Chemicals
Showing 11701–11850 of 41137 results
-
MEK5, also known as MAP2K5, phosphorylates ERK5 (MAPK7) in signaling pathways involved in stress-induced apoptosis, neuronal survival, cardiac development, and angiogenesis.{15424,27915} BIX02189 is a potent inhibitor of both MEK5 and ERK5 (IC50s = 1.5 and 59 nM, respectively), preventing transcriptional activation of the downstream target MEF2C.{27914} It minimally inhibits a panel of related kinases, including MEK1/2 and ERK1/2.{27914} BIX02189 blocks sorbitol-induced phosphorylation of ERK5, without affecting phosphorylation of ERK1/2, in HeLa cells.{27914} It has been used to investigate the roles of MEK5/ERK5 signaling in nerve growth factor-mediated neurite outgrowth and myeloid cell differentiation.{27915,27913}
Brand:CaymanSKU:-Out of stock
MEK5, also known as MAP2K5, phosphorylates ERK5 (MAPK7) in signaling pathways involved in stress-induced apoptosis, neuronal survival, cardiac development, and angiogenesis.{15424,27915} BIX02189 is a potent inhibitor of both MEK5 and ERK5 (IC50s = 1.5 and 59 nM, respectively), preventing transcriptional activation of the downstream target MEF2C.{27914} It minimally inhibits a panel of related kinases, including MEK1/2 and ERK1/2.{27914} BIX02189 blocks sorbitol-induced phosphorylation of ERK5, without affecting phosphorylation of ERK1/2, in HeLa cells.{27914} It has been used to investigate the roles of MEK5/ERK5 signaling in nerve growth factor-mediated neurite outgrowth and myeloid cell differentiation.{27915,27913}
Brand:CaymanSKU:-Out of stock
Bizine is a phenelzine analog that inhibits lysine-specific demethylase 1 (LSD1; Ki(inact) = 59 nM).{32531} It is 23-fold, 63-fold, and >100-fold selective for LSD-1 over monoamine oxidase (MAO) A, MAOB, and LSD2, respectively.{32531} Bizine has been shown to induce bulk histone H3 lysine 4 dimethylation in LNCaP cancer cells (EC50 = ~2 µM) and, at 0.5 µM, to protect neurons exposed to oxidative stress.{32531}
Brand:CaymanSKU:19705 -Available on backorder
Bizine is a phenelzine analog that inhibits lysine-specific demethylase 1 (LSD1; Ki(inact) = 59 nM).{32531} It is 23-fold, 63-fold, and >100-fold selective for LSD-1 over monoamine oxidase (MAO) A, MAOB, and LSD2, respectively.{32531} Bizine has been shown to induce bulk histone H3 lysine 4 dimethylation in LNCaP cancer cells (EC50 = ~2 µM) and, at 0.5 µM, to protect neurons exposed to oxidative stress.{32531}
Brand:CaymanSKU:19705 -Available on backorder
Bizine is a phenelzine analog that inhibits lysine-specific demethylase 1 (LSD1; Ki(inact) = 59 nM).{32531} It is 23-fold, 63-fold, and >100-fold selective for LSD-1 over monoamine oxidase (MAO) A, MAOB, and LSD2, respectively.{32531} Bizine has been shown to induce bulk histone H3 lysine 4 dimethylation in LNCaP cancer cells (EC50 = ~2 µM) and, at 0.5 µM, to protect neurons exposed to oxidative stress.{32531}
Brand:CaymanSKU:19705 -Available on backorder
bk-MDDMA (hydrochloride) (exempt preparation) (Item No. 22879) is a potential psychotropic designer drug of the phenethylamine, amphetamine, and cathinone chemical classes. This product is intended for forensic purposes.
Brand:CaymanSKU:22879 - 1 mgAvailable on backorder
BKT 140 is an antagonist of chemokine (C-X-C motif) receptor 4 (CXCR4; IC50 = 0.91 nM).{54472} It inhibits HIV-1-induced cytopathogenicity in MT-4 cells with an EC50 value of 4 nM. BKT 140 (100 nM) reduces migration of SUP-T1 leukemia and MDA-MB-231 breast cancer cells induced by chemokine (C-X-C) ligand 12 (CXCL12).{54472} It induces apoptosis in NB4 leukemia and RPMI-8226 multiple myeloma cancer cells when used at concentrations 8 and 40 µM.{54473} BKT 140 reduces pulmonary metastasis in an MDA-MB-231 mouse xenograft model.{54472} It also reduces the incidence of arthritis in a mouse model of collagen-induced arthritis.{54474}
Brand:CaymanSKU:30689 - 1 mgAvailable on backorder
BKT 140 is an antagonist of chemokine (C-X-C motif) receptor 4 (CXCR4; IC50 = 0.91 nM).{54472} It inhibits HIV-1-induced cytopathogenicity in MT-4 cells with an EC50 value of 4 nM. BKT 140 (100 nM) reduces migration of SUP-T1 leukemia and MDA-MB-231 breast cancer cells induced by chemokine (C-X-C) ligand 12 (CXCL12).{54472} It induces apoptosis in NB4 leukemia and RPMI-8226 multiple myeloma cancer cells when used at concentrations 8 and 40 µM.{54473} BKT 140 reduces pulmonary metastasis in an MDA-MB-231 mouse xenograft model.{54472} It also reduces the incidence of arthritis in a mouse model of collagen-induced arthritis.{54474}
Brand:CaymanSKU:30689 - 10 mgAvailable on backorder
BKT 140 is an antagonist of chemokine (C-X-C motif) receptor 4 (CXCR4; IC50 = 0.91 nM).{54472} It inhibits HIV-1-induced cytopathogenicity in MT-4 cells with an EC50 value of 4 nM. BKT 140 (100 nM) reduces migration of SUP-T1 leukemia and MDA-MB-231 breast cancer cells induced by chemokine (C-X-C) ligand 12 (CXCL12).{54472} It induces apoptosis in NB4 leukemia and RPMI-8226 multiple myeloma cancer cells when used at concentrations 8 and 40 µM.{54473} BKT 140 reduces pulmonary metastasis in an MDA-MB-231 mouse xenograft model.{54472} It also reduces the incidence of arthritis in a mouse model of collagen-induced arthritis.{54474}
Brand:CaymanSKU:30689 - 5 mgAvailable on backorder
BKT 140 is an antagonist of chemokine (C-X-C motif) receptor 4 (CXCR4; IC50 = 0.91 nM).{54472} It inhibits HIV-1-induced cytopathogenicity in MT-4 cells with an EC50 value of 4 nM. BKT 140 (100 nM) reduces migration of SUP-T1 leukemia and MDA-MB-231 breast cancer cells induced by chemokine (C-X-C) ligand 12 (CXCL12).{54472} It induces apoptosis in NB4 leukemia and RPMI-8226 multiple myeloma cancer cells when used at concentrations 8 and 40 µM.{54473} BKT 140 reduces pulmonary metastasis in an MDA-MB-231 mouse xenograft model.{54472} It also reduces the incidence of arthritis in a mouse model of collagen-induced arthritis.{54474}
Brand:CaymanSKU:30689 - 500 µgAvailable on backorder
Blasticidin A is a bacterial metabolite originally isolated from S. resistomycificus strain 2A-327.{36727} It inhibits aflatoxin production by A. parasiticus without affecting fungal growth (IC50s = 0.25 and 1.6 μM, respectively).{36728} Blasticidin A also decreases ribosomal protein levels and inhibits protein synthesis in S. cerevisiae.
Brand:CaymanSKU:25519 - 1 mgAvailable on backorder
Blasticidin A is a bacterial metabolite originally isolated from S. resistomycificus strain 2A-327.{36727} It inhibits aflatoxin production by A. parasiticus without affecting fungal growth (IC50s = 0.25 and 1.6 μM, respectively).{36728} Blasticidin A also decreases ribosomal protein levels and inhibits protein synthesis in S. cerevisiae.
Brand:CaymanSKU:25519 - 5 mgAvailable on backorder
Bleomycin is a glycopeptide antitumor antibiotic produced by the bacterium S. verticillus. Its mechanism of action causes single- and double-strand DNA breaks in tumor cells, which interrupts the cell cycle.{21617} Bleomycin is thought to achieve this by chelating metal ions, producing a pseudoenzyme that reacts with oxygen to produce superoxide and hydroxide free radicals that cleave DNA.{21617} Bleomycin has been used for the treatment of Hodgkin’s lymphoma in combination with doxorubicin, squamous cell carcinomas, testicular cancer, as well as in animal models of pulmonary fibrosis.{21618, 21616}
Brand:CaymanSKU:-Bleomycin is a glycopeptide antitumor antibiotic produced by the bacterium S. verticillus. Its mechanism of action causes single- and double-strand DNA breaks in tumor cells, which interrupts the cell cycle.{21617} Bleomycin is thought to achieve this by chelating metal ions, producing a pseudoenzyme that reacts with oxygen to produce superoxide and hydroxide free radicals that cleave DNA.{21617} Bleomycin has been used for the treatment of Hodgkin’s lymphoma in combination with doxorubicin, squamous cell carcinomas, testicular cancer, as well as in animal models of pulmonary fibrosis.{21618, 21616}
Brand:CaymanSKU:-Bleomycin is a glycopeptide antitumor antibiotic produced by the bacterium S. verticillus. Its mechanism of action causes single- and double-strand DNA breaks in tumor cells, which interrupts the cell cycle.{21617} Bleomycin is thought to achieve this by chelating metal ions, producing a pseudoenzyme that reacts with oxygen to produce superoxide and hydroxide free radicals that cleave DNA.{21617} Bleomycin has been used for the treatment of Hodgkin’s lymphoma in combination with doxorubicin, squamous cell carcinomas, testicular cancer, as well as in animal models of pulmonary fibrosis.{21618, 21616}
Brand:CaymanSKU:-Bleomycin is a glycopeptide antitumor antibiotic produced by the bacterium S. verticillus. Its mechanism of action causes single- and double-strand DNA breaks in tumor cells, which interrupts the cell cycle.{21617} Bleomycin is thought to achieve this by chelating metal ions, producing a pseudoenzyme that reacts with oxygen to produce superoxide and hydroxide free radicals that cleave DNA.{21617} Bleomycin has been used for the treatment of Hodgkin’s lymphoma in combination with doxorubicin, squamous cell carcinomas, testicular cancer, as well as in animal models of pulmonary fibrosis.{21618, 21616}
Brand:CaymanSKU:-Bleomycin A5 is one of a family of glycopeptide antibiotics first isolated from S. verticillus. As a family, the bleomycins consist of carbohydrate and metal binding domains joined to a variable C-terminal tail through a linker domain.{21617,32411} The metal binding domain and C-terminal tail mediate DNA and RNA binding that, in the presence of oxygen, generates free radicals leading to nucleic acid cleavage.{21617,32411} Bleomycin A5 has a C-terminal that mimics polyamines, facilitating its import into cells via the carnitine transporter SLC22A16.{29262} Cells expressing this transporter are ~300-fold more sensitive to bleomycin A5 than cells lacking this transporter, suggesting that cancer cells that overexpress SCL22A16 might be selectively targeted by this form of bleomycin.{29262}
Brand:CaymanSKU:19692 -Available on backorder
Bleomycin A5 is one of a family of glycopeptide antibiotics first isolated from S. verticillus. As a family, the bleomycins consist of carbohydrate and metal binding domains joined to a variable C-terminal tail through a linker domain.{21617,32411} The metal binding domain and C-terminal tail mediate DNA and RNA binding that, in the presence of oxygen, generates free radicals leading to nucleic acid cleavage.{21617,32411} Bleomycin A5 has a C-terminal that mimics polyamines, facilitating its import into cells via the carnitine transporter SLC22A16.{29262} Cells expressing this transporter are ~300-fold more sensitive to bleomycin A5 than cells lacking this transporter, suggesting that cancer cells that overexpress SCL22A16 might be selectively targeted by this form of bleomycin.{29262}
Brand:CaymanSKU:19692 -Available on backorder
Bleomycin A5 is one of a family of glycopeptide antibiotics first isolated from S. verticillus. As a family, the bleomycins consist of carbohydrate and metal binding domains joined to a variable C-terminal tail through a linker domain.{21617,32411} The metal binding domain and C-terminal tail mediate DNA and RNA binding that, in the presence of oxygen, generates free radicals leading to nucleic acid cleavage.{21617,32411} Bleomycin A5 has a C-terminal that mimics polyamines, facilitating its import into cells via the carnitine transporter SLC22A16.{29262} Cells expressing this transporter are ~300-fold more sensitive to bleomycin A5 than cells lacking this transporter, suggesting that cancer cells that overexpress SCL22A16 might be selectively targeted by this form of bleomycin.{29262}
Brand:CaymanSKU:19692 -Available on backorder
Bleomycin A5 is one of a family of glycopeptide antibiotics first isolated from S. verticillus. As a family, the bleomycins consist of carbohydrate and metal binding domains joined to a variable C-terminal tail through a linker domain.{21617,32411} The metal binding domain and C-terminal tail mediate DNA and RNA binding that, in the presence of oxygen, generates free radicals leading to nucleic acid cleavage.{21617,32411} Bleomycin A5 has a C-terminal that mimics polyamines, facilitating its import into cells via the carnitine transporter SLC22A16.{29262} Cells expressing this transporter are ~300-fold more sensitive to bleomycin A5 than cells lacking this transporter, suggesting that cancer cells that overexpress SCL22A16 might be selectively targeted by this form of bleomycin.{29262}
Brand:CaymanSKU:19692 -Available on backorder
Blinin is a diterpene originally isolated from C. blini with antiulcerogenic activity.{60084,60086} In vivo, blinin decreases gastric mucosal levels of malondialdehyde (MDA) and ulcer area in a rat model of pyloric ligation-induced ulcers.{60086}
Brand:CaymanSKU:30945 - 1 mgAvailable on backorder
Blinin is a diterpene originally isolated from C. blini with antiulcerogenic activity.{60084,60086} In vivo, blinin decreases gastric mucosal levels of malondialdehyde (MDA) and ulcer area in a rat model of pyloric ligation-induced ulcers.{60086}
Brand:CaymanSKU:30945 - 10 mgAvailable on backorder
Blinin is a diterpene originally isolated from C. blini with antiulcerogenic activity.{60084,60086} In vivo, blinin decreases gastric mucosal levels of malondialdehyde (MDA) and ulcer area in a rat model of pyloric ligation-induced ulcers.{60086}
Brand:CaymanSKU:30945 - 5 mgAvailable on backorder
Blinin is a diterpene originally isolated from C. blini with antiulcerogenic activity.{60084,60086} In vivo, blinin decreases gastric mucosal levels of malondialdehyde (MDA) and ulcer area in a rat model of pyloric ligation-induced ulcers.{60086}
Brand:CaymanSKU:30945 - 500 µgAvailable on backorder
Blonanserin is a 4-phenyl-2-(1-piperazinyl) pyridine that acts as an antagonist at dopamine D2, D3, and serotonin 5-HT2A receptors (Kis = 0.14, 0.49, and 0.81 nM, respectively).{26905} It binds to 5-HT6 with a Ki value of 11.7 nM and demonstrates relatively low affinity for 5-HT2C (Ki = 26.4 nM), adrenergic α1 (Ki = 26.7 nM), histamine H1 (Ki = 765 nM), and muscarinic M1 receptors (Ki = 100 nM).{26905} Blonanserin was developed in Japan as a novel antipsychotic that displays 20- and 94-fold higher affinity for D2 receptors compared to haloperidol (Item No. 12014) and risperidone (Item No. 13629), respectively.{26905}
Brand:CaymanSKU:-Out of stock
Blonanserin is a 4-phenyl-2-(1-piperazinyl) pyridine that acts as an antagonist at dopamine D2, D3, and serotonin 5-HT2A receptors (Kis = 0.14, 0.49, and 0.81 nM, respectively).{26905} It binds to 5-HT6 with a Ki value of 11.7 nM and demonstrates relatively low affinity for 5-HT2C (Ki = 26.4 nM), adrenergic α1 (Ki = 26.7 nM), histamine H1 (Ki = 765 nM), and muscarinic M1 receptors (Ki = 100 nM).{26905} Blonanserin was developed in Japan as a novel antipsychotic that displays 20- and 94-fold higher affinity for D2 receptors compared to haloperidol (Item No. 12014) and risperidone (Item No. 13629), respectively.{26905}
Brand:CaymanSKU:-Out of stock
Blonanserin is a 4-phenyl-2-(1-piperazinyl) pyridine that acts as an antagonist at dopamine D2, D3, and serotonin 5-HT2A receptors (Kis = 0.14, 0.49, and 0.81 nM, respectively).{26905} It binds to 5-HT6 with a Ki value of 11.7 nM and demonstrates relatively low affinity for 5-HT2C (Ki = 26.4 nM), adrenergic α1 (Ki = 26.7 nM), histamine H1 (Ki = 765 nM), and muscarinic M1 receptors (Ki = 100 nM).{26905} Blonanserin was developed in Japan as a novel antipsychotic that displays 20- and 94-fold higher affinity for D2 receptors compared to haloperidol (Item No. 12014) and risperidone (Item No. 13629), respectively.{26905}
Brand:CaymanSKU:-Out of stock
Blonanserin is a 4-phenyl-2-(1-piperazinyl) pyridine that acts as an antagonist at dopamine D2, D3, and serotonin 5-HT2A receptors (Kis = 0.14, 0.49, and 0.81 nM, respectively).{26905} It binds to 5-HT6 with a Ki value of 11.7 nM and demonstrates relatively low affinity for 5-HT2C (Ki = 26.4 nM), adrenergic α1 (Ki = 26.7 nM), histamine H1 (Ki = 765 nM), and muscarinic M1 receptors (Ki = 100 nM).{26905} Blonanserin was developed in Japan as a novel antipsychotic that displays 20- and 94-fold higher affinity for D2 receptors compared to haloperidol (Item No. 12014) and risperidone (Item No. 13629), respectively.{26905}
Brand:CaymanSKU:-Out of stock
BLU-285 is a dual inhibitor of KIT receptor and platelet-derived growth factor receptor α (PDGFRα) tyrosine kinases with activating loop mutations (IC50s = 0.27 and 0.24 nM for KITD816V and PDGFRαD842V, respectively).{40523} It is >150-fold selective for KITD816V and PDGFRαD842V over a kinase panel at a concentration of 3 μM. BLU-285 also has activity against a panel of KIT and PDGFRα loop mutants identified in patients with gastrointestinal stromal tumors (GISTs; IC50s = D814Y mastocytoma allograft mouse model and a GIST patient-derived mouse xenograft model in a dose-dependent manner. Formulations containing BLU-285 have been used to treat KIT- and PDGFRα-driven malignancies.
Brand:CaymanSKU:22985 - 1 mgAvailable on backorder
BLU-285 is a dual inhibitor of KIT receptor and platelet-derived growth factor receptor α (PDGFRα) tyrosine kinases with activating loop mutations (IC50s = 0.27 and 0.24 nM for KITD816V and PDGFRαD842V, respectively).{40523} It is >150-fold selective for KITD816V and PDGFRαD842V over a kinase panel at a concentration of 3 μM. BLU-285 also has activity against a panel of KIT and PDGFRα loop mutants identified in patients with gastrointestinal stromal tumors (GISTs; IC50s = D814Y mastocytoma allograft mouse model and a GIST patient-derived mouse xenograft model in a dose-dependent manner. Formulations containing BLU-285 have been used to treat KIT- and PDGFRα-driven malignancies.
Brand:CaymanSKU:22985 - 10 mgAvailable on backorder
BLU-285 is a dual inhibitor of KIT receptor and platelet-derived growth factor receptor α (PDGFRα) tyrosine kinases with activating loop mutations (IC50s = 0.27 and 0.24 nM for KITD816V and PDGFRαD842V, respectively).{40523} It is >150-fold selective for KITD816V and PDGFRαD842V over a kinase panel at a concentration of 3 μM. BLU-285 also has activity against a panel of KIT and PDGFRα loop mutants identified in patients with gastrointestinal stromal tumors (GISTs; IC50s = D814Y mastocytoma allograft mouse model and a GIST patient-derived mouse xenograft model in a dose-dependent manner. Formulations containing BLU-285 have been used to treat KIT- and PDGFRα-driven malignancies.
Brand:CaymanSKU:22985 - 25 mgAvailable on backorder
BLU-285 is a dual inhibitor of KIT receptor and platelet-derived growth factor receptor α (PDGFRα) tyrosine kinases with activating loop mutations (IC50s = 0.27 and 0.24 nM for KITD816V and PDGFRαD842V, respectively).{40523} It is >150-fold selective for KITD816V and PDGFRαD842V over a kinase panel at a concentration of 3 μM. BLU-285 also has activity against a panel of KIT and PDGFRα loop mutants identified in patients with gastrointestinal stromal tumors (GISTs; IC50s = D814Y mastocytoma allograft mouse model and a GIST patient-derived mouse xenograft model in a dose-dependent manner. Formulations containing BLU-285 have been used to treat KIT- and PDGFRα-driven malignancies.
Brand:CaymanSKU:22985 - 5 mgAvailable on backorder
BLU-554 is a potent inhibitor of recombinant fibroblast growth factor receptor 4 (FGFR4; IC50 50 < 10 nM), a marker of FGFR4 inhibition, in MDA-MB-453 breast cancer cells.
Brand:CaymanSKU:22438 -Out of stock
BLU-554 is a potent inhibitor of recombinant fibroblast growth factor receptor 4 (FGFR4; IC50 50 < 10 nM), a marker of FGFR4 inhibition, in MDA-MB-453 breast cancer cells.
Brand:CaymanSKU:22438 -Out of stock
BLU-554 is a potent inhibitor of recombinant fibroblast growth factor receptor 4 (FGFR4; IC50 50 < 10 nM), a marker of FGFR4 inhibition, in MDA-MB-453 breast cancer cells.
Brand:CaymanSKU:22438 -Out of stock
BLU-554 is a potent inhibitor of recombinant fibroblast growth factor receptor 4 (FGFR4; IC50 50 < 10 nM), a marker of FGFR4 inhibition, in MDA-MB-453 breast cancer cells.
Brand:CaymanSKU:22438 -Out of stock
Fibroblast growth factor receptor 4 (FGFR4) is the receptor for fibroblast growth factor 19 (FGF19), which is a tightly controlled hormone that regulates bile acid synthesis and hepatocyte proliferation in the normal liver. Aberrant signaling through the FGFR4/FGF19 signaling complex has been implicated in hepatocellular carcinoma (HCC).{30600} BLU-9931 is a small molecule inhibitor of FGFR4 (IC50 = 3 nM) that is selective for FGFR4 over other FGFR family members (IC50s = 591, 493, and 150 nM for FGFR1, 2, and 3, respectively) and an extensive panel of additional kinases (selectivity score for BLU-9931 at 3 µM is 0.005).{30600} It inhibits proliferation of HCC cell lines with an activated FGFR4 signaling pathway (EC50s = 0.02-0.11 µM) and demonstrates antitumor activity when administered orally at 100 mg/kg to mice bearing HCC xenografts that overexpresses FGF19 due to amplification or to mice bearing liver tumor xenografts that overexpresses FGF19 mRNA but lack FGF19 amplification.{30600}
Brand:CaymanSKU:-Available on backorder
Fibroblast growth factor receptor 4 (FGFR4) is the receptor for fibroblast growth factor 19 (FGF19), which is a tightly controlled hormone that regulates bile acid synthesis and hepatocyte proliferation in the normal liver. Aberrant signaling through the FGFR4/FGF19 signaling complex has been implicated in hepatocellular carcinoma (HCC).{30600} BLU-9931 is a small molecule inhibitor of FGFR4 (IC50 = 3 nM) that is selective for FGFR4 over other FGFR family members (IC50s = 591, 493, and 150 nM for FGFR1, 2, and 3, respectively) and an extensive panel of additional kinases (selectivity score for BLU-9931 at 3 µM is 0.005).{30600} It inhibits proliferation of HCC cell lines with an activated FGFR4 signaling pathway (EC50s = 0.02-0.11 µM) and demonstrates antitumor activity when administered orally at 100 mg/kg to mice bearing HCC xenografts that overexpresses FGF19 due to amplification or to mice bearing liver tumor xenografts that overexpresses FGF19 mRNA but lack FGF19 amplification.{30600}
Brand:CaymanSKU:-Available on backorder
Fibroblast growth factor receptor 4 (FGFR4) is the receptor for fibroblast growth factor 19 (FGF19), which is a tightly controlled hormone that regulates bile acid synthesis and hepatocyte proliferation in the normal liver. Aberrant signaling through the FGFR4/FGF19 signaling complex has been implicated in hepatocellular carcinoma (HCC).{30600} BLU-9931 is a small molecule inhibitor of FGFR4 (IC50 = 3 nM) that is selective for FGFR4 over other FGFR family members (IC50s = 591, 493, and 150 nM for FGFR1, 2, and 3, respectively) and an extensive panel of additional kinases (selectivity score for BLU-9931 at 3 µM is 0.005).{30600} It inhibits proliferation of HCC cell lines with an activated FGFR4 signaling pathway (EC50s = 0.02-0.11 µM) and demonstrates antitumor activity when administered orally at 100 mg/kg to mice bearing HCC xenografts that overexpresses FGF19 due to amplification or to mice bearing liver tumor xenografts that overexpresses FGF19 mRNA but lack FGF19 amplification.{30600}
Brand:CaymanSKU:-Available on backorder
Fibroblast growth factor receptor 4 (FGFR4) is the receptor for fibroblast growth factor 19 (FGF19), which is a tightly controlled hormone that regulates bile acid synthesis and hepatocyte proliferation in the normal liver. Aberrant signaling through the FGFR4/FGF19 signaling complex has been implicated in hepatocellular carcinoma (HCC).{30600} BLU-9931 is a small molecule inhibitor of FGFR4 (IC50 = 3 nM) that is selective for FGFR4 over other FGFR family members (IC50s = 591, 493, and 150 nM for FGFR1, 2, and 3, respectively) and an extensive panel of additional kinases (selectivity score for BLU-9931 at 3 µM is 0.005).{30600} It inhibits proliferation of HCC cell lines with an activated FGFR4 signaling pathway (EC50s = 0.02-0.11 µM) and demonstrates antitumor activity when administered orally at 100 mg/kg to mice bearing HCC xenografts that overexpresses FGF19 due to amplification or to mice bearing liver tumor xenografts that overexpresses FGF19 mRNA but lack FGF19 amplification.{30600}
Brand:CaymanSKU:-Available on backorder
BLX3887 is an inhibitor of 15-lipoxygenase type 1 (15-LO-1; IC50 = 32 nM in a cell-free enzyme assay).{35444} It is selective for 15-LO-1 over 15-LO-2, which it does not inhibit, 5-LO (IC50 = 472 nM), and 12-LO (IC50 = 3,310 nM). BLX3887 inhibits the production of 15-LO metabolites selectively in eosinophils over neutrophils when used at a concentration of 10 µM. It also inhibits endocytosis in, and the migration of, isolated human peripheral blood mononuclear cell-derived dendritic cells in vitro.
Brand:CaymanSKU:27391 - 1 mgAvailable on backorder
BLX3887 is an inhibitor of 15-lipoxygenase type 1 (15-LO-1; IC50 = 32 nM in a cell-free enzyme assay).{35444} It is selective for 15-LO-1 over 15-LO-2, which it does not inhibit, 5-LO (IC50 = 472 nM), and 12-LO (IC50 = 3,310 nM). BLX3887 inhibits the production of 15-LO metabolites selectively in eosinophils over neutrophils when used at a concentration of 10 µM. It also inhibits endocytosis in, and the migration of, isolated human peripheral blood mononuclear cell-derived dendritic cells in vitro.
Brand:CaymanSKU:27391 - 10 mgAvailable on backorder
BLX3887 is an inhibitor of 15-lipoxygenase type 1 (15-LO-1; IC50 = 32 nM in a cell-free enzyme assay).{35444} It is selective for 15-LO-1 over 15-LO-2, which it does not inhibit, 5-LO (IC50 = 472 nM), and 12-LO (IC50 = 3,310 nM). BLX3887 inhibits the production of 15-LO metabolites selectively in eosinophils over neutrophils when used at a concentration of 10 µM. It also inhibits endocytosis in, and the migration of, isolated human peripheral blood mononuclear cell-derived dendritic cells in vitro.
Brand:CaymanSKU:27391 - 5 mgAvailable on backorder
BLX3887 is an inhibitor of 15-lipoxygenase type 1 (15-LO-1; IC50 = 32 nM in a cell-free enzyme assay).{35444} It is selective for 15-LO-1 over 15-LO-2, which it does not inhibit, 5-LO (IC50 = 472 nM), and 12-LO (IC50 = 3,310 nM). BLX3887 inhibits the production of 15-LO metabolites selectively in eosinophils over neutrophils when used at a concentration of 10 µM. It also inhibits endocytosis in, and the migration of, isolated human peripheral blood mononuclear cell-derived dendritic cells in vitro.
Brand:CaymanSKU:27391 - 500 µgAvailable on backorder
BLZ-945 is a selective inhibitor of the colony stimulating factor 1 receptor (CSF1R) with an IC50 value of 1 nM.{31423} It is more than 1,000-fold selective against its closest receptor tyrosine kinase homologs.{31423} It has been shown to inhibit CSF1-dependent proliferation with an EC50 value of 67 nM in bone marrow-derived macrophages.{31423} In glioma-bearing mice, CSF1R inhibition via BLZ-945 can block tumor progression and significantly improve survival.{31423} At 200 mg/kg, BLZ-945 decreased the growth of malignant cells in a mouse mammary tumor virus-driven polyomavirus middle T antigen model of mammary carcinogenesis and in a keratin 14-expressing human papillomavirus type 16 transgenic model of cervical carcinogenesis.{31424}
Brand:CaymanSKU:19626 -Available on backorder
BLZ-945 is a selective inhibitor of the colony stimulating factor 1 receptor (CSF1R) with an IC50 value of 1 nM.{31423} It is more than 1,000-fold selective against its closest receptor tyrosine kinase homologs.{31423} It has been shown to inhibit CSF1-dependent proliferation with an EC50 value of 67 nM in bone marrow-derived macrophages.{31423} In glioma-bearing mice, CSF1R inhibition via BLZ-945 can block tumor progression and significantly improve survival.{31423} At 200 mg/kg, BLZ-945 decreased the growth of malignant cells in a mouse mammary tumor virus-driven polyomavirus middle T antigen model of mammary carcinogenesis and in a keratin 14-expressing human papillomavirus type 16 transgenic model of cervical carcinogenesis.{31424}
Brand:CaymanSKU:19626 -Available on backorder
BLZ-945 is a selective inhibitor of the colony stimulating factor 1 receptor (CSF1R) with an IC50 value of 1 nM.{31423} It is more than 1,000-fold selective against its closest receptor tyrosine kinase homologs.{31423} It has been shown to inhibit CSF1-dependent proliferation with an EC50 value of 67 nM in bone marrow-derived macrophages.{31423} In glioma-bearing mice, CSF1R inhibition via BLZ-945 can block tumor progression and significantly improve survival.{31423} At 200 mg/kg, BLZ-945 decreased the growth of malignant cells in a mouse mammary tumor virus-driven polyomavirus middle T antigen model of mammary carcinogenesis and in a keratin 14-expressing human papillomavirus type 16 transgenic model of cervical carcinogenesis.{31424}
Brand:CaymanSKU:19626 -Available on backorder
BLZ-945 is a selective inhibitor of the colony stimulating factor 1 receptor (CSF1R) with an IC50 value of 1 nM.{31423} It is more than 1,000-fold selective against its closest receptor tyrosine kinase homologs.{31423} It has been shown to inhibit CSF1-dependent proliferation with an EC50 value of 67 nM in bone marrow-derived macrophages.{31423} In glioma-bearing mice, CSF1R inhibition via BLZ-945 can block tumor progression and significantly improve survival.{31423} At 200 mg/kg, BLZ-945 decreased the growth of malignant cells in a mouse mammary tumor virus-driven polyomavirus middle T antigen model of mammary carcinogenesis and in a keratin 14-expressing human papillomavirus type 16 transgenic model of cervical carcinogenesis.{31424}
Brand:CaymanSKU:19626 -Available on backorder
Thromboxane A2 (TXA2) is a potent thrombogenic and vasoconstrictor eicosanoid, produced in large quantities by activated platelets. TXA2 has been implicated as a causal factor in the onset of stroke and myocardial infarction. BM 567 is a dual acting antithrombogenic agent, acting as an inhibitor of thromboxane A2 (TXA2) synthase and as an antagonist of the TP receptor, the G protein-coupled receptor mediating TXA2 activity in platelets and vascular smooth muscle. BM 567 antagonizes the vascular smooth muscle TP receptor with an IC50 value of 1.1 nM. It inhibits platelet TX synthase with an IC50 value of 12 nM.{12979}
Brand:CaymanSKU:10155 - 1 mgAvailable on backorder
Thromboxane A2 (TXA2) is a potent thrombogenic and vasoconstrictor eicosanoid, produced in large quantities by activated platelets. TXA2 has been implicated as a causal factor in the onset of stroke and myocardial infarction. BM 567 is a dual acting antithrombogenic agent, acting as an inhibitor of thromboxane A2 (TXA2) synthase and as an antagonist of the TP receptor, the G protein-coupled receptor mediating TXA2 activity in platelets and vascular smooth muscle. BM 567 antagonizes the vascular smooth muscle TP receptor with an IC50 value of 1.1 nM. It inhibits platelet TX synthase with an IC50 value of 12 nM.{12979}
Brand:CaymanSKU:10155 - 10 mgAvailable on backorder
Thromboxane A2 (TXA2) is a potent thrombogenic and vasoconstrictor eicosanoid, produced in large quantities by activated platelets. TXA2 has been implicated as a causal factor in the onset of stroke and myocardial infarction. BM 567 is a dual acting antithrombogenic agent, acting as an inhibitor of thromboxane A2 (TXA2) synthase and as an antagonist of the TP receptor, the G protein-coupled receptor mediating TXA2 activity in platelets and vascular smooth muscle. BM 567 antagonizes the vascular smooth muscle TP receptor with an IC50 value of 1.1 nM. It inhibits platelet TX synthase with an IC50 value of 12 nM.{12979}
Brand:CaymanSKU:10155 - 5 mgAvailable on backorder
BM212 is an antimycobacterial compound.{37196} It inhibits the growth of laboratory and clinical isolate M. tuberculosis strains (MICs = 0.7-1.5 μg/ml), including strains resistant to ethambutol (Item No. 23713), isoniazid (Item No. 20378), rifampicin (Item No. 14423), and rifabutin (Item No. 16468). BM212 also inhibits the growth of M. fortuitum, M. smegmatis, M. kansasii, and M. avium strains (MICs = 3.1-12.5, 3.1-25, 3.1-6.2, and 0.4-3.1 μg/ml, respectively). It inhibits replication of intracellular M. tuberculosis in infected U937 macrophages in a dose-dependent manner at concentrations ranging from 0.5-10 μg/ml. Some M. smegmatis, M. bovis BCG, and M. tuberculosis H37Rv mutant strains carry mutations in the mycobacterium membrane protein large 3 (mmpL3) gene and are resistant to BM212, indicating mmpL3 is likely a cellular target of BM212.{37197}
Brand:CaymanSKU:22986 - 1 mgAvailable on backorder
BM212 is an antimycobacterial compound.{37196} It inhibits the growth of laboratory and clinical isolate M. tuberculosis strains (MICs = 0.7-1.5 μg/ml), including strains resistant to ethambutol (Item No. 23713), isoniazid (Item No. 20378), rifampicin (Item No. 14423), and rifabutin (Item No. 16468). BM212 also inhibits the growth of M. fortuitum, M. smegmatis, M. kansasii, and M. avium strains (MICs = 3.1-12.5, 3.1-25, 3.1-6.2, and 0.4-3.1 μg/ml, respectively). It inhibits replication of intracellular M. tuberculosis in infected U937 macrophages in a dose-dependent manner at concentrations ranging from 0.5-10 μg/ml. Some M. smegmatis, M. bovis BCG, and M. tuberculosis H37Rv mutant strains carry mutations in the mycobacterium membrane protein large 3 (mmpL3) gene and are resistant to BM212, indicating mmpL3 is likely a cellular target of BM212.{37197}
Brand:CaymanSKU:22986 - 10 mgAvailable on backorder
BM212 is an antimycobacterial compound.{37196} It inhibits the growth of laboratory and clinical isolate M. tuberculosis strains (MICs = 0.7-1.5 μg/ml), including strains resistant to ethambutol (Item No. 23713), isoniazid (Item No. 20378), rifampicin (Item No. 14423), and rifabutin (Item No. 16468). BM212 also inhibits the growth of M. fortuitum, M. smegmatis, M. kansasii, and M. avium strains (MICs = 3.1-12.5, 3.1-25, 3.1-6.2, and 0.4-3.1 μg/ml, respectively). It inhibits replication of intracellular M. tuberculosis in infected U937 macrophages in a dose-dependent manner at concentrations ranging from 0.5-10 μg/ml. Some M. smegmatis, M. bovis BCG, and M. tuberculosis H37Rv mutant strains carry mutations in the mycobacterium membrane protein large 3 (mmpL3) gene and are resistant to BM212, indicating mmpL3 is likely a cellular target of BM212.{37197}
Brand:CaymanSKU:22986 - 5 mgAvailable on backorder
BMDB (hydrochloride) (Item No. 24062) is an analytical reference standard categorized as a cathinone.{50425} This product is intended for research and forensic applications.
Brand:CaymanSKU:24062 - 1 mgAvailable on backorder
BMDB (hydrochloride) (Item No. 24062) is an analytical reference standard categorized as a cathinone.{50425} This product is intended for research and forensic applications.
Brand:CaymanSKU:24062 - 5 mgAvailable on backorder
BMH-21 is an inhibitor of RNA polymerase I.{41313} It binds to GC-rich sequences in DNA and ribosomal DNA (rDNA) and inhibits RNA polymerase I transcription in vitro. It inhibits expression of the 47S rRNA transcript (IC50 = 60 nM), disrupts the structure of the nucleolus, and leads to removal of the RNA polymerase complex from rDNA by inducing dissociation and destruction of RPA194 through a proteasome-dependent mechanism. BMH-21 also activates p53 in the nanomolar range.{41312} It reduces viability of several cancer cell lines but not of non-cancerous cells (IC50s = 0.7, 1.9, ≥40, and 2.7 µM for A375, human diploid fibroblasts, primary human melanocytes, and HIMEC cells, respectively). BMH-21 intercalates with DNA but does not induce DNA damage via the ataxia-telangiectasia mutated (ATM) kinase pathway. BMH-21 (25 mg/kg) inhibits tumor growth in melanoma and colon cancer mouse xenograft models.{41313}
Brand:CaymanSKU:22282 -Out of stock
BMH-21 is an inhibitor of RNA polymerase I.{41313} It binds to GC-rich sequences in DNA and ribosomal DNA (rDNA) and inhibits RNA polymerase I transcription in vitro. It inhibits expression of the 47S rRNA transcript (IC50 = 60 nM), disrupts the structure of the nucleolus, and leads to removal of the RNA polymerase complex from rDNA by inducing dissociation and destruction of RPA194 through a proteasome-dependent mechanism. BMH-21 also activates p53 in the nanomolar range.{41312} It reduces viability of several cancer cell lines but not of non-cancerous cells (IC50s = 0.7, 1.9, ≥40, and 2.7 µM for A375, human diploid fibroblasts, primary human melanocytes, and HIMEC cells, respectively). BMH-21 intercalates with DNA but does not induce DNA damage via the ataxia-telangiectasia mutated (ATM) kinase pathway. BMH-21 (25 mg/kg) inhibits tumor growth in melanoma and colon cancer mouse xenograft models.{41313}
Brand:CaymanSKU:22282 -Out of stock
BMH-21 is an inhibitor of RNA polymerase I.{41313} It binds to GC-rich sequences in DNA and ribosomal DNA (rDNA) and inhibits RNA polymerase I transcription in vitro. It inhibits expression of the 47S rRNA transcript (IC50 = 60 nM), disrupts the structure of the nucleolus, and leads to removal of the RNA polymerase complex from rDNA by inducing dissociation and destruction of RPA194 through a proteasome-dependent mechanism. BMH-21 also activates p53 in the nanomolar range.{41312} It reduces viability of several cancer cell lines but not of non-cancerous cells (IC50s = 0.7, 1.9, ≥40, and 2.7 µM for A375, human diploid fibroblasts, primary human melanocytes, and HIMEC cells, respectively). BMH-21 intercalates with DNA but does not induce DNA damage via the ataxia-telangiectasia mutated (ATM) kinase pathway. BMH-21 (25 mg/kg) inhibits tumor growth in melanoma and colon cancer mouse xenograft models.{41313}
Brand:CaymanSKU:22282 -Out of stock
BMK ethyl glycidate (Item No. 9002713) is an analytical reference standard that is categorized as a precursor to phenylacetone (Item Nos. 16103 and 16444). Phenylacetone has been used as a precursor in the illicit synthesis of methamphetamine and amphetamine and is classified as a schedule II controlled substance in the United States.{30927,26603,26602} This product is intended for forensic and research applications.
Brand:CaymanSKU:9002713 - 10 mgAvailable on backorder
BMK ethyl glycidate (Item No. 9002713) is an analytical reference standard that is categorized as a precursor to phenylacetone (Item Nos. 16103 and 16444). Phenylacetone has been used as a precursor in the illicit synthesis of methamphetamine and amphetamine and is classified as a schedule II controlled substance in the United States.{30927,26603,26602} This product is intended for forensic and research applications.
Brand:CaymanSKU:9002713 - 5 mgAvailable on backorder
BMK ethyl glycidate (Item No. 9002713) is an analytical reference standard that is categorized as a precursor to phenylacetone (Item Nos. 16103 and 16444). Phenylacetone has been used as a precursor in the illicit synthesis of methamphetamine and amphetamine and is classified as a schedule II controlled substance in the United States.{30927,26603,26602} This product is intended for forensic and research applications.
Brand:CaymanSKU:9002713 - 50 mgAvailable on backorder
BMK glycidic acid (Item No. 19682) is an analytical reference standard that is categorized as a precursor to the production of phenylacetone (Item Nos. 16103 | 16444). Phenylacetone has been used as a precursor in the illicit synthesis of methamphetamine and amphetamine and is classified as a schedule II controlled substance in the United States.{30927,26603,26602} This product is intended for forensic and research applications.
Brand:CaymanSKU:19682 -Available on backorder
BMK glycidic acid (Item No. 19682) is an analytical reference standard that is categorized as a precursor to the production of phenylacetone (Item Nos. 16103 | 16444). Phenylacetone has been used as a precursor in the illicit synthesis of methamphetamine and amphetamine and is classified as a schedule II controlled substance in the United States.{30927,26603,26602} This product is intended for forensic and research applications.
Brand:CaymanSKU:19682 -Available on backorder
BMK methyl glycidate (Item No. 9002714) is an analytical reference standard that is categorized as a precursor to phenylacetone (Item Nos. 16103 and 16444). Phenylacetone has been used as a precursor in the illicit synthesis of methamphetamine and amphetamine and is classified as a schedule II controlled substance in the United States.{30927,26603,26602} This product is intended for forensic and research applications.
Brand:CaymanSKU:9002714 - 10 mgAvailable on backorder
BMK methyl glycidate (Item No. 9002714) is an analytical reference standard that is categorized as a precursor to phenylacetone (Item Nos. 16103 and 16444). Phenylacetone has been used as a precursor in the illicit synthesis of methamphetamine and amphetamine and is classified as a schedule II controlled substance in the United States.{30927,26603,26602} This product is intended for forensic and research applications.
Brand:CaymanSKU:9002714 - 5 mgAvailable on backorder
BMK methyl glycidate (Item No. 9002714) is an analytical reference standard that is categorized as a precursor to phenylacetone (Item Nos. 16103 and 16444). Phenylacetone has been used as a precursor in the illicit synthesis of methamphetamine and amphetamine and is classified as a schedule II controlled substance in the United States.{30927,26603,26602} This product is intended for forensic and research applications.
Brand:CaymanSKU:9002714 - 50 mgAvailable on backorder
Inhibition of histone deacetylase (HDAC) enzymes by compounds such as trichostatin A can have wide ranging effects in cancer, cell differentiation, and other aspects of gene expression regulation.{10663} BML-210 is a small molecule inhibitor of HDAC with an IC50 value of 30 µM when tested in HeLa cell nuclear extracts using 200 µM acetylated fluorometric substrate{14835} (substrate available in Cayman’s HDAC Activity and Inhibitor Screening Assay Kits – Item Nos. 10011563 and 10011564).
Brand:CaymanSKU:10005019 - 1 mgAvailable on backorder
Inhibition of histone deacetylase (HDAC) enzymes by compounds such as trichostatin A can have wide ranging effects in cancer, cell differentiation, and other aspects of gene expression regulation.{10663} BML-210 is a small molecule inhibitor of HDAC with an IC50 value of 30 µM when tested in HeLa cell nuclear extracts using 200 µM acetylated fluorometric substrate{14835} (substrate available in Cayman’s HDAC Activity and Inhibitor Screening Assay Kits – Item Nos. 10011563 and 10011564).
Brand:CaymanSKU:10005019 - 10 mgAvailable on backorder
Inhibition of histone deacetylase (HDAC) enzymes by compounds such as trichostatin A can have wide ranging effects in cancer, cell differentiation, and other aspects of gene expression regulation.{10663} BML-210 is a small molecule inhibitor of HDAC with an IC50 value of 30 µM when tested in HeLa cell nuclear extracts using 200 µM acetylated fluorometric substrate{14835} (substrate available in Cayman’s HDAC Activity and Inhibitor Screening Assay Kits – Item Nos. 10011563 and 10011564).
Brand:CaymanSKU:10005019 - 25 mgAvailable on backorder
Inhibition of histone deacetylase (HDAC) enzymes by compounds such as trichostatin A can have wide ranging effects in cancer, cell differentiation, and other aspects of gene expression regulation.{10663} BML-210 is a small molecule inhibitor of HDAC with an IC50 value of 30 µM when tested in HeLa cell nuclear extracts using 200 µM acetylated fluorometric substrate{14835} (substrate available in Cayman’s HDAC Activity and Inhibitor Screening Assay Kits – Item Nos. 10011563 and 10011564).
Brand:CaymanSKU:10005019 - 5 mgAvailable on backorder
BML-278 is an activator of sirtuin 1 (SIRT1) that has an EC150 value (effective concentration able to increase the enzyme by 150%) of 1 µM.{34113} It less potently activates SIRT2 and SIRT3 (EC150s = 25 and 50 µM, respectively).{34113} BML-278 induces hypoacetylation on α-tubulin in U937 cells that are pretreated with SAHA (Item No. 10009929), a histone deacetylase inhibitor. It arrests cell cycling at the G1/S phase, reduces senescence in primary human mesenchymal cells, and significantly increases mitochondrial density in murine C2C12 myoblasts.{34113}
Brand:CaymanSKU:20209 -Available on backorder
BML-278 is an activator of sirtuin 1 (SIRT1) that has an EC150 value (effective concentration able to increase the enzyme by 150%) of 1 µM.{34113} It less potently activates SIRT2 and SIRT3 (EC150s = 25 and 50 µM, respectively).{34113} BML-278 induces hypoacetylation on α-tubulin in U937 cells that are pretreated with SAHA (Item No. 10009929), a histone deacetylase inhibitor. It arrests cell cycling at the G1/S phase, reduces senescence in primary human mesenchymal cells, and significantly increases mitochondrial density in murine C2C12 myoblasts.{34113}
Brand:CaymanSKU:20209 -Available on backorder
BML-278 is an activator of sirtuin 1 (SIRT1) that has an EC150 value (effective concentration able to increase the enzyme by 150%) of 1 µM.{34113} It less potently activates SIRT2 and SIRT3 (EC150s = 25 and 50 µM, respectively).{34113} BML-278 induces hypoacetylation on α-tubulin in U937 cells that are pretreated with SAHA (Item No. 10009929), a histone deacetylase inhibitor. It arrests cell cycling at the G1/S phase, reduces senescence in primary human mesenchymal cells, and significantly increases mitochondrial density in murine C2C12 myoblasts.{34113}
Brand:CaymanSKU:20209 -Available on backorder
BML-278 is an activator of sirtuin 1 (SIRT1) that has an EC150 value (effective concentration able to increase the enzyme by 150%) of 1 µM.{34113} It less potently activates SIRT2 and SIRT3 (EC150s = 25 and 50 µM, respectively).{34113} BML-278 induces hypoacetylation on α-tubulin in U937 cells that are pretreated with SAHA (Item No. 10009929), a histone deacetylase inhibitor. It arrests cell cycling at the G1/S phase, reduces senescence in primary human mesenchymal cells, and significantly increases mitochondrial density in murine C2C12 myoblasts.{34113}
Brand:CaymanSKU:20209 -Available on backorder
BMN 673 is an orally available poly(ADP-ribose) polymerase (PARP) inhibitor with an IC50 value of 0.57 nM.{32032} It similarly binds to PARP1 and PARP2 with Ki values of 1.2 and 0.85 nM, respectively, but has no effect on PARG.{32032} BMN 673 selectively targets tumor cells with BRCA1, BRCA2, or PTEN gene mutations and elicits antitumor activity in xenografted tumors in mice.{32032}
Brand:CaymanSKU:19782 -Available on backorder
BMN 673 is an orally available poly(ADP-ribose) polymerase (PARP) inhibitor with an IC50 value of 0.57 nM.{32032} It similarly binds to PARP1 and PARP2 with Ki values of 1.2 and 0.85 nM, respectively, but has no effect on PARG.{32032} BMN 673 selectively targets tumor cells with BRCA1, BRCA2, or PTEN gene mutations and elicits antitumor activity in xenografted tumors in mice.{32032}
Brand:CaymanSKU:19782 -Available on backorder
BMN 673 is an orally available poly(ADP-ribose) polymerase (PARP) inhibitor with an IC50 value of 0.57 nM.{32032} It similarly binds to PARP1 and PARP2 with Ki values of 1.2 and 0.85 nM, respectively, but has no effect on PARG.{32032} BMN 673 selectively targets tumor cells with BRCA1, BRCA2, or PTEN gene mutations and elicits antitumor activity in xenografted tumors in mice.{32032}
Brand:CaymanSKU:19782 -Available on backorder
BMN 673 is an orally available poly(ADP-ribose) polymerase (PARP) inhibitor with an IC50 value of 0.57 nM.{32032} It similarly binds to PARP1 and PARP2 with Ki values of 1.2 and 0.85 nM, respectively, but has no effect on PARG.{32032} BMN 673 selectively targets tumor cells with BRCA1, BRCA2, or PTEN gene mutations and elicits antitumor activity in xenografted tumors in mice.{32032}
Brand:CaymanSKU:19782 -Available on backorder
BMP-22 is an inhibitor of autotaxin (IC50 = 170 nM).{35710} It is selective for autotaxin over the phosphodiesterases NPP6 and NPP7 at 10 μM. BMP-22 (0.1-1,000 nM) inhibits autotaxin-mediated production of lysophosphatidic acid (LPA) from lysophosphatidylcholine (LPC; Item No. 24331) in vitro in a concentration-dependent manner. It inhibits LPC-dependent MM1 cell invasion of a human umbilical vein endothelial cell (HUVEC) monolayer. BMP-22 (0.5 mg/kg per day) decreases the number of lung metastatic foci in a B16/F10 syngeneic mouse melanoma model of lung metastasis.
Brand:CaymanSKU:27264 - 1 mgAvailable on backorder
BMP-22 is an inhibitor of autotaxin (IC50 = 170 nM).{35710} It is selective for autotaxin over the phosphodiesterases NPP6 and NPP7 at 10 μM. BMP-22 (0.1-1,000 nM) inhibits autotaxin-mediated production of lysophosphatidic acid (LPA) from lysophosphatidylcholine (LPC; Item No. 24331) in vitro in a concentration-dependent manner. It inhibits LPC-dependent MM1 cell invasion of a human umbilical vein endothelial cell (HUVEC) monolayer. BMP-22 (0.5 mg/kg per day) decreases the number of lung metastatic foci in a B16/F10 syngeneic mouse melanoma model of lung metastasis.
Brand:CaymanSKU:27264 - 10 mgAvailable on backorder