - 10 mgAvailable on backorder
AMG-Tie2-1 is an inhibitor of tunica interna endothelial cell kinase 2 (Tie2) and VEGF receptor 2 (VEGFR2) with IC50 values of 1 and 3 nM, respectively, in a homogenous time-resolved fluorescence (HTRF) assay.{46498} It inhibits angiopoietin 1-induced Tie2 autophosphorylation in EA.hy926 human endothelial cells (IC50 = 10 nM).
Brand:CaymanSKU:28850 - 25 mgAvailable on backorder
AMG-Tie2-1 is an inhibitor of tunica interna endothelial cell kinase 2 (Tie2) and VEGF receptor 2 (VEGFR2) with IC50 values of 1 and 3 nM, respectively, in a homogenous time-resolved fluorescence (HTRF) assay.{46498} It inhibits angiopoietin 1-induced Tie2 autophosphorylation in EA.hy926 human endothelial cells (IC50 = 10 nM).
Brand:CaymanSKU:28850 - 5 mgAvailable on backorder
Amicoumacin B is an amicoumacin that has been found in N. jinanensis and has quorum-sensing inhibitory activity.{60120} It is active against C. violaceum (MIC = 250 µg/ml) and reduces the expression of the C. violaceum operons vioA, vioB, vioD, and vioE, but increases the expression of vioC, indicating quorum sensing inhibitory activity.{60121} Amicoumacin B increases the expression of bone morphogenetic protein 2 (BMP2) in MG-63 cells.{60120,60122}
Brand:CaymanSKU:31777 - 2.5 mgAvailable on backorder
Amicoumacin B is an amicoumacin that has been found in N. jinanensis and has quorum-sensing inhibitory activity.{60120} It is active against C. violaceum (MIC = 250 µg/ml) and reduces the expression of the C. violaceum operons vioA, vioB, vioD, and vioE, but increases the expression of vioC, indicating quorum sensing inhibitory activity.{60121} Amicoumacin B increases the expression of bone morphogenetic protein 2 (BMP2) in MG-63 cells.{60120,60122}
Brand:CaymanSKU:31777 - 500 µgAvailable on backorder
Diacylglycerol acyltransferases (DGATs) catalyze the final step in triglyceride synthesis. DGAT-1 deficient mice demonstrate a phenotype that is protective against the development of diet-induced obesity or insulin resistance, implicating the actions of this enzyme in the development of such metabolic disorders. Amidepsine A is a fungal metabolite isolated from the culture broth of Humicola sp. FO-2942 that inhibits DGAT activity (IC50 = 10.2 µM in rat liver microsomes).{29217} It inhibits triacylglycerol formation in Raji cells with an IC50 value of 15.5 µM.{29217}
Brand:CaymanSKU:-Available on backorder
Diacylglycerol acyltransferases (DGATs) catalyze the final step in triglyceride synthesis. DGAT-1 deficient mice demonstrate a phenotype that is protective against the development of diet-induced obesity or insulin resistance, implicating the actions of this enzyme in the development of such metabolic disorders. Amidepsine A is a fungal metabolite isolated from the culture broth of Humicola sp. FO-2942 that inhibits DGAT activity (IC50 = 10.2 µM in rat liver microsomes).{29217} It inhibits triacylglycerol formation in Raji cells with an IC50 value of 15.5 µM.{29217}
Brand:CaymanSKU:-Available on backorder
Diacylglycerol acyltransferases (DGATs) catalyze the final step in triglyceride synthesis. DGAT-1 deficient mice demonstrate a phenotype that is protective against the development of diet-induced obesity or insulin resistance, implicating the actions of this enzyme in the development of such metabolic disorders. Amidepsine D is a fungal metabolite isolated from the culture broth of Humicola sp. FO-2942 that inhibits DGAT activity (IC50 = 17.5 µM in rat liver microsomes).{29217} It inhibits triacylglycerol formation in Raji cells with an IC50 value of 2.8 µM.{29217}
Brand:CaymanSKU:-Available on backorder
Diacylglycerol acyltransferases (DGATs) catalyze the final step in triglyceride synthesis. DGAT-1 deficient mice demonstrate a phenotype that is protective against the development of diet-induced obesity or insulin resistance, implicating the actions of this enzyme in the development of such metabolic disorders. Amidepsine D is a fungal metabolite isolated from the culture broth of Humicola sp. FO-2942 that inhibits DGAT activity (IC50 = 17.5 µM in rat liver microsomes).{29217} It inhibits triacylglycerol formation in Raji cells with an IC50 value of 2.8 µM.{29217}
Brand:CaymanSKU:-Available on backorder
Amifostine is a prodrug that through dephosphorylation by alkaline phosphatase is converted to an active thiol, WR 1065 that has free radical scavenging, DNA protective, and hypoxia inducing activities.{25648} Because of the differential expression of alkaline phosphatase in normal versus neoplastic tissues, the cytoprotection conferred by amifostine is selective, enabling as much as 100-fold greater accumulation of WR 1065 in normal tissues than in tumor cells.{25648} Amifostine has been used to reduce toxicity in normal tissues exposed to radiation or chemotherapeutic agents.{25648} In mouse fibroblasts and various cancer cells, amifostine (IC50 = 4 mM) has been shown to activate p53 protein, to induce the expression of the cyclin-dependent kinase inhibitor p21, and to arrest cells at the G1/S transition through a p53-dependent mechanism.{25649}
Brand:CaymanSKU:-Amifostine is a prodrug that through dephosphorylation by alkaline phosphatase is converted to an active thiol, WR 1065 that has free radical scavenging, DNA protective, and hypoxia inducing activities.{25648} Because of the differential expression of alkaline phosphatase in normal versus neoplastic tissues, the cytoprotection conferred by amifostine is selective, enabling as much as 100-fold greater accumulation of WR 1065 in normal tissues than in tumor cells.{25648} Amifostine has been used to reduce toxicity in normal tissues exposed to radiation or chemotherapeutic agents.{25648} In mouse fibroblasts and various cancer cells, amifostine (IC50 = 4 mM) has been shown to activate p53 protein, to induce the expression of the cyclin-dependent kinase inhibitor p21, and to arrest cells at the G1/S transition through a p53-dependent mechanism.{25649}
Brand:CaymanSKU:-Amifostine is a prodrug that through dephosphorylation by alkaline phosphatase is converted to an active thiol, WR 1065 that has free radical scavenging, DNA protective, and hypoxia inducing activities.{25648} Because of the differential expression of alkaline phosphatase in normal versus neoplastic tissues, the cytoprotection conferred by amifostine is selective, enabling as much as 100-fold greater accumulation of WR 1065 in normal tissues than in tumor cells.{25648} Amifostine has been used to reduce toxicity in normal tissues exposed to radiation or chemotherapeutic agents.{25648} In mouse fibroblasts and various cancer cells, amifostine (IC50 = 4 mM) has been shown to activate p53 protein, to induce the expression of the cyclin-dependent kinase inhibitor p21, and to arrest cells at the G1/S transition through a p53-dependent mechanism.{25649}
Brand:CaymanSKU:-Amifostine thiol is a radioprotective agent and an active metabolite of amifostine (Item No. 14398).{52402} It is formed from amifostine by plasma membrane-bound alkaline phosphatase. Amifostine thiol scavenges ABTS (Item No. 27317) radicals in a cell-free assay.{47394} It prevents single- and double-stranded DNA breaks induced by γ-radiation, as well as inhibits γ-radiation-induced mutations at the hypoxanthine-guanine phosphoribosyl transferase (HGPRT) locus in V79-B310H lung fibroblast cells when used at a concentration of 4 mM.{52403,52404,52405} Amifostine thiol also reduces cis-DDP-induced mutations at the HGPRT locus in V79-B310H cells.{52406} It increases survival, reduces the loss of bone marrow progenitor cells, and inhibits decreases in intestinal collagen thickness and crypt and Paneth cell density in mice exposed to total body γ-irradiation when administered at a dose of 500 mg/kg prior to irradiation.{52407}
Brand:CaymanSKU:-Available on backorder
Amifostine thiol is a radioprotective agent and an active metabolite of amifostine (Item No. 14398).{52402} It is formed from amifostine by plasma membrane-bound alkaline phosphatase. Amifostine thiol scavenges ABTS (Item No. 27317) radicals in a cell-free assay.{47394} It prevents single- and double-stranded DNA breaks induced by γ-radiation, as well as inhibits γ-radiation-induced mutations at the hypoxanthine-guanine phosphoribosyl transferase (HGPRT) locus in V79-B310H lung fibroblast cells when used at a concentration of 4 mM.{52403,52404,52405} Amifostine thiol also reduces cis-DDP-induced mutations at the HGPRT locus in V79-B310H cells.{52406} It increases survival, reduces the loss of bone marrow progenitor cells, and inhibits decreases in intestinal collagen thickness and crypt and Paneth cell density in mice exposed to total body γ-irradiation when administered at a dose of 500 mg/kg prior to irradiation.{52407}
Brand:CaymanSKU:-Available on backorder
Amifostine thiol is a radioprotective agent and an active metabolite of amifostine (Item No. 14398).{52402} It is formed from amifostine by plasma membrane-bound alkaline phosphatase. Amifostine thiol scavenges ABTS (Item No. 27317) radicals in a cell-free assay.{47394} It prevents single- and double-stranded DNA breaks induced by γ-radiation, as well as inhibits γ-radiation-induced mutations at the hypoxanthine-guanine phosphoribosyl transferase (HGPRT) locus in V79-B310H lung fibroblast cells when used at a concentration of 4 mM.{52403,52404,52405} Amifostine thiol also reduces cis-DDP-induced mutations at the HGPRT locus in V79-B310H cells.{52406} It increases survival, reduces the loss of bone marrow progenitor cells, and inhibits decreases in intestinal collagen thickness and crypt and Paneth cell density in mice exposed to total body γ-irradiation when administered at a dose of 500 mg/kg prior to irradiation.{52407}
Brand:CaymanSKU:-Available on backorder
Amikacin is an aminoglycoside antibiotic derived from kanamycin A. Like other aminoglycosides, amikacin binds to bacterial ribosomes and disrupts translation.{25245} However, the specific binding sites differ between different aminoglycoside antibiotics, as do the mechanisms of resistance.{25245,25244,25243,25242} Amikacin is effective against Gram-negative and Gram-positive bacteria.{25244}
Brand:CaymanSKU:-Amikacin is an aminoglycoside antibiotic derived from kanamycin A. Like other aminoglycosides, amikacin binds to bacterial ribosomes and disrupts translation.{25245} However, the specific binding sites differ between different aminoglycoside antibiotics, as do the mechanisms of resistance.{25245,25244,25243,25242} Amikacin is effective against Gram-negative and Gram-positive bacteria.{25244}
Brand:CaymanSKU:-Amiloride (hydrochloride) (Item No. 26295) is an analytical reference standard categorized as a diuretic.{33139} Formulations containing diuretics, including amiloride, have been misused in sports for weight reduction and as masking agents. This product is intended for use in analytical forensic applications. This product is also available as a general research tool (Item No. 14409).
Brand:CaymanSKU:26295 - 1 mgAvailable on backorder
Amiloride (hydrochloride) (Item No. 26295) is an analytical reference standard categorized as a diuretic.{33139} Formulations containing diuretics, including amiloride, have been misused in sports for weight reduction and as masking agents. This product is intended for use in analytical forensic applications. This product is also available as a general research tool (Item No. 14409).
Brand:CaymanSKU:26295 - 5 mgAvailable on backorder
Amino tadalafil is an analog of tadalafil (Item No. 14024), a potent inhibitor of phosphodiesterase 5 with applications in several conditions, including erectile dysfunction, pulmonary arterial hypertension, and lower urinary tract dysfunction.{32875} Amino tadalafil has been detected as an illegal adulterant in a dietary supplement marketed for “tonic effect.”{32874}
Brand:CaymanSKU:20876 -Out of stock
Amino tadalafil is an analog of tadalafil (Item No. 14024), a potent inhibitor of phosphodiesterase 5 with applications in several conditions, including erectile dysfunction, pulmonary arterial hypertension, and lower urinary tract dysfunction.{32875} Amino tadalafil has been detected as an illegal adulterant in a dietary supplement marketed for “tonic effect.”{32874}
Brand:CaymanSKU:20876 -Out of stock
Amino tadalafil is an analog of tadalafil (Item No. 14024), a potent inhibitor of phosphodiesterase 5 with applications in several conditions, including erectile dysfunction, pulmonary arterial hypertension, and lower urinary tract dysfunction.{32875} Amino tadalafil has been detected as an illegal adulterant in a dietary supplement marketed for “tonic effect.”{32874}
Brand:CaymanSKU:20876 -Out of stock
Amino tadalafil is an analog of tadalafil (Item No. 14024), a potent inhibitor of phosphodiesterase 5 with applications in several conditions, including erectile dysfunction, pulmonary arterial hypertension, and lower urinary tract dysfunction.{32875} Amino tadalafil has been detected as an illegal adulterant in a dietary supplement marketed for “tonic effect.”{32874}
Brand:CaymanSKU:20876 -Out of stock
Aminoacetone is a threonine and glycine catabolite that can be converted to methylglyoxal by amine oxidases.{28509} It has been identified as one of several endogenous sources of methylglyoxal found in the plasma of diabetes patients.{28508} As a pro-oxidant, 0.10-5 mM aminoacetone can induce cell death in RINm5f pancreatic β-cells.{28508} Aminoacetone is used as a growth substrate for Pseudomonas.{28507}
Brand:CaymanSKU:-Available on backorder
Aminoacetone is a threonine and glycine catabolite that can be converted to methylglyoxal by amine oxidases.{28509} It has been identified as one of several endogenous sources of methylglyoxal found in the plasma of diabetes patients.{28508} As a pro-oxidant, 0.10-5 mM aminoacetone can induce cell death in RINm5f pancreatic β-cells.{28508} Aminoacetone is used as a growth substrate for Pseudomonas.{28507}
Brand:CaymanSKU:-Available on backorder
Aminoacetone is a threonine and glycine catabolite that can be converted to methylglyoxal by amine oxidases.{28509} It has been identified as one of several endogenous sources of methylglyoxal found in the plasma of diabetes patients.{28508} As a pro-oxidant, 0.10-5 mM aminoacetone can induce cell death in RINm5f pancreatic β-cells.{28508} Aminoacetone is used as a growth substrate for Pseudomonas.{28507}
Brand:CaymanSKU:-Available on backorder
Ethylene, an important plant regulator, is synthesized from S-adenosyl-L-methionine by the sequential action of 1-amino-cyclopropane-carboxylate (ACC) synthases (ACSs) and ACC oxidases (ACOs). Aminoethoxyvinyl glycine is an inhibitor of ethylene biosynthesis that, at 1 µM, blocks the activity of both ACSs and ACOs.{25600} Through this action, it reduces ethylene-mediated changes in plant growth and development.{25602,25599,25598} Aminoethoxyvinyl glycine also inhibits cystathionine γ-lyase (Ki = 10.5 μM) with slow- and tight-binding characteristics.{17812}
Brand:CaymanSKU:-Ethylene, an important plant regulator, is synthesized from S-adenosyl-L-methionine by the sequential action of 1-amino-cyclopropane-carboxylate (ACC) synthases (ACSs) and ACC oxidases (ACOs). Aminoethoxyvinyl glycine is an inhibitor of ethylene biosynthesis that, at 1 µM, blocks the activity of both ACSs and ACOs.{25600} Through this action, it reduces ethylene-mediated changes in plant growth and development.{25602,25599,25598} Aminoethoxyvinyl glycine also inhibits cystathionine γ-lyase (Ki = 10.5 μM) with slow- and tight-binding characteristics.{17812}
Brand:CaymanSKU:-Ethylene, an important plant regulator, is synthesized from S-adenosyl-L-methionine by the sequential action of 1-amino-cyclopropane-carboxylate (ACC) synthases (ACSs) and ACC oxidases (ACOs). Aminoethoxyvinyl glycine is an inhibitor of ethylene biosynthesis that, at 1 µM, blocks the activity of both ACSs and ACOs.{25600} Through this action, it reduces ethylene-mediated changes in plant growth and development.{25602,25599,25598} Aminoethoxyvinyl glycine also inhibits cystathionine γ-lyase (Ki = 10.5 μM) with slow- and tight-binding characteristics.{17812}
Brand:CaymanSKU:-Ethylene, an important plant regulator, is synthesized from S-adenosyl-L-methionine by the sequential action of 1-amino-cyclopropane-carboxylate (ACC) synthases (ACSs) and ACC oxidases (ACOs). Aminoethoxyvinyl glycine is an inhibitor of ethylene biosynthesis that, at 1 µM, blocks the activity of both ACSs and ACOs.{25600} Through this action, it reduces ethylene-mediated changes in plant growth and development.{25602,25599,25598} Aminoethoxyvinyl glycine also inhibits cystathionine γ-lyase (Ki = 10.5 μM) with slow- and tight-binding characteristics.{17812}
Brand:CaymanSKU:-Aminoglutethimide is an aromatase inhibitor (IC50 = 7.5 µM).{27484} Aromatase inhibitors, including aminoglutethimide, inhibit estrogen synthesis via aromatase, suppressing estrogen levels in post-menopausal women. Formulations containing aromatase inhibitors have been used to treat estrogen receptor-positive breast cancer in post-menopausal women.{22657,11203}
Brand:CaymanSKU:20947 -Out of stock
Aminoglutethimide is an aromatase inhibitor (IC50 = 7.5 µM).{27484} Aromatase inhibitors, including aminoglutethimide, inhibit estrogen synthesis via aromatase, suppressing estrogen levels in post-menopausal women. Formulations containing aromatase inhibitors have been used to treat estrogen receptor-positive breast cancer in post-menopausal women.{22657,11203}
Brand:CaymanSKU:20947 -Out of stock
Aminoglutethimide is an aromatase inhibitor (IC50 = 7.5 µM).{27484} Aromatase inhibitors, including aminoglutethimide, inhibit estrogen synthesis via aromatase, suppressing estrogen levels in post-menopausal women. Formulations containing aromatase inhibitors have been used to treat estrogen receptor-positive breast cancer in post-menopausal women.{22657,11203}
Brand:CaymanSKU:20947 -Out of stock
Aminoguanidine is equipotent to L-NMMA and L-NNA as an inhibitor of iNOS.{1856,1859} The IC50 values for inhibition of mouse iNOS and rat nNOS are 5.4 and 160 µM, respectively.{1859} Aminoguanidine also inhibits induction of iNOS protein expression by endotoxin in rat macrophages.{3447}
Brand:CaymanSKU:81530 - 10 gAvailable on backorder
Aminoguanidine is equipotent to L-NMMA and L-NNA as an inhibitor of iNOS.{1856,1859} The IC50 values for inhibition of mouse iNOS and rat nNOS are 5.4 and 160 µM, respectively.{1859} Aminoguanidine also inhibits induction of iNOS protein expression by endotoxin in rat macrophages.{3447}
Brand:CaymanSKU:81530 - 100 gAvailable on backorder
Aminoguanidine is equipotent to L-NMMA and L-NNA as an inhibitor of iNOS.{1856,1859} The IC50 values for inhibition of mouse iNOS and rat nNOS are 5.4 and 160 µM, respectively.{1859} Aminoguanidine also inhibits induction of iNOS protein expression by endotoxin in rat macrophages.{3447}
Brand:CaymanSKU:81530 - 25 gAvailable on backorder
Aminoguanidine is equipotent to L-NMMA and L-NNA as an inhibitor of iNOS.{1856,1859} The IC50 values for inhibition of mouse iNOS and rat nNOS are 5.4 and 160 µM, respectively.{1859} Aminoguanidine also inhibits induction of iNOS protein expression by endotoxin in rat macrophages.{3447}
Brand:CaymanSKU:81530 - 50 gAvailable on backorder
Aminooxyacetic acid is a GABA transaminase (GABA-T) inhibitor (Ki = 9.16 μM) that induces GABA accumulation in the brain.{51157} It also inhibits cystathionine β synthase (CBS) and cystathionine γ lyase (CSE; IC50s = 8.5 and 1.1 μM, respectively).{51158} Aminooxyacetic acid (100 mg/kg) decreases GABA-T activity, without affecting glutamic acid decarboxylase (GAD) activity, and increases GABA levels in all regions of rat brain.{51159} It also decreases GABA-T activity and increases GABA in mouse brain when administered at a dose of 13 mg/kg.{51160} Aminooxyacetic acid inhibits 3-mercaptopropionic acid-, strychnine-, and pentetrazole-induced seizures in mice (ED50s = 53, 130, and 85 mg/kg, respectively), however, it exhibits neurotoxicity in the chimney test (ED50 = 62 mg/kg) and is lethal (LD50 = 105 mg/kg) to mice.
Brand:CaymanSKU:28298 - 1 gAvailable on backorder
Aminooxyacetic acid is a GABA transaminase (GABA-T) inhibitor (Ki = 9.16 μM) that induces GABA accumulation in the brain.{51157} It also inhibits cystathionine β synthase (CBS) and cystathionine γ lyase (CSE; IC50s = 8.5 and 1.1 μM, respectively).{51158} Aminooxyacetic acid (100 mg/kg) decreases GABA-T activity, without affecting glutamic acid decarboxylase (GAD) activity, and increases GABA levels in all regions of rat brain.{51159} It also decreases GABA-T activity and increases GABA in mouse brain when administered at a dose of 13 mg/kg.{51160} Aminooxyacetic acid inhibits 3-mercaptopropionic acid-, strychnine-, and pentetrazole-induced seizures in mice (ED50s = 53, 130, and 85 mg/kg, respectively), however, it exhibits neurotoxicity in the chimney test (ED50 = 62 mg/kg) and is lethal (LD50 = 105 mg/kg) to mice.
Brand:CaymanSKU:28298 - 100 mgAvailable on backorder