Chemicals
Showing 29701–29850 of 41137 results
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NS309 is a nonselective activator of small- and intermediate-conductance Ca2+-activated K+ (SK/KCa2 and IK/KCa3.1) channels (EC50s range from 0.12-1.2 µM for SK channels and 10-90 nM for IK channels).{27789,25556} It can also activate voltage-gated Kv11.1 channels (hERG; IC50 = 1 µM), but does not, however, affect large conductance (BK/KCa1.1) channels.{27789,25556,27794} NS309 can modulate neuronal firing patterns by enhancing SK-mediated hyperpolarizing effects.{27789,25556} It is 730-fold (SK channels) and 7,400-fold (IK channels) more potent than 1-EBIO (Item No. 14575) and often used in conjunction with CyPPA (Item No. 15614) to distinguish between SK1 and SK3 subtypes.{27789,25556}
Brand:CaymanSKU:-Available on backorder
NS309 is a nonselective activator of small- and intermediate-conductance Ca2+-activated K+ (SK/KCa2 and IK/KCa3.1) channels (EC50s range from 0.12-1.2 µM for SK channels and 10-90 nM for IK channels).{27789,25556} It can also activate voltage-gated Kv11.1 channels (hERG; IC50 = 1 µM), but does not, however, affect large conductance (BK/KCa1.1) channels.{27789,25556,27794} NS309 can modulate neuronal firing patterns by enhancing SK-mediated hyperpolarizing effects.{27789,25556} It is 730-fold (SK channels) and 7,400-fold (IK channels) more potent than 1-EBIO (Item No. 14575) and often used in conjunction with CyPPA (Item No. 15614) to distinguish between SK1 and SK3 subtypes.{27789,25556}
Brand:CaymanSKU:-Available on backorder
Cytochrome c, which leaks from the mitochondrial intermembrane space into the cytosol, causes oligomerization of apoptotic protease-activating factor 1 (Apaf-1), forming a caspase activation complex known as the apoptosome.{30930} NS3694 is a cell-permeable diarylurea compound that inhibits apoptosome formation and caspase activation.{30929} It blocks cytochrome c-induced caspase activation in HeLa cell cytosolic extracts with an IC50 value of approximately 50 µM.{30929} NS3694 prevents the formation of apoptosomes, which prevents the association of procaspases with Apaf-1.{30929} It suppresses caspase activation and apoptosis in cells treated with either TNF-α or staurosporine (Item No. 81590).{30929} NS3694 is used to examine the role of apoptosome-mediated caspase activation in cell death.{30931,28612,30928}
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Cytochrome c, which leaks from the mitochondrial intermembrane space into the cytosol, causes oligomerization of apoptotic protease-activating factor 1 (Apaf-1), forming a caspase activation complex known as the apoptosome.{30930} NS3694 is a cell-permeable diarylurea compound that inhibits apoptosome formation and caspase activation.{30929} It blocks cytochrome c-induced caspase activation in HeLa cell cytosolic extracts with an IC50 value of approximately 50 µM.{30929} NS3694 prevents the formation of apoptosomes, which prevents the association of procaspases with Apaf-1.{30929} It suppresses caspase activation and apoptosis in cells treated with either TNF-α or staurosporine (Item No. 81590).{30929} NS3694 is used to examine the role of apoptosome-mediated caspase activation in cell death.{30931,28612,30928}
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Cytochrome c, which leaks from the mitochondrial intermembrane space into the cytosol, causes oligomerization of apoptotic protease-activating factor 1 (Apaf-1), forming a caspase activation complex known as the apoptosome.{30930} NS3694 is a cell-permeable diarylurea compound that inhibits apoptosome formation and caspase activation.{30929} It blocks cytochrome c-induced caspase activation in HeLa cell cytosolic extracts with an IC50 value of approximately 50 µM.{30929} NS3694 prevents the formation of apoptosomes, which prevents the association of procaspases with Apaf-1.{30929} It suppresses caspase activation and apoptosis in cells treated with either TNF-α or staurosporine (Item No. 81590).{30929} NS3694 is used to examine the role of apoptosome-mediated caspase activation in cell death.{30931,28612,30928}
Brand:CaymanSKU:-Available on backorder
Cytochrome c, which leaks from the mitochondrial intermembrane space into the cytosol, causes oligomerization of apoptotic protease-activating factor 1 (Apaf-1), forming a caspase activation complex known as the apoptosome.{30930} NS3694 is a cell-permeable diarylurea compound that inhibits apoptosome formation and caspase activation.{30929} It blocks cytochrome c-induced caspase activation in HeLa cell cytosolic extracts with an IC50 value of approximately 50 µM.{30929} NS3694 prevents the formation of apoptosomes, which prevents the association of procaspases with Apaf-1.{30929} It suppresses caspase activation and apoptosis in cells treated with either TNF-α or staurosporine (Item No. 81590).{30929} NS3694 is used to examine the role of apoptosome-mediated caspase activation in cell death.{30931,28612,30928}
Brand:CaymanSKU:-Available on backorder
NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50 = 200 nM in a cell-free kinase assay).{24025} It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50 = 240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.{42938} NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.{42939}
Brand:CaymanSKU:19811 -Available on backorder
NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50 = 200 nM in a cell-free kinase assay).{24025} It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50 = 240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.{42938} NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.{42939}
Brand:CaymanSKU:19811 -Available on backorder
NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50 = 200 nM in a cell-free kinase assay).{24025} It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50 = 240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.{42938} NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.{42939}
Brand:CaymanSKU:19811 -Available on backorder
NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50 = 200 nM in a cell-free kinase assay).{24025} It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50 = 240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.{42938} NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.{42939}
Brand:CaymanSKU:19811 -Available on backorder
NSC 12 is an extracellular trap for fibroblast growth factor 2 (FGF2) that binds FGF2 (Kd = 51 µM) and interferes with its interaction with FGFR1, without affecting the ability of FGF2 to bind heparin or heparin sulfate proteoglycans (HSPGs).{32843} NSC 12 also binds several other, but not all, FGF isoforms with Kd values ranging between 16 and 120 µM, preventing them from forming HSPG/FGF/FGFR ternary complexes.{32843} NSC 12 inhibits FGF-dependent angiogenesis and tumor cell proliferation in vitro and reduces tumor growth in mice.{32843}
Brand:CaymanSKU:20117 -Available on backorder
NSC 12 is an extracellular trap for fibroblast growth factor 2 (FGF2) that binds FGF2 (Kd = 51 µM) and interferes with its interaction with FGFR1, without affecting the ability of FGF2 to bind heparin or heparin sulfate proteoglycans (HSPGs).{32843} NSC 12 also binds several other, but not all, FGF isoforms with Kd values ranging between 16 and 120 µM, preventing them from forming HSPG/FGF/FGFR ternary complexes.{32843} NSC 12 inhibits FGF-dependent angiogenesis and tumor cell proliferation in vitro and reduces tumor growth in mice.{32843}
Brand:CaymanSKU:20117 -Available on backorder
NSC 12 is an extracellular trap for fibroblast growth factor 2 (FGF2) that binds FGF2 (Kd = 51 µM) and interferes with its interaction with FGFR1, without affecting the ability of FGF2 to bind heparin or heparin sulfate proteoglycans (HSPGs).{32843} NSC 12 also binds several other, but not all, FGF isoforms with Kd values ranging between 16 and 120 µM, preventing them from forming HSPG/FGF/FGFR ternary complexes.{32843} NSC 12 inhibits FGF-dependent angiogenesis and tumor cell proliferation in vitro and reduces tumor growth in mice.{32843}
Brand:CaymanSKU:20117 -Available on backorder
NSC 12 is an extracellular trap for fibroblast growth factor 2 (FGF2) that binds FGF2 (Kd = 51 µM) and interferes with its interaction with FGFR1, without affecting the ability of FGF2 to bind heparin or heparin sulfate proteoglycans (HSPGs).{32843} NSC 12 also binds several other, but not all, FGF isoforms with Kd values ranging between 16 and 120 µM, preventing them from forming HSPG/FGF/FGFR ternary complexes.{32843} NSC 12 inhibits FGF-dependent angiogenesis and tumor cell proliferation in vitro and reduces tumor growth in mice.{32843}
Brand:CaymanSKU:20117 -Available on backorder
NSC 146109 is an activator of the tumor suppressor p53 that increases expression of p53 and the p53 target DR5 in wild-type and p53-knockout HCT116 colon adenocarcinoma cells.{36574} It is selective for p53, having no effect on p73 expression in HCT116 cells at a concentration of 2 μM. NSC 146109 activates p53, which induces cell accumulation in the sub-G0/G1 phase and apoptosis in MCF-7 breast cancer cells.{36575} It increases p53 expression, decreases expression of the p53 suppressor MDMX, and reduces viability in a panel of breast cancer cell lines when used at a concentration of 0.5 μM. NSC 146109 also reduces growth of AMC-HN9 head and neck carcinoma (HNC) cells in vitro and in vivo when administered alone or in combination with cisplatin (Item No. 13119) in a mouse xenograft model at a dose of 70 mg/kg.{36576}
Brand:CaymanSKU:-Out of stock
NSC 146109 is an activator of the tumor suppressor p53 that increases expression of p53 and the p53 target DR5 in wild-type and p53-knockout HCT116 colon adenocarcinoma cells.{36574} It is selective for p53, having no effect on p73 expression in HCT116 cells at a concentration of 2 μM. NSC 146109 activates p53, which induces cell accumulation in the sub-G0/G1 phase and apoptosis in MCF-7 breast cancer cells.{36575} It increases p53 expression, decreases expression of the p53 suppressor MDMX, and reduces viability in a panel of breast cancer cell lines when used at a concentration of 0.5 μM. NSC 146109 also reduces growth of AMC-HN9 head and neck carcinoma (HNC) cells in vitro and in vivo when administered alone or in combination with cisplatin (Item No. 13119) in a mouse xenograft model at a dose of 70 mg/kg.{36576}
Brand:CaymanSKU:-Out of stock
NSC 146109 is an activator of the tumor suppressor p53 that increases expression of p53 and the p53 target DR5 in wild-type and p53-knockout HCT116 colon adenocarcinoma cells.{36574} It is selective for p53, having no effect on p73 expression in HCT116 cells at a concentration of 2 μM. NSC 146109 activates p53, which induces cell accumulation in the sub-G0/G1 phase and apoptosis in MCF-7 breast cancer cells.{36575} It increases p53 expression, decreases expression of the p53 suppressor MDMX, and reduces viability in a panel of breast cancer cell lines when used at a concentration of 0.5 μM. NSC 146109 also reduces growth of AMC-HN9 head and neck carcinoma (HNC) cells in vitro and in vivo when administered alone or in combination with cisplatin (Item No. 13119) in a mouse xenograft model at a dose of 70 mg/kg.{36576}
Brand:CaymanSKU:-Out of stock
NSC 146109 is an activator of the tumor suppressor p53 that increases expression of p53 and the p53 target DR5 in wild-type and p53-knockout HCT116 colon adenocarcinoma cells.{36574} It is selective for p53, having no effect on p73 expression in HCT116 cells at a concentration of 2 μM. NSC 146109 activates p53, which induces cell accumulation in the sub-G0/G1 phase and apoptosis in MCF-7 breast cancer cells.{36575} It increases p53 expression, decreases expression of the p53 suppressor MDMX, and reduces viability in a panel of breast cancer cell lines when used at a concentration of 0.5 μM. NSC 146109 also reduces growth of AMC-HN9 head and neck carcinoma (HNC) cells in vitro and in vivo when administered alone or in combination with cisplatin (Item No. 13119) in a mouse xenograft model at a dose of 70 mg/kg.{36576}
Brand:CaymanSKU:-Out of stock
NSC 15520 is an inhibitor of replication protein A 70 (RPA70) dsDNA binding.{44008} It selectively inhibits dsDNA over ssDNA binding to RPA70 when used at concentrations ranging from 25 to 400 µM. NSC 15520 also inhibits the protein-protein interaction between the cell cycle checkpoint control proteins p53 or Rad9 and RPA70.
Brand:CaymanSKU:26020 - 1 mgAvailable on backorder
NSC 15520 is an inhibitor of replication protein A 70 (RPA70) dsDNA binding.{44008} It selectively inhibits dsDNA over ssDNA binding to RPA70 when used at concentrations ranging from 25 to 400 µM. NSC 15520 also inhibits the protein-protein interaction between the cell cycle checkpoint control proteins p53 or Rad9 and RPA70.
Brand:CaymanSKU:26020 - 10 mgAvailable on backorder
NSC 15520 is an inhibitor of replication protein A 70 (RPA70) dsDNA binding.{44008} It selectively inhibits dsDNA over ssDNA binding to RPA70 when used at concentrations ranging from 25 to 400 µM. NSC 15520 also inhibits the protein-protein interaction between the cell cycle checkpoint control proteins p53 or Rad9 and RPA70.
Brand:CaymanSKU:26020 - 25 mgAvailable on backorder
NSC 15520 is an inhibitor of replication protein A 70 (RPA70) dsDNA binding.{44008} It selectively inhibits dsDNA over ssDNA binding to RPA70 when used at concentrations ranging from 25 to 400 µM. NSC 15520 also inhibits the protein-protein interaction between the cell cycle checkpoint control proteins p53 or Rad9 and RPA70.
Brand:CaymanSKU:26020 - 5 mgAvailable on backorder
NSC 185058 is an inhibitor of ATG4B, a cysteine protease that activates LC3B during the initiation of autophagy.{37384} It inhibits ATG4B cleavage of LC3B-GST (IC50 = 51 µM) and reduces LC3B lipidation induced by starvation in Saos-2 cells. NSC 185058 (100 µM) reduces starvation-induced autophagy and prevents autophagic vacuole formation in Saos-2 and MDA-MB-468 cells. It decreases phosphorylation of ribosomal protein S6 (RPS6) only marginally and does not affect phosphatidylinositol 3-kinase (PI3K) activity, indicating a direct role on ATG4B rather than through the mammalian target of rapamycin (mTOR) and PI3K signaling pathways. NSC 185058 (100 mg/kg) decreases autophagic vacuoles in vivo in mouse liver, inhibits tumor growth in an osteosarcoma nude mouse xenograft model, and decreases the number of autophagic vacuoles in osteosarcoma tumors.
Brand:CaymanSKU:23957 - 1 mgAvailable on backorder
NSC 185058 is an inhibitor of ATG4B, a cysteine protease that activates LC3B during the initiation of autophagy.{37384} It inhibits ATG4B cleavage of LC3B-GST (IC50 = 51 µM) and reduces LC3B lipidation induced by starvation in Saos-2 cells. NSC 185058 (100 µM) reduces starvation-induced autophagy and prevents autophagic vacuole formation in Saos-2 and MDA-MB-468 cells. It decreases phosphorylation of ribosomal protein S6 (RPS6) only marginally and does not affect phosphatidylinositol 3-kinase (PI3K) activity, indicating a direct role on ATG4B rather than through the mammalian target of rapamycin (mTOR) and PI3K signaling pathways. NSC 185058 (100 mg/kg) decreases autophagic vacuoles in vivo in mouse liver, inhibits tumor growth in an osteosarcoma nude mouse xenograft model, and decreases the number of autophagic vacuoles in osteosarcoma tumors.
Brand:CaymanSKU:23957 - 5 mgAvailable on backorder
NSC 207895 is an inhibitor of the p53-binding protein MDMX.{48617} It decreases MDMX promoter activity in a reporter assay using HT-1080 cells in a concentration-dependent manner. NSC 207895 (5 µmol/L) decreases the expression and protein levels of MDMX and increases the expression of the p53 target gene CDKN1 (p21) in MCF-7 cells overexpressing MDMX. It also increases the expression of the pro-apoptotic genes PUMA, Bax, and PIG3. NSC 207895 (5 µmol/L) induces apoptosis and decreases cell viability in MCF-7 cells in a p53-dependent manner. It also induces p53-independent apoptosis in wild-type, mutated, and truncated p53 Ewing sarcoma cell lines (IC50s = 98.9-1,613, 236-299, and 121-396 nM, respectively) selectively over wild-type and p53-null osteosarcoma cells (IC50s = 3,690-5,416 and 2,143 nM, respectively).{48617,48618}
Brand:CaymanSKU:27949 - 1 mgAvailable on backorder
NSC 207895 is an inhibitor of the p53-binding protein MDMX.{48617} It decreases MDMX promoter activity in a reporter assay using HT-1080 cells in a concentration-dependent manner. NSC 207895 (5 µmol/L) decreases the expression and protein levels of MDMX and increases the expression of the p53 target gene CDKN1 (p21) in MCF-7 cells overexpressing MDMX. It also increases the expression of the pro-apoptotic genes PUMA, Bax, and PIG3. NSC 207895 (5 µmol/L) induces apoptosis and decreases cell viability in MCF-7 cells in a p53-dependent manner. It also induces p53-independent apoptosis in wild-type, mutated, and truncated p53 Ewing sarcoma cell lines (IC50s = 98.9-1,613, 236-299, and 121-396 nM, respectively) selectively over wild-type and p53-null osteosarcoma cells (IC50s = 3,690-5,416 and 2,143 nM, respectively).{48617,48618}
Brand:CaymanSKU:27949 - 10 mgAvailable on backorder
NSC 207895 is an inhibitor of the p53-binding protein MDMX.{48617} It decreases MDMX promoter activity in a reporter assay using HT-1080 cells in a concentration-dependent manner. NSC 207895 (5 µmol/L) decreases the expression and protein levels of MDMX and increases the expression of the p53 target gene CDKN1 (p21) in MCF-7 cells overexpressing MDMX. It also increases the expression of the pro-apoptotic genes PUMA, Bax, and PIG3. NSC 207895 (5 µmol/L) induces apoptosis and decreases cell viability in MCF-7 cells in a p53-dependent manner. It also induces p53-independent apoptosis in wild-type, mutated, and truncated p53 Ewing sarcoma cell lines (IC50s = 98.9-1,613, 236-299, and 121-396 nM, respectively) selectively over wild-type and p53-null osteosarcoma cells (IC50s = 3,690-5,416 and 2,143 nM, respectively).{48617,48618}
Brand:CaymanSKU:27949 - 25 mgAvailable on backorder
NSC 207895 is an inhibitor of the p53-binding protein MDMX.{48617} It decreases MDMX promoter activity in a reporter assay using HT-1080 cells in a concentration-dependent manner. NSC 207895 (5 µmol/L) decreases the expression and protein levels of MDMX and increases the expression of the p53 target gene CDKN1 (p21) in MCF-7 cells overexpressing MDMX. It also increases the expression of the pro-apoptotic genes PUMA, Bax, and PIG3. NSC 207895 (5 µmol/L) induces apoptosis and decreases cell viability in MCF-7 cells in a p53-dependent manner. It also induces p53-independent apoptosis in wild-type, mutated, and truncated p53 Ewing sarcoma cell lines (IC50s = 98.9-1,613, 236-299, and 121-396 nM, respectively) selectively over wild-type and p53-null osteosarcoma cells (IC50s = 3,690-5,416 and 2,143 nM, respectively).{48617,48618}
Brand:CaymanSKU:27949 - 5 mgAvailable on backorder
Casein Kinase 2 (CK2) is a serine/threonine-selective protein kinase involved in many signal transduction pathways. CK2 is known to negatively regulate apoptosis, and its activity is increased in many proliferating tissues and tumors, which lends promise as an anticancer drug target. NSC 210902 inhibits CK2 with an IC50 value of 1 µM and competitively inhibits binding of ATP with a Ki value of 0.28 µM.{16238} NSC 210902 is selective for CK2 as it only minimally inhibits the activities of other protein kinases (e.g., JNK3, GSK3, Cdk5, and MSK1).{16238}
Brand:CaymanSKU:10011255 - 1 mgAvailable on backorder
Casein Kinase 2 (CK2) is a serine/threonine-selective protein kinase involved in many signal transduction pathways. CK2 is known to negatively regulate apoptosis, and its activity is increased in many proliferating tissues and tumors, which lends promise as an anticancer drug target. NSC 210902 inhibits CK2 with an IC50 value of 1 µM and competitively inhibits binding of ATP with a Ki value of 0.28 µM.{16238} NSC 210902 is selective for CK2 as it only minimally inhibits the activities of other protein kinases (e.g., JNK3, GSK3, Cdk5, and MSK1).{16238}
Brand:CaymanSKU:10011255 - 10 mgAvailable on backorder
Casein Kinase 2 (CK2) is a serine/threonine-selective protein kinase involved in many signal transduction pathways. CK2 is known to negatively regulate apoptosis, and its activity is increased in many proliferating tissues and tumors, which lends promise as an anticancer drug target. NSC 210902 inhibits CK2 with an IC50 value of 1 µM and competitively inhibits binding of ATP with a Ki value of 0.28 µM.{16238} NSC 210902 is selective for CK2 as it only minimally inhibits the activities of other protein kinases (e.g., JNK3, GSK3, Cdk5, and MSK1).{16238}
Brand:CaymanSKU:10011255 - 5 mgAvailable on backorder
Casein Kinase 2 (CK2) is a serine/threonine-selective protein kinase involved in many signal transduction pathways. CK2 is known to negatively regulate apoptosis, and its activity is increased in many proliferating tissues and tumors, which lends promise as an anticancer drug target. NSC 210902 inhibits CK2 with an IC50 value of 1 µM and competitively inhibits binding of ATP with a Ki value of 0.28 µM.{16238} NSC 210902 is selective for CK2 as it only minimally inhibits the activities of other protein kinases (e.g., JNK3, GSK3, Cdk5, and MSK1).{16238}
Brand:CaymanSKU:10011255 - 50 mgAvailable on backorder
NSC 228155 is an activator of the EGF receptor (EGFR) and an inhibitor of the interaction between the kinase inducible domain (KID) of CREB and the KID-interacting (KIX) domain of CREB-binding protein (CBP; IC50 = 0.36 μM).{45576,45577} It increases phosphorylation of EGFR at Tyr1068 in MDA-MB-468 cells (EC50 = 52 μM), as well as phosphorylation of ERK1 and ERK2.{45576} NSC 228155 (100 μM) also induces transactivation of InsR, EphA1, ErbB2, ErbB3, IGF-1R, Mer, and ROR1 in MDA-MB-468 cells. It inhibits CREB-mediated transcription (IC50 = 2.09 μM), as well as transcription mediated by the constitutively active mutant VP16-CREB (IC50 = 6.14 μM), in HEK293T cell-based reporter assays.{45577} NSC 228155 also inhibits P. aeruginosa ribonucleotide reductase (IC50 = 26 μM) and is active against P. aeruginosa with an MIC value of 50 μM.{45578}
Brand:CaymanSKU:28856 - 10 mgAvailable on backorder
NSC 228155 is an activator of the EGF receptor (EGFR) and an inhibitor of the interaction between the kinase inducible domain (KID) of CREB and the KID-interacting (KIX) domain of CREB-binding protein (CBP; IC50 = 0.36 μM).{45576,45577} It increases phosphorylation of EGFR at Tyr1068 in MDA-MB-468 cells (EC50 = 52 μM), as well as phosphorylation of ERK1 and ERK2.{45576} NSC 228155 (100 μM) also induces transactivation of InsR, EphA1, ErbB2, ErbB3, IGF-1R, Mer, and ROR1 in MDA-MB-468 cells. It inhibits CREB-mediated transcription (IC50 = 2.09 μM), as well as transcription mediated by the constitutively active mutant VP16-CREB (IC50 = 6.14 μM), in HEK293T cell-based reporter assays.{45577} NSC 228155 also inhibits P. aeruginosa ribonucleotide reductase (IC50 = 26 μM) and is active against P. aeruginosa with an MIC value of 50 μM.{45578}
Brand:CaymanSKU:28856 - 25 mgAvailable on backorder
NSC 228155 is an activator of the EGF receptor (EGFR) and an inhibitor of the interaction between the kinase inducible domain (KID) of CREB and the KID-interacting (KIX) domain of CREB-binding protein (CBP; IC50 = 0.36 μM).{45576,45577} It increases phosphorylation of EGFR at Tyr1068 in MDA-MB-468 cells (EC50 = 52 μM), as well as phosphorylation of ERK1 and ERK2.{45576} NSC 228155 (100 μM) also induces transactivation of InsR, EphA1, ErbB2, ErbB3, IGF-1R, Mer, and ROR1 in MDA-MB-468 cells. It inhibits CREB-mediated transcription (IC50 = 2.09 μM), as well as transcription mediated by the constitutively active mutant VP16-CREB (IC50 = 6.14 μM), in HEK293T cell-based reporter assays.{45577} NSC 228155 also inhibits P. aeruginosa ribonucleotide reductase (IC50 = 26 μM) and is active against P. aeruginosa with an MIC value of 50 μM.{45578}
Brand:CaymanSKU:28856 - 5 mgAvailable on backorder
NSC 23005 is a small molecule inhibitor of p18, as determined by an in silico screen.{38496} It promotes expansion of murine and human hematopoietic stem cells (HSCs) with an ED50 value of 5.21 nM in a single-cell in vitro culture assay using isolated murine bone marrow cells. NSC 23005 increases the number of long-term HSCs following treatment with a CDK2 inhibitor but not a CDK4/6 inhibitor, indicating that it mediates its effects by blocking p18 inhibition of CDK4/6. It increases HSC proliferation without affecting differentiation, inducing cytotoxicity, or affecting leukemia cell proliferation.
Brand:CaymanSKU:23327 - 1 mgAvailable on backorder
NSC 23005 is a small molecule inhibitor of p18, as determined by an in silico screen.{38496} It promotes expansion of murine and human hematopoietic stem cells (HSCs) with an ED50 value of 5.21 nM in a single-cell in vitro culture assay using isolated murine bone marrow cells. NSC 23005 increases the number of long-term HSCs following treatment with a CDK2 inhibitor but not a CDK4/6 inhibitor, indicating that it mediates its effects by blocking p18 inhibition of CDK4/6. It increases HSC proliferation without affecting differentiation, inducing cytotoxicity, or affecting leukemia cell proliferation.
Brand:CaymanSKU:23327 - 10 mgAvailable on backorder
NSC 23005 is a small molecule inhibitor of p18, as determined by an in silico screen.{38496} It promotes expansion of murine and human hematopoietic stem cells (HSCs) with an ED50 value of 5.21 nM in a single-cell in vitro culture assay using isolated murine bone marrow cells. NSC 23005 increases the number of long-term HSCs following treatment with a CDK2 inhibitor but not a CDK4/6 inhibitor, indicating that it mediates its effects by blocking p18 inhibition of CDK4/6. It increases HSC proliferation without affecting differentiation, inducing cytotoxicity, or affecting leukemia cell proliferation.
Brand:CaymanSKU:23327 - 5 mgAvailable on backorder
Rac1 is a GTPase that is involved in the regulation of the cell cycle, cell-cell adhesion, motility, and differentiation.{18310} Rac1 is activated by its interaction with specific guanine nucleotide exchange factors (GEFs). NSC 23766 is a cell-permeable, reversible inhibitor of Rac1 activation by the Rac-specific GEFs TrioN and Tiam 1 (IC50 = 50 μM).{18308} It has no effect on the closely related GTPases, Cdc42 and RhoA. NSC23766 has been used to investigate the role of Rac1 in such diverse cellular functions as stem cell mobilization, epithelial cell migration, angiogenesis, leukemia cell migration and growth, and gene expression.{18309,18307,18306,18304,18305}
Brand:CaymanSKU:- Rac1 is a GTPase that is involved in the regulation of the cell cycle, cell-cell adhesion, motility, and differentiation.{18310} Rac1 is activated by its interaction with specific guanine nucleotide exchange factors (GEFs). NSC 23766 is a cell-permeable, reversible inhibitor of Rac1 activation by the Rac-specific GEFs TrioN and Tiam 1 (IC50 = 50 μM).{18308} It has no effect on the closely related GTPases, Cdc42 and RhoA. NSC23766 has been used to investigate the role of Rac1 in such diverse cellular functions as stem cell mobilization, epithelial cell migration, angiogenesis, leukemia cell migration and growth, and gene expression.{18309,18307,18306,18304,18305}
Brand:CaymanSKU:- Rac1 is a GTPase that is involved in the regulation of the cell cycle, cell-cell adhesion, motility, and differentiation.{18310} Rac1 is activated by its interaction with specific guanine nucleotide exchange factors (GEFs). NSC 23766 is a cell-permeable, reversible inhibitor of Rac1 activation by the Rac-specific GEFs TrioN and Tiam 1 (IC50 = 50 μM).{18308} It has no effect on the closely related GTPases, Cdc42 and RhoA. NSC23766 has been used to investigate the role of Rac1 in such diverse cellular functions as stem cell mobilization, epithelial cell migration, angiogenesis, leukemia cell migration and growth, and gene expression.{18309,18307,18306,18304,18305}
Brand:CaymanSKU:- Rac1 is a GTPase that is involved in the regulation of the cell cycle, cell-cell adhesion, motility, and differentiation.{18310} Rac1 is activated by its interaction with specific guanine nucleotide exchange factors (GEFs). NSC 23766 is a cell-permeable, reversible inhibitor of Rac1 activation by the Rac-specific GEFs TrioN and Tiam 1 (IC50 = 50 μM).{18308} It has no effect on the closely related GTPases, Cdc42 and RhoA. NSC23766 has been used to investigate the role of Rac1 in such diverse cellular functions as stem cell mobilization, epithelial cell migration, angiogenesis, leukemia cell migration and growth, and gene expression.{18309,18307,18306,18304,18305}
Brand:CaymanSKU:-
NSC 23925 is a non-substrate inhibitor of P-glycoprotein (P-gp).{49228} It selectively reverses multidrug resistance mediated by P-gp over resistance mediated by multidrug resistance-associated protein 1 (MRP1/ABCC1) or breast cancer resistance protein (BCRP/ABCG2). It resensitizes paclitaxel-resistant SKOV3TR and OVCAR-8TR cells to paclitaxel (Item No. 10461). NSC 23925 reverses P-gp efflux, increasing the intracellular accumulation of P-gp substrates, including calcein AM (Item No. 14948) in multidrug-resistant SKOV3TR and OVCAR-8TR cells. It prevents paclitaxel-induced overexpression of the P-gp gene MDR1 and P-gp protein level increases in OVCAR-8 cells.{49229} It also prevents the development of paclitaxel-induced multidrug resistance in a SKOV3 mouse xenograft model when administered at a dose of 50 mg/kg per day in combination with paclitaxel.
Brand:CaymanSKU:21947 -Out of stock
NSC 23925 is a non-substrate inhibitor of P-glycoprotein (P-gp).{49228} It selectively reverses multidrug resistance mediated by P-gp over resistance mediated by multidrug resistance-associated protein 1 (MRP1/ABCC1) or breast cancer resistance protein (BCRP/ABCG2). It resensitizes paclitaxel-resistant SKOV3TR and OVCAR-8TR cells to paclitaxel (Item No. 10461). NSC 23925 reverses P-gp efflux, increasing the intracellular accumulation of P-gp substrates, including calcein AM (Item No. 14948) in multidrug-resistant SKOV3TR and OVCAR-8TR cells. It prevents paclitaxel-induced overexpression of the P-gp gene MDR1 and P-gp protein level increases in OVCAR-8 cells.{49229} It also prevents the development of paclitaxel-induced multidrug resistance in a SKOV3 mouse xenograft model when administered at a dose of 50 mg/kg per day in combination with paclitaxel.
Brand:CaymanSKU:21947 -Out of stock
NSC 23925 is a non-substrate inhibitor of P-glycoprotein (P-gp).{49228} It selectively reverses multidrug resistance mediated by P-gp over resistance mediated by multidrug resistance-associated protein 1 (MRP1/ABCC1) or breast cancer resistance protein (BCRP/ABCG2). It resensitizes paclitaxel-resistant SKOV3TR and OVCAR-8TR cells to paclitaxel (Item No. 10461). NSC 23925 reverses P-gp efflux, increasing the intracellular accumulation of P-gp substrates, including calcein AM (Item No. 14948) in multidrug-resistant SKOV3TR and OVCAR-8TR cells. It prevents paclitaxel-induced overexpression of the P-gp gene MDR1 and P-gp protein level increases in OVCAR-8 cells.{49229} It also prevents the development of paclitaxel-induced multidrug resistance in a SKOV3 mouse xenograft model when administered at a dose of 50 mg/kg per day in combination with paclitaxel.
Brand:CaymanSKU:21947 -Out of stock
NSC 23925 is a non-substrate inhibitor of P-glycoprotein (P-gp).{49228} It selectively reverses multidrug resistance mediated by P-gp over resistance mediated by multidrug resistance-associated protein 1 (MRP1/ABCC1) or breast cancer resistance protein (BCRP/ABCG2). It resensitizes paclitaxel-resistant SKOV3TR and OVCAR-8TR cells to paclitaxel (Item No. 10461). NSC 23925 reverses P-gp efflux, increasing the intracellular accumulation of P-gp substrates, including calcein AM (Item No. 14948) in multidrug-resistant SKOV3TR and OVCAR-8TR cells. It prevents paclitaxel-induced overexpression of the P-gp gene MDR1 and P-gp protein level increases in OVCAR-8 cells.{49229} It also prevents the development of paclitaxel-induced multidrug resistance in a SKOV3 mouse xenograft model when administered at a dose of 50 mg/kg per day in combination with paclitaxel.
Brand:CaymanSKU:21947 -Out of stock
NSC 245214 is a thienyl cycloalkanone that is part of the US National Cancer Institute small molecule repository. The biological activity of this compound has not been reported.
Brand:CaymanSKU:9002543 - 1 mgAvailable on backorder
NSC 245214 is a thienyl cycloalkanone that is part of the US National Cancer Institute small molecule repository. The biological activity of this compound has not been reported.
Brand:CaymanSKU:9002543 - 10 mgAvailable on backorder
NSC 245214 is a thienyl cycloalkanone that is part of the US National Cancer Institute small molecule repository. The biological activity of this compound has not been reported.
Brand:CaymanSKU:9002543 - 25 mgAvailable on backorder
NSC 245214 is a thienyl cycloalkanone that is part of the US National Cancer Institute small molecule repository. The biological activity of this compound has not been reported.
Brand:CaymanSKU:9002543 - 5 mgAvailable on backorder
NSC 319726 is a reactivator of p53R175, a p53 conformational mutant that cannot bind DNA.{36321} It selectively inhibits growth of human tumor cell lines containing mutant p53 over those containing wild-type p53 (IC50s = 0.1-1 and >10 μM, respectively). NSC 319726 induces apoptosis in TOV112D (p53R175H), but not OVCAR3 (p53R248W) or SKOV3 (p53-/-), cells at a concentration of 1 μM. It restores a wild-type conformation to human p53175 and mouse p53R172 mutant proteins and induces expression of p53 target genes in TOV112D cells. In vivo, NSC 319726 (1 mg/kg) inhibits tumor growth in TOV112D, but not H460 (p53+/+), mouse xenograft model. NSC 319726 also has broad-spectrum antifungal activity (MIC50s = 0.1-2 μg/ml against a panel of pathogenic fungi) with >800-fold selectivity for fungi over human HUH-7 and HepG2 cells.{36322}
Brand:CaymanSKU:23701 - 10 mgAvailable on backorder
NSC 319726 is a reactivator of p53R175, a p53 conformational mutant that cannot bind DNA.{36321} It selectively inhibits growth of human tumor cell lines containing mutant p53 over those containing wild-type p53 (IC50s = 0.1-1 and >10 μM, respectively). NSC 319726 induces apoptosis in TOV112D (p53R175H), but not OVCAR3 (p53R248W) or SKOV3 (p53-/-), cells at a concentration of 1 μM. It restores a wild-type conformation to human p53175 and mouse p53R172 mutant proteins and induces expression of p53 target genes in TOV112D cells. In vivo, NSC 319726 (1 mg/kg) inhibits tumor growth in TOV112D, but not H460 (p53+/+), mouse xenograft model. NSC 319726 also has broad-spectrum antifungal activity (MIC50s = 0.1-2 μg/ml against a panel of pathogenic fungi) with >800-fold selectivity for fungi over human HUH-7 and HepG2 cells.{36322}
Brand:CaymanSKU:23701 - 25 mgAvailable on backorder
NSC 319726 is a reactivator of p53R175, a p53 conformational mutant that cannot bind DNA.{36321} It selectively inhibits growth of human tumor cell lines containing mutant p53 over those containing wild-type p53 (IC50s = 0.1-1 and >10 μM, respectively). NSC 319726 induces apoptosis in TOV112D (p53R175H), but not OVCAR3 (p53R248W) or SKOV3 (p53-/-), cells at a concentration of 1 μM. It restores a wild-type conformation to human p53175 and mouse p53R172 mutant proteins and induces expression of p53 target genes in TOV112D cells. In vivo, NSC 319726 (1 mg/kg) inhibits tumor growth in TOV112D, but not H460 (p53+/+), mouse xenograft model. NSC 319726 also has broad-spectrum antifungal activity (MIC50s = 0.1-2 μg/ml against a panel of pathogenic fungi) with >800-fold selectivity for fungi over human HUH-7 and HepG2 cells.{36322}
Brand:CaymanSKU:23701 - 5 mgAvailable on backorder
Nucleophosmin is a nucleolar phosphoprotein involved in cell proliferation, cytoplasmic/nuclear shuttle transportation, nucleic acid binding, ribonucleic cleavage, centrosome duplication, and molecular chaperoning. Its activity is dependent on oligomerization at its N-terminal domain, and it is abundantly expressed in tumor and developing cells where it serves to inhibit both cellular differentiation and apoptosis.{27213} NSC 348884 is a small molecule that inhibits the formation of nucleophosmin dimers by disrupting a required binding pocket. It can inhibit cell proliferation and induce apoptosis in various cancer cell lines with IC50 values ranging from 1.4-4 µM.{27213,27214}
Brand:CaymanSKU:-Out of stock
Nucleophosmin is a nucleolar phosphoprotein involved in cell proliferation, cytoplasmic/nuclear shuttle transportation, nucleic acid binding, ribonucleic cleavage, centrosome duplication, and molecular chaperoning. Its activity is dependent on oligomerization at its N-terminal domain, and it is abundantly expressed in tumor and developing cells where it serves to inhibit both cellular differentiation and apoptosis.{27213} NSC 348884 is a small molecule that inhibits the formation of nucleophosmin dimers by disrupting a required binding pocket. It can inhibit cell proliferation and induce apoptosis in various cancer cell lines with IC50 values ranging from 1.4-4 µM.{27213,27214}
Brand:CaymanSKU:-Out of stock
Nucleophosmin is a nucleolar phosphoprotein involved in cell proliferation, cytoplasmic/nuclear shuttle transportation, nucleic acid binding, ribonucleic cleavage, centrosome duplication, and molecular chaperoning. Its activity is dependent on oligomerization at its N-terminal domain, and it is abundantly expressed in tumor and developing cells where it serves to inhibit both cellular differentiation and apoptosis.{27213} NSC 348884 is a small molecule that inhibits the formation of nucleophosmin dimers by disrupting a required binding pocket. It can inhibit cell proliferation and induce apoptosis in various cancer cell lines with IC50 values ranging from 1.4-4 µM.{27213,27214}
Brand:CaymanSKU:-Out of stock
Nucleophosmin is a nucleolar phosphoprotein involved in cell proliferation, cytoplasmic/nuclear shuttle transportation, nucleic acid binding, ribonucleic cleavage, centrosome duplication, and molecular chaperoning. Its activity is dependent on oligomerization at its N-terminal domain, and it is abundantly expressed in tumor and developing cells where it serves to inhibit both cellular differentiation and apoptosis.{27213} NSC 348884 is a small molecule that inhibits the formation of nucleophosmin dimers by disrupting a required binding pocket. It can inhibit cell proliferation and induce apoptosis in various cancer cell lines with IC50 values ranging from 1.4-4 µM.{27213,27214}
Brand:CaymanSKU:-Out of stock
NSC 5844 is a bis-quinoline with diverse biological activities.{41174,41175,41176} It inhibits the growth of P. falciparum strains that are sensitive (D-6) and resistant (W-2) to chloroquine (Item No. 14194) in vitro (IC50s = 17 and 27 nM, respectively) but lacks activity against P. berghei in vivo.{41174} NSC 5844 inhibits the growth of MDA-MB-468 and MCF-7 breast cancer cells with GI50 values of 7.35 and 14.80 μM, respectively.{41175} It also inhibits 24% of botulinum neurotoxin serotype A light chain (BoNT/A LC) metalloprotease activity at a concentration of 20 μM.{41176}
Brand:CaymanSKU:23443 - 10 mgAvailable on backorder
NSC 5844 is a bis-quinoline with diverse biological activities.{41174,41175,41176} It inhibits the growth of P. falciparum strains that are sensitive (D-6) and resistant (W-2) to chloroquine (Item No. 14194) in vitro (IC50s = 17 and 27 nM, respectively) but lacks activity against P. berghei in vivo.{41174} NSC 5844 inhibits the growth of MDA-MB-468 and MCF-7 breast cancer cells with GI50 values of 7.35 and 14.80 μM, respectively.{41175} It also inhibits 24% of botulinum neurotoxin serotype A light chain (BoNT/A LC) metalloprotease activity at a concentration of 20 μM.{41176}
Brand:CaymanSKU:23443 - 25 mgAvailable on backorder
NSC 5844 is a bis-quinoline with diverse biological activities.{41174,41175,41176} It inhibits the growth of P. falciparum strains that are sensitive (D-6) and resistant (W-2) to chloroquine (Item No. 14194) in vitro (IC50s = 17 and 27 nM, respectively) but lacks activity against P. berghei in vivo.{41174} NSC 5844 inhibits the growth of MDA-MB-468 and MCF-7 breast cancer cells with GI50 values of 7.35 and 14.80 μM, respectively.{41175} It also inhibits 24% of botulinum neurotoxin serotype A light chain (BoNT/A LC) metalloprotease activity at a concentration of 20 μM.{41176}
Brand:CaymanSKU:23443 - 5 mgAvailable on backorder
NSC 5844 is a bis-quinoline with diverse biological activities.{41174,41175,41176} It inhibits the growth of P. falciparum strains that are sensitive (D-6) and resistant (W-2) to chloroquine (Item No. 14194) in vitro (IC50s = 17 and 27 nM, respectively) but lacks activity against P. berghei in vivo.{41174} NSC 5844 inhibits the growth of MDA-MB-468 and MCF-7 breast cancer cells with GI50 values of 7.35 and 14.80 μM, respectively.{41175} It also inhibits 24% of botulinum neurotoxin serotype A light chain (BoNT/A LC) metalloprotease activity at a concentration of 20 μM.{41176}
Brand:CaymanSKU:23443 - 50 mgAvailable on backorder
NSC 59984 is a reactivator of p53 that restores wild-type p53 signaling by activating p73-dependent apoptosis in mutant p53-expressing colon cancer cells.{31961} It is reported to induce cell death in colon cancer cells (EC50 = 8.38 µM in p53-null HCT116 cells) without evident toxicity toward normal cells.{31961} NSC 59984 has been shown to induce p53 mutant protein degradation via MDM2-mediated ubiquitination.{31961}
Brand:CaymanSKU:19919 -Available on backorder
NSC 59984 is a reactivator of p53 that restores wild-type p53 signaling by activating p73-dependent apoptosis in mutant p53-expressing colon cancer cells.{31961} It is reported to induce cell death in colon cancer cells (EC50 = 8.38 µM in p53-null HCT116 cells) without evident toxicity toward normal cells.{31961} NSC 59984 has been shown to induce p53 mutant protein degradation via MDM2-mediated ubiquitination.{31961}
Brand:CaymanSKU:19919 -Available on backorder
NSC 59984 is a reactivator of p53 that restores wild-type p53 signaling by activating p73-dependent apoptosis in mutant p53-expressing colon cancer cells.{31961} It is reported to induce cell death in colon cancer cells (EC50 = 8.38 µM in p53-null HCT116 cells) without evident toxicity toward normal cells.{31961} NSC 59984 has been shown to induce p53 mutant protein degradation via MDM2-mediated ubiquitination.{31961}
Brand:CaymanSKU:19919 -Available on backorder
NSC 59984 is a reactivator of p53 that restores wild-type p53 signaling by activating p73-dependent apoptosis in mutant p53-expressing colon cancer cells.{31961} It is reported to induce cell death in colon cancer cells (EC50 = 8.38 µM in p53-null HCT116 cells) without evident toxicity toward normal cells.{31961} NSC 59984 has been shown to induce p53 mutant protein degradation via MDM2-mediated ubiquitination.{31961}
Brand:CaymanSKU:19919 -Available on backorder
NSC 617145 is an inhibitor of WRN helicase (IC50 = 230 nM) that inhibits the ATPase, but not exonuclease, activity of WRN helicase in a concentration-dependent manner.{38654} It is selective for WRN over BLM, FANCJ, ChlR1, RecQ, and UvrD helicases, only exhibiting 7% inhibition of RECQ1 at a concentration of 5 µM. NSC 617145 inhibits growth of HeLa cells via formation of DNA double strand breaks (DSBs) and induction of apoptosis in a WRN helicase-dependent manner. NSC 617145 also acts synergistically with mitomycin C (Item No. 11435) to inhibit growth as well as induce DSBs and chromosomal abnormalities in Fanconia-anemia deficient (FA-D2-/-) cells.
Brand:CaymanSKU:21973 -Out of stock
NSC 617145 is an inhibitor of WRN helicase (IC50 = 230 nM) that inhibits the ATPase, but not exonuclease, activity of WRN helicase in a concentration-dependent manner.{38654} It is selective for WRN over BLM, FANCJ, ChlR1, RecQ, and UvrD helicases, only exhibiting 7% inhibition of RECQ1 at a concentration of 5 µM. NSC 617145 inhibits growth of HeLa cells via formation of DNA double strand breaks (DSBs) and induction of apoptosis in a WRN helicase-dependent manner. NSC 617145 also acts synergistically with mitomycin C (Item No. 11435) to inhibit growth as well as induce DSBs and chromosomal abnormalities in Fanconia-anemia deficient (FA-D2-/-) cells.
Brand:CaymanSKU:21973 -Out of stock
NSC 617145 is an inhibitor of WRN helicase (IC50 = 230 nM) that inhibits the ATPase, but not exonuclease, activity of WRN helicase in a concentration-dependent manner.{38654} It is selective for WRN over BLM, FANCJ, ChlR1, RecQ, and UvrD helicases, only exhibiting 7% inhibition of RECQ1 at a concentration of 5 µM. NSC 617145 inhibits growth of HeLa cells via formation of DNA double strand breaks (DSBs) and induction of apoptosis in a WRN helicase-dependent manner. NSC 617145 also acts synergistically with mitomycin C (Item No. 11435) to inhibit growth as well as induce DSBs and chromosomal abnormalities in Fanconia-anemia deficient (FA-D2-/-) cells.
Brand:CaymanSKU:21973 -Out of stock
NSC 617145 is an inhibitor of WRN helicase (IC50 = 230 nM) that inhibits the ATPase, but not exonuclease, activity of WRN helicase in a concentration-dependent manner.{38654} It is selective for WRN over BLM, FANCJ, ChlR1, RecQ, and UvrD helicases, only exhibiting 7% inhibition of RECQ1 at a concentration of 5 µM. NSC 617145 inhibits growth of HeLa cells via formation of DNA double strand breaks (DSBs) and induction of apoptosis in a WRN helicase-dependent manner. NSC 617145 also acts synergistically with mitomycin C (Item No. 11435) to inhibit growth as well as induce DSBs and chromosomal abnormalities in Fanconia-anemia deficient (FA-D2-/-) cells.
Brand:CaymanSKU:21973 -Out of stock
NSC 624206 is an inhibitor of ubiquitin-activating enzyme (E1) that specifically blocks ubiquitin-thioester formation (IC50 = 13 µM) but has no effect on ubiquitin adenylation.{34092} Through this action, NSC 624206 prevents the ubiquitination and degradation of the tumor suppressor protein p27 in vitro.{34092}
Brand:CaymanSKU:20569 -Available on backorder
NSC 624206 is an inhibitor of ubiquitin-activating enzyme (E1) that specifically blocks ubiquitin-thioester formation (IC50 = 13 µM) but has no effect on ubiquitin adenylation.{34092} Through this action, NSC 624206 prevents the ubiquitination and degradation of the tumor suppressor protein p27 in vitro.{34092}
Brand:CaymanSKU:20569 -Available on backorder
NSC 624206 is an inhibitor of ubiquitin-activating enzyme (E1) that specifically blocks ubiquitin-thioester formation (IC50 = 13 µM) but has no effect on ubiquitin adenylation.{34092} Through this action, NSC 624206 prevents the ubiquitination and degradation of the tumor suppressor protein p27 in vitro.{34092}
Brand:CaymanSKU:20569 -Available on backorder
NSC 624206 is an inhibitor of ubiquitin-activating enzyme (E1) that specifically blocks ubiquitin-thioester formation (IC50 = 13 µM) but has no effect on ubiquitin adenylation.{34092} Through this action, NSC 624206 prevents the ubiquitination and degradation of the tumor suppressor protein p27 in vitro.{34092}
Brand:CaymanSKU:20569 -Available on backorder
Protein ubiquitination is a dynamic process that can be reversed by deubiquitinating enzymes (DUBs) that remove ubiquitin from proteins, sparing them from degradation by the proteasome. The DUBs have been divided into various groups, the largest being the ubiquitin-specific proteases (USPs). NSC 632839 inhibits USP2 and USP7 as well as the ubiquitin-like SUMO peptidase SENP2 with EC50 values of 45, 37, and 9.8 µM, respectively.{27604} It is reported to inhibit apoptosis through a Bcl-2-dependent and apoptosome-independent pathway of caspase activation (IC50 = 15.7 µM in cells sensitized by E1A, an adenoviral oncogene).{27605}
Brand:CaymanSKU:-Out of stock
Protein ubiquitination is a dynamic process that can be reversed by deubiquitinating enzymes (DUBs) that remove ubiquitin from proteins, sparing them from degradation by the proteasome. The DUBs have been divided into various groups, the largest being the ubiquitin-specific proteases (USPs). NSC 632839 inhibits USP2 and USP7 as well as the ubiquitin-like SUMO peptidase SENP2 with EC50 values of 45, 37, and 9.8 µM, respectively.{27604} It is reported to inhibit apoptosis through a Bcl-2-dependent and apoptosome-independent pathway of caspase activation (IC50 = 15.7 µM in cells sensitized by E1A, an adenoviral oncogene).{27605}
Brand:CaymanSKU:-Out of stock
Protein ubiquitination is a dynamic process that can be reversed by deubiquitinating enzymes (DUBs) that remove ubiquitin from proteins, sparing them from degradation by the proteasome. The DUBs have been divided into various groups, the largest being the ubiquitin-specific proteases (USPs). NSC 632839 inhibits USP2 and USP7 as well as the ubiquitin-like SUMO peptidase SENP2 with EC50 values of 45, 37, and 9.8 µM, respectively.{27604} It is reported to inhibit apoptosis through a Bcl-2-dependent and apoptosome-independent pathway of caspase activation (IC50 = 15.7 µM in cells sensitized by E1A, an adenoviral oncogene).{27605}
Brand:CaymanSKU:-Out of stock
Protein ubiquitination is a dynamic process that can be reversed by deubiquitinating enzymes (DUBs) that remove ubiquitin from proteins, sparing them from degradation by the proteasome. The DUBs have been divided into various groups, the largest being the ubiquitin-specific proteases (USPs). NSC 632839 inhibits USP2 and USP7 as well as the ubiquitin-like SUMO peptidase SENP2 with EC50 values of 45, 37, and 9.8 µM, respectively.{27604} It is reported to inhibit apoptosis through a Bcl-2-dependent and apoptosome-independent pathway of caspase activation (IC50 = 15.7 µM in cells sensitized by E1A, an adenoviral oncogene).{27605}
Brand:CaymanSKU:-Out of stock
Three genes encode dual specificity phosphatases that are Cdc25 homologs. The phosphatases, Cdc25A through C, are proto-oncogenes and are often over-expressed in cancers. NSC 663284 is a potent, cell-permeable, and irreversible inhibitor of all Cdc25 isoforms, with preference for Cdc25A (IC50 = 29, 95, and 89 nM for Cdc25A, Cdc25B2, and Cdc25C, respectively).{17980} NSC 663284 poorly inhibits other phosphatases, including Vaccinia virus VH1-related (IC50 = 4.0 μM), PTP1B (no inhibition), and the mitogen-activated protein kinase phosphatases (MKP) MKP-1 or -3 (no inhibition).{17980,17978} By inhibiting Cdc25 isoforms, NSC 663284 prevents the dephosphorylation and activation of Cdk1 and Cdk2,{17979,17981} arrests cells at both G1 and G2/M phases,{17979} and prevents the proliferation of several human tumor cell lines.{17980,17979,17982}
Brand:CaymanSKU:- Three genes encode dual specificity phosphatases that are Cdc25 homologs. The phosphatases, Cdc25A through C, are proto-oncogenes and are often over-expressed in cancers. NSC 663284 is a potent, cell-permeable, and irreversible inhibitor of all Cdc25 isoforms, with preference for Cdc25A (IC50 = 29, 95, and 89 nM for Cdc25A, Cdc25B2, and Cdc25C, respectively).{17980} NSC 663284 poorly inhibits other phosphatases, including Vaccinia virus VH1-related (IC50 = 4.0 μM), PTP1B (no inhibition), and the mitogen-activated protein kinase phosphatases (MKP) MKP-1 or -3 (no inhibition).{17980,17978} By inhibiting Cdc25 isoforms, NSC 663284 prevents the dephosphorylation and activation of Cdk1 and Cdk2,{17979,17981} arrests cells at both G1 and G2/M phases,{17979} and prevents the proliferation of several human tumor cell lines.{17980,17979,17982}
Brand:CaymanSKU:- Three genes encode dual specificity phosphatases that are Cdc25 homologs. The phosphatases, Cdc25A through C, are proto-oncogenes and are often over-expressed in cancers. NSC 663284 is a potent, cell-permeable, and irreversible inhibitor of all Cdc25 isoforms, with preference for Cdc25A (IC50 = 29, 95, and 89 nM for Cdc25A, Cdc25B2, and Cdc25C, respectively).{17980} NSC 663284 poorly inhibits other phosphatases, including Vaccinia virus VH1-related (IC50 = 4.0 μM), PTP1B (no inhibition), and the mitogen-activated protein kinase phosphatases (MKP) MKP-1 or -3 (no inhibition).{17980,17978} By inhibiting Cdc25 isoforms, NSC 663284 prevents the dephosphorylation and activation of Cdk1 and Cdk2,{17979,17981} arrests cells at both G1 and G2/M phases,{17979} and prevents the proliferation of several human tumor cell lines.{17980,17979,17982}
Brand:CaymanSKU:- Three genes encode dual specificity phosphatases that are Cdc25 homologs. The phosphatases, Cdc25A through C, are proto-oncogenes and are often over-expressed in cancers. NSC 663284 is a potent, cell-permeable, and irreversible inhibitor of all Cdc25 isoforms, with preference for Cdc25A (IC50 = 29, 95, and 89 nM for Cdc25A, Cdc25B2, and Cdc25C, respectively).{17980} NSC 663284 poorly inhibits other phosphatases, including Vaccinia virus VH1-related (IC50 = 4.0 μM), PTP1B (no inhibition), and the mitogen-activated protein kinase phosphatases (MKP) MKP-1 or -3 (no inhibition).{17980,17978} By inhibiting Cdc25 isoforms, NSC 663284 prevents the dephosphorylation and activation of Cdk1 and Cdk2,{17979,17981} arrests cells at both G1 and G2/M phases,{17979} and prevents the proliferation of several human tumor cell lines.{17980,17979,17982}
Brand:CaymanSKU:-