Cayman
Showing 32701–32850 of 45550 results
-
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:-NSC 668036 is an inhibitor of the Dishevelled (Dvl) protein PDZ domain (Kd = 240 μM for mouse Dvl1 PDZ domain).{38844} NSC 668036 interacts with Dvl PDZ at the same binding site as Dapper and Frizzled, native binding partners in the Wnt signaling pathway. NSC 668036 (180 ng) reduces expression of the Wnt target gene, Siamois, in Xenopus embryos and inhibits the ability of injected Wnt3A to induce formation of a secondary axis. At concentrations greater than 10 μM, NSC 668036 inhibits proliferation of NIH/3T3 fibroblasts, restrains their migration in a scratch assay, and blocks the accelerating effect of TGF-β on fibroblast migration.{38845} NSC 668036 (5 mg/kg per day for 14 days) reduces the severity of pulmonary fibrosis in mice by bleomycin (Item No. 13877). NSC 668036 also blocks the bleomycin-induced pulmonary expression of α-smooth muscle actin (α-SMA), collagen I, TGF-β, and β-catenin by 30-50%.
Brand:CaymanSKU:23499 - 1 mgAvailable on backorder
NSC 668036 is an inhibitor of the Dishevelled (Dvl) protein PDZ domain (Kd = 240 μM for mouse Dvl1 PDZ domain).{38844} NSC 668036 interacts with Dvl PDZ at the same binding site as Dapper and Frizzled, native binding partners in the Wnt signaling pathway. NSC 668036 (180 ng) reduces expression of the Wnt target gene, Siamois, in Xenopus embryos and inhibits the ability of injected Wnt3A to induce formation of a secondary axis. At concentrations greater than 10 μM, NSC 668036 inhibits proliferation of NIH/3T3 fibroblasts, restrains their migration in a scratch assay, and blocks the accelerating effect of TGF-β on fibroblast migration.{38845} NSC 668036 (5 mg/kg per day for 14 days) reduces the severity of pulmonary fibrosis in mice by bleomycin (Item No. 13877). NSC 668036 also blocks the bleomycin-induced pulmonary expression of α-smooth muscle actin (α-SMA), collagen I, TGF-β, and β-catenin by 30-50%.
Brand:CaymanSKU:23499 - 10 mgAvailable on backorder
NSC 668036 is an inhibitor of the Dishevelled (Dvl) protein PDZ domain (Kd = 240 μM for mouse Dvl1 PDZ domain).{38844} NSC 668036 interacts with Dvl PDZ at the same binding site as Dapper and Frizzled, native binding partners in the Wnt signaling pathway. NSC 668036 (180 ng) reduces expression of the Wnt target gene, Siamois, in Xenopus embryos and inhibits the ability of injected Wnt3A to induce formation of a secondary axis. At concentrations greater than 10 μM, NSC 668036 inhibits proliferation of NIH/3T3 fibroblasts, restrains their migration in a scratch assay, and blocks the accelerating effect of TGF-β on fibroblast migration.{38845} NSC 668036 (5 mg/kg per day for 14 days) reduces the severity of pulmonary fibrosis in mice by bleomycin (Item No. 13877). NSC 668036 also blocks the bleomycin-induced pulmonary expression of α-smooth muscle actin (α-SMA), collagen I, TGF-β, and β-catenin by 30-50%.
Brand:CaymanSKU:23499 - 25 mgAvailable on backorder
NSC 668036 is an inhibitor of the Dishevelled (Dvl) protein PDZ domain (Kd = 240 μM for mouse Dvl1 PDZ domain).{38844} NSC 668036 interacts with Dvl PDZ at the same binding site as Dapper and Frizzled, native binding partners in the Wnt signaling pathway. NSC 668036 (180 ng) reduces expression of the Wnt target gene, Siamois, in Xenopus embryos and inhibits the ability of injected Wnt3A to induce formation of a secondary axis. At concentrations greater than 10 μM, NSC 668036 inhibits proliferation of NIH/3T3 fibroblasts, restrains their migration in a scratch assay, and blocks the accelerating effect of TGF-β on fibroblast migration.{38845} NSC 668036 (5 mg/kg per day for 14 days) reduces the severity of pulmonary fibrosis in mice by bleomycin (Item No. 13877). NSC 668036 also blocks the bleomycin-induced pulmonary expression of α-smooth muscle actin (α-SMA), collagen I, TGF-β, and β-catenin by 30-50%.
Brand:CaymanSKU:23499 - 5 mgAvailable on backorder
NSC 66811 is a potent inhibitor of murine double minute 2 (Mdm2) interaction with p53 by binding Mdm2 (Ki = 120 nM), in this way activating p53.{31195} NSC 66811 induces the accumulation of p21, p53, and Mdm2 in human colon cancer cells in vitro. Inhibitors of the Mdm2-p53 interaction, including NSC 66811, induce p53- and p21-dependent cell cycle arrest and p53-dependent cell death in tumor cell lines.{31196}
Brand:CaymanSKU:-Out of stock
NSC 66811 is a potent inhibitor of murine double minute 2 (Mdm2) interaction with p53 by binding Mdm2 (Ki = 120 nM), in this way activating p53.{31195} NSC 66811 induces the accumulation of p21, p53, and Mdm2 in human colon cancer cells in vitro. Inhibitors of the Mdm2-p53 interaction, including NSC 66811, induce p53- and p21-dependent cell cycle arrest and p53-dependent cell death in tumor cell lines.{31196}
Brand:CaymanSKU:-Out of stock
NSC 66811 is a potent inhibitor of murine double minute 2 (Mdm2) interaction with p53 by binding Mdm2 (Ki = 120 nM), in this way activating p53.{31195} NSC 66811 induces the accumulation of p21, p53, and Mdm2 in human colon cancer cells in vitro. Inhibitors of the Mdm2-p53 interaction, including NSC 66811, induce p53- and p21-dependent cell cycle arrest and p53-dependent cell death in tumor cell lines.{31196}
Brand:CaymanSKU:-Out of stock
NSC 697923 is a selective inhibitor of the E2 ubiquitin-conjugating enzyme Ubc13 when heterodimerized with Uev1A, blocking polyubiquitin chain formation at concentrations of 0.5 to 2 µM in vitro.{31222} It also inhibits NF-κB activation by PMA and other agonists, presumably through its effects on Ubc13.{31222} NSC 697923 blocks proliferation and induces apoptosis in diffuse large B cell lymphoma and neuroblastoma cells.{31222,31221} It has antitumor efficacy in vivo in neuroblastoma orthotopic xenografts, when given intraperitoneally.{31221}
Brand:CaymanSKU:-NSC 697923 is a selective inhibitor of the E2 ubiquitin-conjugating enzyme Ubc13 when heterodimerized with Uev1A, blocking polyubiquitin chain formation at concentrations of 0.5 to 2 µM in vitro.{31222} It also inhibits NF-κB activation by PMA and other agonists, presumably through its effects on Ubc13.{31222} NSC 697923 blocks proliferation and induces apoptosis in diffuse large B cell lymphoma and neuroblastoma cells.{31222,31221} It has antitumor efficacy in vivo in neuroblastoma orthotopic xenografts, when given intraperitoneally.{31221}
Brand:CaymanSKU:-NSC 697923 is a selective inhibitor of the E2 ubiquitin-conjugating enzyme Ubc13 when heterodimerized with Uev1A, blocking polyubiquitin chain formation at concentrations of 0.5 to 2 µM in vitro.{31222} It also inhibits NF-κB activation by PMA and other agonists, presumably through its effects on Ubc13.{31222} NSC 697923 blocks proliferation and induces apoptosis in diffuse large B cell lymphoma and neuroblastoma cells.{31222,31221} It has antitumor efficacy in vivo in neuroblastoma orthotopic xenografts, when given intraperitoneally.{31221}
Brand:CaymanSKU:-NSC 781406 is a dual inhibitor of PI3K and mammalian target of rapamycin (mTOR; IC50s = 2.0, 9.4, 2.7, 14, and 5.4 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, and mTOR, respectively).{52165} It inhibits cell growth in the NCI-60 panel of cancer cell lines (mean GI50 = 65 nM). NSC 781406 (30 mg/kg) reduces tumor volume in a BEL-7404 hepatic cancer mouse xenograft model.
Brand:CaymanSKU:29226 - 1 mgAvailable on backorder
NSC 781406 is a dual inhibitor of PI3K and mammalian target of rapamycin (mTOR; IC50s = 2.0, 9.4, 2.7, 14, and 5.4 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, and mTOR, respectively).{52165} It inhibits cell growth in the NCI-60 panel of cancer cell lines (mean GI50 = 65 nM). NSC 781406 (30 mg/kg) reduces tumor volume in a BEL-7404 hepatic cancer mouse xenograft model.
Brand:CaymanSKU:29226 - 10 mgAvailable on backorder
NSC 781406 is a dual inhibitor of PI3K and mammalian target of rapamycin (mTOR; IC50s = 2.0, 9.4, 2.7, 14, and 5.4 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, and mTOR, respectively).{52165} It inhibits cell growth in the NCI-60 panel of cancer cell lines (mean GI50 = 65 nM). NSC 781406 (30 mg/kg) reduces tumor volume in a BEL-7404 hepatic cancer mouse xenograft model.
Brand:CaymanSKU:29226 - 5 mgAvailable on backorder
The Src homology region 2 domain-containing phosphatases (SHP) known as SHP-1 and SHP-2 act downstream of receptor and non-receptor tyrosine kinase to modulate signal transduction.{23672} NSC 87877 is a cell-permeable, inhibitor of both SHP-1 and SHP-2 (IC50 = 355 and 318 nM, respectively).{23672} It is much less effective against other protein tyrosine phosphatases and the dual-specificity phosphatase 26.{23672,23671} Through its effects on SHP-1 or SHP-2, NSC 87877 blocks epidermal growth factor receptor-induced activation of Ras and ERK1/2 in HEK293 cells, stimulates store-operated calcium entry in response to thrombin in platelets, and increased acetylcholine receptor clustering in myotubes.{23672,23669,23670}
Brand:CaymanSKU:-The Src homology region 2 domain-containing phosphatases (SHP) known as SHP-1 and SHP-2 act downstream of receptor and non-receptor tyrosine kinase to modulate signal transduction.{23672} NSC 87877 is a cell-permeable, inhibitor of both SHP-1 and SHP-2 (IC50 = 355 and 318 nM, respectively).{23672} It is much less effective against other protein tyrosine phosphatases and the dual-specificity phosphatase 26.{23672,23671} Through its effects on SHP-1 or SHP-2, NSC 87877 blocks epidermal growth factor receptor-induced activation of Ras and ERK1/2 in HEK293 cells, stimulates store-operated calcium entry in response to thrombin in platelets, and increased acetylcholine receptor clustering in myotubes.{23672,23669,23670}
Brand:CaymanSKU:-The Src homology region 2 domain-containing phosphatases (SHP) known as SHP-1 and SHP-2 act downstream of receptor and non-receptor tyrosine kinase to modulate signal transduction.{23672} NSC 87877 is a cell-permeable, inhibitor of both SHP-1 and SHP-2 (IC50 = 355 and 318 nM, respectively).{23672} It is much less effective against other protein tyrosine phosphatases and the dual-specificity phosphatase 26.{23672,23671} Through its effects on SHP-1 or SHP-2, NSC 87877 blocks epidermal growth factor receptor-induced activation of Ras and ERK1/2 in HEK293 cells, stimulates store-operated calcium entry in response to thrombin in platelets, and increased acetylcholine receptor clustering in myotubes.{23672,23669,23670}
Brand:CaymanSKU:-The Src homology region 2 domain-containing phosphatases (SHP) known as SHP-1 and SHP-2 act downstream of receptor and non-receptor tyrosine kinase to modulate signal transduction.{23672} NSC 87877 is a cell-permeable, inhibitor of both SHP-1 and SHP-2 (IC50 = 355 and 318 nM, respectively).{23672} It is much less effective against other protein tyrosine phosphatases and the dual-specificity phosphatase 26.{23672,23671} Through its effects on SHP-1 or SHP-2, NSC 87877 blocks epidermal growth factor receptor-induced activation of Ras and ERK1/2 in HEK293 cells, stimulates store-operated calcium entry in response to thrombin in platelets, and increased acetylcholine receptor clustering in myotubes.{23672,23669,23670}
Brand:CaymanSKU:-NSC 95397 is a 1,4-naphthoquinone-based irreversible inhibitor of Cdc25 dual-specificity phosphatases, with Ki values of 32, 96, and 40 nM for Cdc25A, Cdc25B, and Cdc25C, respectively.{33364} It displays >125-fold selectivity for Cdc25 over VH1-related dual-specificity phosphatase and protein tyrosine phosphatase 1b. NSC 95397 significantly inhibits the growth of human and murine carcinoma cells, blocking G2/M phase transition.{33364,17981} In rat liver epithelial cells, NSC 95397 induces cell cycle arrest, which is associated with phosphorylation of EGFR, activation of ERK1/2, phosphorylation of connexin43, and downregulation of gap junctional intercellular communication.{33365}
Brand:CaymanSKU:21431 -Out of stock
NSC 95397 is a 1,4-naphthoquinone-based irreversible inhibitor of Cdc25 dual-specificity phosphatases, with Ki values of 32, 96, and 40 nM for Cdc25A, Cdc25B, and Cdc25C, respectively.{33364} It displays >125-fold selectivity for Cdc25 over VH1-related dual-specificity phosphatase and protein tyrosine phosphatase 1b. NSC 95397 significantly inhibits the growth of human and murine carcinoma cells, blocking G2/M phase transition.{33364,17981} In rat liver epithelial cells, NSC 95397 induces cell cycle arrest, which is associated with phosphorylation of EGFR, activation of ERK1/2, phosphorylation of connexin43, and downregulation of gap junctional intercellular communication.{33365}
Brand:CaymanSKU:21431 -Out of stock
NSC 95397 is a 1,4-naphthoquinone-based irreversible inhibitor of Cdc25 dual-specificity phosphatases, with Ki values of 32, 96, and 40 nM for Cdc25A, Cdc25B, and Cdc25C, respectively.{33364} It displays >125-fold selectivity for Cdc25 over VH1-related dual-specificity phosphatase and protein tyrosine phosphatase 1b. NSC 95397 significantly inhibits the growth of human and murine carcinoma cells, blocking G2/M phase transition.{33364,17981} In rat liver epithelial cells, NSC 95397 induces cell cycle arrest, which is associated with phosphorylation of EGFR, activation of ERK1/2, phosphorylation of connexin43, and downregulation of gap junctional intercellular communication.{33365}
Brand:CaymanSKU:21431 -Out of stock
NSC 95397 is a 1,4-naphthoquinone-based irreversible inhibitor of Cdc25 dual-specificity phosphatases, with Ki values of 32, 96, and 40 nM for Cdc25A, Cdc25B, and Cdc25C, respectively.{33364} It displays >125-fold selectivity for Cdc25 over VH1-related dual-specificity phosphatase and protein tyrosine phosphatase 1b. NSC 95397 significantly inhibits the growth of human and murine carcinoma cells, blocking G2/M phase transition.{33364,17981} In rat liver epithelial cells, NSC 95397 induces cell cycle arrest, which is associated with phosphorylation of EGFR, activation of ERK1/2, phosphorylation of connexin43, and downregulation of gap junctional intercellular communication.{33365}
Brand:CaymanSKU:21431 -Out of stock
NSI-189 (Item No. 26166) is an analytical reference standard categorized as an antidepressant.{46075} This product is intended for research and forensic applications.
Brand:CaymanSKU:26166 - 1 mgAvailable on backorder
NSI-189 (Item No. 26166) is an analytical reference standard categorized as an antidepressant.{46075} This product is intended for research and forensic applications.
Brand:CaymanSKU:26166 - 5 mgAvailable on backorder
NU 1025 is an inhibitor of poly(ADP-ribose) polymerases (PARP) (IC50 = 400 nM).{23208} It enhances the cytotoxicity of γ-irradiation and certain anticancer drugs.{23204,23205} NU 1025 is also used to study the regulation of deoxyribonucleic acid repair by PARP enzymes.{23206}
Brand:CaymanSKU:-NU 1025 is an inhibitor of poly(ADP-ribose) polymerases (PARP) (IC50 = 400 nM).{23208} It enhances the cytotoxicity of γ-irradiation and certain anticancer drugs.{23204,23205} NU 1025 is also used to study the regulation of deoxyribonucleic acid repair by PARP enzymes.{23206}
Brand:CaymanSKU:-NU 1025 is an inhibitor of poly(ADP-ribose) polymerases (PARP) (IC50 = 400 nM).{23208} It enhances the cytotoxicity of γ-irradiation and certain anticancer drugs.{23204,23205} NU 1025 is also used to study the regulation of deoxyribonucleic acid repair by PARP enzymes.{23206}
Brand:CaymanSKU:-NU 1025 is an inhibitor of poly(ADP-ribose) polymerases (PARP) (IC50 = 400 nM).{23208} It enhances the cytotoxicity of γ-irradiation and certain anticancer drugs.{23204,23205} NU 1025 is also used to study the regulation of deoxyribonucleic acid repair by PARP enzymes.{23206}
Brand:CaymanSKU:-NU 2058 is an inhibitor of cyclin-dependent kinase 1 (Cdk1) and Cdk2 (IC50s = 7.0 and 17 µM, respectively).{21729,21732} Increased Cdk activity is often associated with human tumors, and inhibitors of Cdks, including NU 2058, can arrest cell cycling in cancer cells in vitro.{21732,33762,33763}
Brand:CaymanSKU:21415 -Out of stock
NU 2058 is an inhibitor of cyclin-dependent kinase 1 (Cdk1) and Cdk2 (IC50s = 7.0 and 17 µM, respectively).{21729,21732} Increased Cdk activity is often associated with human tumors, and inhibitors of Cdks, including NU 2058, can arrest cell cycling in cancer cells in vitro.{21732,33762,33763}
Brand:CaymanSKU:21415 -Out of stock
NU 2058 is an inhibitor of cyclin-dependent kinase 1 (Cdk1) and Cdk2 (IC50s = 7.0 and 17 µM, respectively).{21729,21732} Increased Cdk activity is often associated with human tumors, and inhibitors of Cdks, including NU 2058, can arrest cell cycling in cancer cells in vitro.{21732,33762,33763}
Brand:CaymanSKU:21415 -Out of stock
NU 2058 is an inhibitor of cyclin-dependent kinase 1 (Cdk1) and Cdk2 (IC50s = 7.0 and 17 µM, respectively).{21729,21732} Increased Cdk activity is often associated with human tumors, and inhibitors of Cdks, including NU 2058, can arrest cell cycling in cancer cells in vitro.{21732,33762,33763}
Brand:CaymanSKU:21415 -Out of stock
Cyclin-dependent kinases (CDKs) play a key role in regulating cell division by phosphorylating distinct substrates in different phases of the cell cycle. Cell cycle deregulation in many cancers often results from altered CDK activity. Thus, CDKs are potential pharmacological targets for anticancer agents. NU 6027 inhibits both CDK1 and CDK2 with IC50 values of 2.9 and 2.2 µM, respectively.{21732} It has been shown to inhibit cellular ataxia telangiectasia mutated and Rad3-related kinase activity (IC50 = 6.7 µM) and impair G2/M arrest in various human cancer cells, potentiating the cytotoxic effects of DNA-damaging, anticancer agents such as cisplatin.{26368}
Brand:CaymanSKU:-Cyclin-dependent kinases (CDKs) play a key role in regulating cell division by phosphorylating distinct substrates in different phases of the cell cycle. Cell cycle deregulation in many cancers often results from altered CDK activity. Thus, CDKs are potential pharmacological targets for anticancer agents. NU 6027 inhibits both CDK1 and CDK2 with IC50 values of 2.9 and 2.2 µM, respectively.{21732} It has been shown to inhibit cellular ataxia telangiectasia mutated and Rad3-related kinase activity (IC50 = 6.7 µM) and impair G2/M arrest in various human cancer cells, potentiating the cytotoxic effects of DNA-damaging, anticancer agents such as cisplatin.{26368}
Brand:CaymanSKU:-Cyclin-dependent kinases (CDKs) play a key role in regulating cell division by phosphorylating distinct substrates in different phases of the cell cycle. Cell cycle deregulation in many cancers often results from altered CDK activity. Thus, CDKs are potential pharmacological targets for anticancer agents. NU 6027 inhibits both CDK1 and CDK2 with IC50 values of 2.9 and 2.2 µM, respectively.{21732} It has been shown to inhibit cellular ataxia telangiectasia mutated and Rad3-related kinase activity (IC50 = 6.7 µM) and impair G2/M arrest in various human cancer cells, potentiating the cytotoxic effects of DNA-damaging, anticancer agents such as cisplatin.{26368}
Brand:CaymanSKU:-Cyclin-dependent kinases (CDKs) play a key role in regulating cell division by phosphorylating distinct substrates in different phases of the cell cycle. Cell cycle deregulation in many cancers often results from altered CDK activity. Thus, CDKs are potential pharmacological targets for anticancer agents. NU 6027 inhibits both CDK1 and CDK2 with IC50 values of 2.9 and 2.2 µM, respectively.{21732} It has been shown to inhibit cellular ataxia telangiectasia mutated and Rad3-related kinase activity (IC50 = 6.7 µM) and impair G2/M arrest in various human cancer cells, potentiating the cytotoxic effects of DNA-damaging, anticancer agents such as cisplatin.{26368}
Brand:CaymanSKU:-Cyclin-dependent kinases (CDKs) play a key role in regulating cell division by phosphorylating distinct substrates in different phases of the cell cycle. Cell cycle deregulation in many cancers often results from altered CDK activity. Thus, CDKs are potential pharmacological targets for anticancer agents. NU 6102 is a potent inhibitor of Cdk1 and Cdk2 with Ki values of 9 and 6 nM and IC50 values of 9.5 and 5.4 nM, respectively.{21732,21729} NU 6102 inhibits Cdk4 activity with an IC50 value of 1.6 μM, suggesting it is most selective for Cdk2.{21731} Time-lapse videomicroscopy reveals that 20 μM NU 6102 delays cell entry into mitosis where most cells appear to eventually complete mitotic division but cannot correctly undergo cytokinesis, and hence become binucleated with an abnormal number of centrosomes.{21730} In SKUT-1B cancer cells a 24 h exposure to NU 6102 induced G2 arrest, inhibition of target protein phosphorylation, and cytotoxicity with an LC50 value of 2.6 μM.{21728}
Brand:CaymanSKU:-Cyclin-dependent kinases (CDKs) play a key role in regulating cell division by phosphorylating distinct substrates in different phases of the cell cycle. Cell cycle deregulation in many cancers often results from altered CDK activity. Thus, CDKs are potential pharmacological targets for anticancer agents. NU 6102 is a potent inhibitor of Cdk1 and Cdk2 with Ki values of 9 and 6 nM and IC50 values of 9.5 and 5.4 nM, respectively.{21732,21729} NU 6102 inhibits Cdk4 activity with an IC50 value of 1.6 μM, suggesting it is most selective for Cdk2.{21731} Time-lapse videomicroscopy reveals that 20 μM NU 6102 delays cell entry into mitosis where most cells appear to eventually complete mitotic division but cannot correctly undergo cytokinesis, and hence become binucleated with an abnormal number of centrosomes.{21730} In SKUT-1B cancer cells a 24 h exposure to NU 6102 induced G2 arrest, inhibition of target protein phosphorylation, and cytotoxicity with an LC50 value of 2.6 μM.{21728}
Brand:CaymanSKU:-NU 6140 is a cyclin-dependent kinase 2 (Cdk2) inhibitor (IC50 = 0.41 μM) that demonstrates 10- to 36-fold selectivity against Cdk2-cyclin A compared to Cdk1-cyclin B, Cdk4-cyclin D, Cdk5-p25, or Cdk7-cyclin H.{28149} NU 6140 has been found to induce cell-cycle arrest at the G2-M phase and to potentiate the apoptotic effect of paclitaxel (Item No. 10461) in HeLa cells by inhibiting the anti-apoptotic protein, survivin.{28149}
Brand:CaymanSKU:-Out of stock
NU 6140 is a cyclin-dependent kinase 2 (Cdk2) inhibitor (IC50 = 0.41 μM) that demonstrates 10- to 36-fold selectivity against Cdk2-cyclin A compared to Cdk1-cyclin B, Cdk4-cyclin D, Cdk5-p25, or Cdk7-cyclin H.{28149} NU 6140 has been found to induce cell-cycle arrest at the G2-M phase and to potentiate the apoptotic effect of paclitaxel (Item No. 10461) in HeLa cells by inhibiting the anti-apoptotic protein, survivin.{28149}
Brand:CaymanSKU:-Out of stock
NU 6140 is a cyclin-dependent kinase 2 (Cdk2) inhibitor (IC50 = 0.41 μM) that demonstrates 10- to 36-fold selectivity against Cdk2-cyclin A compared to Cdk1-cyclin B, Cdk4-cyclin D, Cdk5-p25, or Cdk7-cyclin H.{28149} NU 6140 has been found to induce cell-cycle arrest at the G2-M phase and to potentiate the apoptotic effect of paclitaxel (Item No. 10461) in HeLa cells by inhibiting the anti-apoptotic protein, survivin.{28149}
Brand:CaymanSKU:-Out of stock
NU 6140 is a cyclin-dependent kinase 2 (Cdk2) inhibitor (IC50 = 0.41 μM) that demonstrates 10- to 36-fold selectivity against Cdk2-cyclin A compared to Cdk1-cyclin B, Cdk4-cyclin D, Cdk5-p25, or Cdk7-cyclin H.{28149} NU 6140 has been found to induce cell-cycle arrest at the G2-M phase and to potentiate the apoptotic effect of paclitaxel (Item No. 10461) in HeLa cells by inhibiting the anti-apoptotic protein, survivin.{28149}
Brand:CaymanSKU:-Out of stock
DNA-dependent protein kinase (DNA-PK) binds to strand breaks produced during normal cellular processes or in response to genotoxic stresses, such as ionizing radiation, targeting substrates that facilitate DNA repair. NU 7026 is a cell-permeable, potent, specific, and ATP-competitive inhibitor of DNA-PK (IC50 = 230 nM).{17273} It poorly inhibits phosphioinositide 3 kinase (IC50 = 13 μM) and is inactive against ataxia telangiectasia mutated kinase, ATR, and poly (ADP-ribose) polymerase.{17273} NU 7026 impairs cellular DNA double strand break repair and decreases survival in cells exposed to ionizing radiation.{17273} It also potentiates the cytotoxicity of topoisomerase II poisons used in the treatment of leukemia. For example, it potentiates the growth inhibitory effects of mitoxantrone in K562 cells more than 10-fold.{17274}
Brand:CaymanSKU:-DNA-dependent protein kinase (DNA-PK) binds to strand breaks produced during normal cellular processes or in response to genotoxic stresses, such as ionizing radiation, targeting substrates that facilitate DNA repair. NU 7026 is a cell-permeable, potent, specific, and ATP-competitive inhibitor of DNA-PK (IC50 = 230 nM).{17273} It poorly inhibits phosphioinositide 3 kinase (IC50 = 13 μM) and is inactive against ataxia telangiectasia mutated kinase, ATR, and poly (ADP-ribose) polymerase.{17273} NU 7026 impairs cellular DNA double strand break repair and decreases survival in cells exposed to ionizing radiation.{17273} It also potentiates the cytotoxicity of topoisomerase II poisons used in the treatment of leukemia. For example, it potentiates the growth inhibitory effects of mitoxantrone in K562 cells more than 10-fold.{17274}
Brand:CaymanSKU:-DNA-dependent protein kinase (DNA-PK) binds to strand breaks produced during normal cellular processes or in response to genotoxic stresses, such as ionizing radiation, targeting substrates that facilitate DNA repair. NU 7026 is a cell-permeable, potent, specific, and ATP-competitive inhibitor of DNA-PK (IC50 = 230 nM).{17273} It poorly inhibits phosphioinositide 3 kinase (IC50 = 13 μM) and is inactive against ataxia telangiectasia mutated kinase, ATR, and poly (ADP-ribose) polymerase.{17273} NU 7026 impairs cellular DNA double strand break repair and decreases survival in cells exposed to ionizing radiation.{17273} It also potentiates the cytotoxicity of topoisomerase II poisons used in the treatment of leukemia. For example, it potentiates the growth inhibitory effects of mitoxantrone in K562 cells more than 10-fold.{17274}
Brand:CaymanSKU:-DNA-dependent protein kinase (DNA-PK) binds to strand breaks produced during normal cellular processes or in response to genotoxic stresses, such as ionizing radiation, targeting substrates that facilitate DNA repair. NU 7026 is a cell-permeable, potent, specific, and ATP-competitive inhibitor of DNA-PK (IC50 = 230 nM).{17273} It poorly inhibits phosphioinositide 3 kinase (IC50 = 13 μM) and is inactive against ataxia telangiectasia mutated kinase, ATR, and poly (ADP-ribose) polymerase.{17273} NU 7026 impairs cellular DNA double strand break repair and decreases survival in cells exposed to ionizing radiation.{17273} It also potentiates the cytotoxicity of topoisomerase II poisons used in the treatment of leukemia. For example, it potentiates the growth inhibitory effects of mitoxantrone in K562 cells more than 10-fold.{17274}
Brand:CaymanSKU:-DNA-dependent protein kinase (DNA-PK) catalyzes nonhomologous end-joining, which is required to repair lethal DNA double-strand breaks. Because cells that are defective in DNA double-strand break repair are highly sensitive to ionizing radiation and topoisomerase II poisons, modulating DNA-PK is one strategy to defer cancer cell resistance to radiation or chemotherapeutic treatments.{17273} NU 7441 is a selective DNA-PK inhibitor with an IC50 value of 14 nM.{23765} It inhibits other members of the PI3K-related kinase family, including mTOR, PI3K, ataxia telangiectasia mutated (ATM), and ataxia telangiectasia and Rad3 related (ATR) with IC50 values of 1.7, 5, >100, and >100 μM, respectively.{23765} NU 7441 has been shown to increase the cytotoxicity of ionizing radiation and etoposide (Item No. 12092) in human colon cancer cell lines in vitro and to potentiate the effects of etoposide in mice bearing human colon cancer xenograft tumors in vivo.{23764}
Brand:CaymanSKU:-DNA-dependent protein kinase (DNA-PK) catalyzes nonhomologous end-joining, which is required to repair lethal DNA double-strand breaks. Because cells that are defective in DNA double-strand break repair are highly sensitive to ionizing radiation and topoisomerase II poisons, modulating DNA-PK is one strategy to defer cancer cell resistance to radiation or chemotherapeutic treatments.{17273} NU 7441 is a selective DNA-PK inhibitor with an IC50 value of 14 nM.{23765} It inhibits other members of the PI3K-related kinase family, including mTOR, PI3K, ataxia telangiectasia mutated (ATM), and ataxia telangiectasia and Rad3 related (ATR) with IC50 values of 1.7, 5, >100, and >100 μM, respectively.{23765} NU 7441 has been shown to increase the cytotoxicity of ionizing radiation and etoposide (Item No. 12092) in human colon cancer cell lines in vitro and to potentiate the effects of etoposide in mice bearing human colon cancer xenograft tumors in vivo.{23764}
Brand:CaymanSKU:-DNA-dependent protein kinase (DNA-PK) catalyzes nonhomologous end-joining, which is required to repair lethal DNA double-strand breaks. Because cells that are defective in DNA double-strand break repair are highly sensitive to ionizing radiation and topoisomerase II poisons, modulating DNA-PK is one strategy to defer cancer cell resistance to radiation or chemotherapeutic treatments.{17273} NU 7441 is a selective DNA-PK inhibitor with an IC50 value of 14 nM.{23765} It inhibits other members of the PI3K-related kinase family, including mTOR, PI3K, ataxia telangiectasia mutated (ATM), and ataxia telangiectasia and Rad3 related (ATR) with IC50 values of 1.7, 5, >100, and >100 μM, respectively.{23765} NU 7441 has been shown to increase the cytotoxicity of ionizing radiation and etoposide (Item No. 12092) in human colon cancer cell lines in vitro and to potentiate the effects of etoposide in mice bearing human colon cancer xenograft tumors in vivo.{23764}
Brand:CaymanSKU:-DNA-dependent protein kinase (DNA-PK) catalyzes nonhomologous end-joining, which is required to repair lethal DNA double-strand breaks. Because cells that are defective in DNA double-strand break repair are highly sensitive to ionizing radiation and topoisomerase II poisons, modulating DNA-PK is one strategy to defer cancer cell resistance to radiation or chemotherapeutic treatments.{17273} NU 7441 is a selective DNA-PK inhibitor with an IC50 value of 14 nM.{23765} It inhibits other members of the PI3K-related kinase family, including mTOR, PI3K, ataxia telangiectasia mutated (ATM), and ataxia telangiectasia and Rad3 related (ATR) with IC50 values of 1.7, 5, >100, and >100 μM, respectively.{23765} NU 7441 has been shown to increase the cytotoxicity of ionizing radiation and etoposide (Item No. 12092) in human colon cancer cell lines in vitro and to potentiate the effects of etoposide in mice bearing human colon cancer xenograft tumors in vivo.{23764}
Brand:CaymanSKU:-NUC-1031 is a prodrug form of the anticancer nucleoside analog gemcitabine (Item No. 11690).{43518,43517} NUC-1031 is more lipophilic than gemcitabine and enters cells through passive diffusion.{43518} It inhibits the growth of L1210, CEM, MP-2, and BxPC-3 cancer cells in vitro (IC50 = 35, 30, 60, and 40 nM, respectively).{43517} NUC-1031 (0.076 mmol/kg) reduces tumor growth in Mia-PaCa-2 and BxPC-3 mouse xenograft models, which are partially responsive and resistant to gemcitabine, respectively.{43519}
Brand:CaymanSKU:9003247 - 1 mgAvailable on backorder
NUC-1031 is a prodrug form of the anticancer nucleoside analog gemcitabine (Item No. 11690).{43518,43517} NUC-1031 is more lipophilic than gemcitabine and enters cells through passive diffusion.{43518} It inhibits the growth of L1210, CEM, MP-2, and BxPC-3 cancer cells in vitro (IC50 = 35, 30, 60, and 40 nM, respectively).{43517} NUC-1031 (0.076 mmol/kg) reduces tumor growth in Mia-PaCa-2 and BxPC-3 mouse xenograft models, which are partially responsive and resistant to gemcitabine, respectively.{43519}
Brand:CaymanSKU:9003247 - 10 mgAvailable on backorder
NUC-1031 is a prodrug form of the anticancer nucleoside analog gemcitabine (Item No. 11690).{43518,43517} NUC-1031 is more lipophilic than gemcitabine and enters cells through passive diffusion.{43518} It inhibits the growth of L1210, CEM, MP-2, and BxPC-3 cancer cells in vitro (IC50 = 35, 30, 60, and 40 nM, respectively).{43517} NUC-1031 (0.076 mmol/kg) reduces tumor growth in Mia-PaCa-2 and BxPC-3 mouse xenograft models, which are partially responsive and resistant to gemcitabine, respectively.{43519}
Brand:CaymanSKU:9003247 - 5 mgAvailable on backorder
Nuclear yellow is a DNA-selective dye that is used to label DNA content in live and fixed cells. Upon binding to DNA, nuclear yellow fluoresces, and this fluorescence can be measured using fluorescence microscopy, microplate fluorometry, or flow cytometry. Nuclear yellow has commonly been used in combination with retrograde tracers for two-color neuronal mapping.{45032} It can also be used to photoconvert diaminobenzidine (DAB) into an electron-dense reaction product for light and electron microscopy applications.{45033} Nuclear yellow displays excitation/emission maxima of 355/495 nm, respectively.
Brand:CaymanSKU:25178 - 10 mgAvailable on backorder
Nuclear yellow is a DNA-selective dye that is used to label DNA content in live and fixed cells. Upon binding to DNA, nuclear yellow fluoresces, and this fluorescence can be measured using fluorescence microscopy, microplate fluorometry, or flow cytometry. Nuclear yellow has commonly been used in combination with retrograde tracers for two-color neuronal mapping.{45032} It can also be used to photoconvert diaminobenzidine (DAB) into an electron-dense reaction product for light and electron microscopy applications.{45033} Nuclear yellow displays excitation/emission maxima of 355/495 nm, respectively.
Brand:CaymanSKU:25178 - 25 mgAvailable on backorder
Nuclear yellow is a DNA-selective dye that is used to label DNA content in live and fixed cells. Upon binding to DNA, nuclear yellow fluoresces, and this fluorescence can be measured using fluorescence microscopy, microplate fluorometry, or flow cytometry. Nuclear yellow has commonly been used in combination with retrograde tracers for two-color neuronal mapping.{45032} It can also be used to photoconvert diaminobenzidine (DAB) into an electron-dense reaction product for light and electron microscopy applications.{45033} Nuclear yellow displays excitation/emission maxima of 355/495 nm, respectively.
Brand:CaymanSKU:25178 - 5 mgAvailable on backorder
Nucleozin is an antiviral inhibitor of influenza nucleoprotein accumulation, preventing it from translocating into the nucleus of host cells.{58045} It inhibits MDCK cell infection by influenza A and H5N1 (EC50s = 0.069 and 0.33 µM, respectively), as well as a clinical isolate of H3N2 (EC50 = 0.16 µM). Nucleozin reduces the lung viral load and increases the survival rate in a mouse model of influenza H5N1 infection.
Brand:CaymanSKU:30363 - 10 mgAvailable on backorder
Nucleozin is an antiviral inhibitor of influenza nucleoprotein accumulation, preventing it from translocating into the nucleus of host cells.{58045} It inhibits MDCK cell infection by influenza A and H5N1 (EC50s = 0.069 and 0.33 µM, respectively), as well as a clinical isolate of H3N2 (EC50 = 0.16 µM). Nucleozin reduces the lung viral load and increases the survival rate in a mouse model of influenza H5N1 infection.
Brand:CaymanSKU:30363 - 25 mgAvailable on backorder
Nucleozin is an antiviral inhibitor of influenza nucleoprotein accumulation, preventing it from translocating into the nucleus of host cells.{58045} It inhibits MDCK cell infection by influenza A and H5N1 (EC50s = 0.069 and 0.33 µM, respectively), as well as a clinical isolate of H3N2 (EC50 = 0.16 µM). Nucleozin reduces the lung viral load and increases the survival rate in a mouse model of influenza H5N1 infection.
Brand:CaymanSKU:30363 - 5 mgAvailable on backorder
Nucleozin is an antiviral inhibitor of influenza nucleoprotein accumulation, preventing it from translocating into the nucleus of host cells.{58045} It inhibits MDCK cell infection by influenza A and H5N1 (EC50s = 0.069 and 0.33 µM, respectively), as well as a clinical isolate of H3N2 (EC50 = 0.16 µM). Nucleozin reduces the lung viral load and increases the survival rate in a mouse model of influenza H5N1 infection.
Brand:CaymanSKU:30363 - 50 mgAvailable on backorder
Nudifloramide, known more commonly as N-methyl-2-pyridone-5-carboxamide (2-Py), is a metabolite of niacin via nicotinamide. It can be measured in serum and urine as part of metabolomic studies of niacin or nicotinamide intake and usage.{33023,33024} Circulating levels of nudifloramide can be elevated and associated with toxic effects in patients receiving supplemental nicotinamide.{33022}
Brand:CaymanSKU:20507 -Available on backorder
Nudifloramide, known more commonly as N-methyl-2-pyridone-5-carboxamide (2-Py), is a metabolite of niacin via nicotinamide. It can be measured in serum and urine as part of metabolomic studies of niacin or nicotinamide intake and usage.{33023,33024} Circulating levels of nudifloramide can be elevated and associated with toxic effects in patients receiving supplemental nicotinamide.{33022}
Brand:CaymanSKU:20507 -Available on backorder
Nudifloramide, known more commonly as N-methyl-2-pyridone-5-carboxamide (2-Py), is a metabolite of niacin via nicotinamide. It can be measured in serum and urine as part of metabolomic studies of niacin or nicotinamide intake and usage.{33023,33024} Circulating levels of nudifloramide can be elevated and associated with toxic effects in patients receiving supplemental nicotinamide.{33022}
Brand:CaymanSKU:20507 -Available on backorder
Nudifloramide, known more commonly as N-methyl-2-pyridone-5-carboxamide (2-Py), is a metabolite of niacin via nicotinamide. It can be measured in serum and urine as part of metabolomic studies of niacin or nicotinamide intake and usage.{33023,33024} Circulating levels of nudifloramide can be elevated and associated with toxic effects in patients receiving supplemental nicotinamide.{33022}
Brand:CaymanSKU:20507 -Available on backorder
Scriptaid (Item No. 10572) is a histone deacetylase (HDAC) inhibitor that has an optimal concentration of 6-8 μM in a cell-based assay, is less toxic than trichostatin A, and works in a wide variety of biological systems.{18409} Nullscript is an analog of scriptaid that lacks the HDAC inhibitory effects of scriptaid.{18409} It is used as a negative control in experiments involving scriptaid.{18409}
Brand:CaymanSKU:-Out of stock
Scriptaid (Item No. 10572) is a histone deacetylase (HDAC) inhibitor that has an optimal concentration of 6-8 μM in a cell-based assay, is less toxic than trichostatin A, and works in a wide variety of biological systems.{18409} Nullscript is an analog of scriptaid that lacks the HDAC inhibitory effects of scriptaid.{18409} It is used as a negative control in experiments involving scriptaid.{18409}
Brand:CaymanSKU:-Out of stock
Scriptaid (Item No. 10572) is a histone deacetylase (HDAC) inhibitor that has an optimal concentration of 6-8 μM in a cell-based assay, is less toxic than trichostatin A, and works in a wide variety of biological systems.{18409} Nullscript is an analog of scriptaid that lacks the HDAC inhibitory effects of scriptaid.{18409} It is used as a negative control in experiments involving scriptaid.{18409}
Brand:CaymanSKU:-Out of stock
NVP-231 is a potent and reversible inhibitor of ceramide kinase (IC50 = 12 nM).{22065} It is selective for ceramide kinase over SPHK1, SPHK2, DAGKa, PI3Ka, PI4Kb, VPS34, GCS, SMS-1, and CERT (IC50s = >5 mM). NVP-231 inhibits formation of ceramide-1-phosphate (C1P; IC50 = 10 nM) and cell death in ceramide kinase overexpressing COS cells (COS-CerK). It also inhibits C1P formation and tube formation in murine dermal microvascular endothelial cells when used at a concentration of 100 nM.{22067}
Brand:CaymanSKU:-NVP-231 is a potent and reversible inhibitor of ceramide kinase (IC50 = 12 nM).{22065} It is selective for ceramide kinase over SPHK1, SPHK2, DAGKa, PI3Ka, PI4Kb, VPS34, GCS, SMS-1, and CERT (IC50s = >5 mM). NVP-231 inhibits formation of ceramide-1-phosphate (C1P; IC50 = 10 nM) and cell death in ceramide kinase overexpressing COS cells (COS-CerK). It also inhibits C1P formation and tube formation in murine dermal microvascular endothelial cells when used at a concentration of 100 nM.{22067}
Brand:CaymanSKU:-NVP-231 is a potent and reversible inhibitor of ceramide kinase (IC50 = 12 nM).{22065} It is selective for ceramide kinase over SPHK1, SPHK2, DAGKa, PI3Ka, PI4Kb, VPS34, GCS, SMS-1, and CERT (IC50s = >5 mM). NVP-231 inhibits formation of ceramide-1-phosphate (C1P; IC50 = 10 nM) and cell death in ceramide kinase overexpressing COS cells (COS-CerK). It also inhibits C1P formation and tube formation in murine dermal microvascular endothelial cells when used at a concentration of 100 nM.{22067}
Brand:CaymanSKU:-NVP-231 is a potent and reversible inhibitor of ceramide kinase (IC50 = 12 nM).{22065} It is selective for ceramide kinase over SPHK1, SPHK2, DAGKa, PI3Ka, PI4Kb, VPS34, GCS, SMS-1, and CERT (IC50s = >5 mM). NVP-231 inhibits formation of ceramide-1-phosphate (C1P; IC50 = 10 nM) and cell death in ceramide kinase overexpressing COS cells (COS-CerK). It also inhibits C1P formation and tube formation in murine dermal microvascular endothelial cells when used at a concentration of 100 nM.{22067}
Brand:CaymanSKU:-NVP-AAM077 is an NMDA receptor antagonist (IC50 = 0.008 µM).{61130} It is selective for NMDA receptors containing NR1A/NR2A subunits over NMDA receptors containing NR1A/NR2B subunits (IC50s = 0.27 and 29.6 µM, respectively, in X. laevis oocytes expressing receptors containing the respective subunits). NVP-AAM077 inhibits seizures induced by maximal electroshock (MES) in mice with an ED50 value of 23 mg/kg. It increases the activity of neuronal nitric oxide synthase (nNOS) in primary hippocampal neurons.{61131} NVP-AAM077 (10 mg/kg) inhibits proliferation of neural progenitor cells (NPCs) in the subventricular zone (SVZ) and in the subgranular zone (SGZ) of the hippocampal dentate gyrus of adult mice, an effect not seen in nNOS-/- mice. It also increases the escape latency and decreases the percentage of time spent in the target quadrant in the Morris water maze.
Brand:CaymanSKU:30622 - 1 mgAvailable on backorder
NVP-AAM077 is an NMDA receptor antagonist (IC50 = 0.008 µM).{61130} It is selective for NMDA receptors containing NR1A/NR2A subunits over NMDA receptors containing NR1A/NR2B subunits (IC50s = 0.27 and 29.6 µM, respectively, in X. laevis oocytes expressing receptors containing the respective subunits). NVP-AAM077 inhibits seizures induced by maximal electroshock (MES) in mice with an ED50 value of 23 mg/kg. It increases the activity of neuronal nitric oxide synthase (nNOS) in primary hippocampal neurons.{61131} NVP-AAM077 (10 mg/kg) inhibits proliferation of neural progenitor cells (NPCs) in the subventricular zone (SVZ) and in the subgranular zone (SGZ) of the hippocampal dentate gyrus of adult mice, an effect not seen in nNOS-/- mice. It also increases the escape latency and decreases the percentage of time spent in the target quadrant in the Morris water maze.
Brand:CaymanSKU:30622 - 10 mgAvailable on backorder
NVP-AAM077 is an NMDA receptor antagonist (IC50 = 0.008 µM).{61130} It is selective for NMDA receptors containing NR1A/NR2A subunits over NMDA receptors containing NR1A/NR2B subunits (IC50s = 0.27 and 29.6 µM, respectively, in X. laevis oocytes expressing receptors containing the respective subunits). NVP-AAM077 inhibits seizures induced by maximal electroshock (MES) in mice with an ED50 value of 23 mg/kg. It increases the activity of neuronal nitric oxide synthase (nNOS) in primary hippocampal neurons.{61131} NVP-AAM077 (10 mg/kg) inhibits proliferation of neural progenitor cells (NPCs) in the subventricular zone (SVZ) and in the subgranular zone (SGZ) of the hippocampal dentate gyrus of adult mice, an effect not seen in nNOS-/- mice. It also increases the escape latency and decreases the percentage of time spent in the target quadrant in the Morris water maze.
Brand:CaymanSKU:30622 - 25 mgAvailable on backorder
NVP-AAM077 is an NMDA receptor antagonist (IC50 = 0.008 µM).{61130} It is selective for NMDA receptors containing NR1A/NR2A subunits over NMDA receptors containing NR1A/NR2B subunits (IC50s = 0.27 and 29.6 µM, respectively, in X. laevis oocytes expressing receptors containing the respective subunits). NVP-AAM077 inhibits seizures induced by maximal electroshock (MES) in mice with an ED50 value of 23 mg/kg. It increases the activity of neuronal nitric oxide synthase (nNOS) in primary hippocampal neurons.{61131} NVP-AAM077 (10 mg/kg) inhibits proliferation of neural progenitor cells (NPCs) in the subventricular zone (SVZ) and in the subgranular zone (SGZ) of the hippocampal dentate gyrus of adult mice, an effect not seen in nNOS-/- mice. It also increases the escape latency and decreases the percentage of time spent in the target quadrant in the Morris water maze.
Brand:CaymanSKU:30622 - 5 mgAvailable on backorder
NVP-ACC789 is an inhibitor of VEGF receptor tyrosine kinases (VEGFRs; IC50s = 0.38, 0.02, 0.18, and 0.23 μM for human VEGFR1, 2, 3, and mouse Vegfr2, respectively).{37221} It is selective for VEGFRs over FGFRs and PDGFRα (IC50s = >10 μM) but has activity at PDGFRβ (IC50 = 1.4 μM) in an enzyme assay. NVP-ACC789 inhibits VEGF-induced VEGFR2 autophosphorylation (IC50 = 11.5 nM in CHO cells transfected with the human receptor). It also inhibits VEGF- and bFGF-induced angiogenesis and cell migration of BAE and BME cells. In vivo, NVP-ACC789 blocks bFGF- and VEGF-induced angiogenesis (ED50s = 9 and 26 mg/kg, respectively) in a mouse model of growth factor-induced angiogenesis.
Brand:CaymanSKU:23458 - 1 mgAvailable on backorder
NVP-ACC789 is an inhibitor of VEGF receptor tyrosine kinases (VEGFRs; IC50s = 0.38, 0.02, 0.18, and 0.23 μM for human VEGFR1, 2, 3, and mouse Vegfr2, respectively).{37221} It is selective for VEGFRs over FGFRs and PDGFRα (IC50s = >10 μM) but has activity at PDGFRβ (IC50 = 1.4 μM) in an enzyme assay. NVP-ACC789 inhibits VEGF-induced VEGFR2 autophosphorylation (IC50 = 11.5 nM in CHO cells transfected with the human receptor). It also inhibits VEGF- and bFGF-induced angiogenesis and cell migration of BAE and BME cells. In vivo, NVP-ACC789 blocks bFGF- and VEGF-induced angiogenesis (ED50s = 9 and 26 mg/kg, respectively) in a mouse model of growth factor-induced angiogenesis.
Brand:CaymanSKU:23458 - 10 mgAvailable on backorder
NVP-ACC789 is an inhibitor of VEGF receptor tyrosine kinases (VEGFRs; IC50s = 0.38, 0.02, 0.18, and 0.23 μM for human VEGFR1, 2, 3, and mouse Vegfr2, respectively).{37221} It is selective for VEGFRs over FGFRs and PDGFRα (IC50s = >10 μM) but has activity at PDGFRβ (IC50 = 1.4 μM) in an enzyme assay. NVP-ACC789 inhibits VEGF-induced VEGFR2 autophosphorylation (IC50 = 11.5 nM in CHO cells transfected with the human receptor). It also inhibits VEGF- and bFGF-induced angiogenesis and cell migration of BAE and BME cells. In vivo, NVP-ACC789 blocks bFGF- and VEGF-induced angiogenesis (ED50s = 9 and 26 mg/kg, respectively) in a mouse model of growth factor-induced angiogenesis.
Brand:CaymanSKU:23458 - 5 mgAvailable on backorder
NVP-ADW742 is an insulin-like growth factor 1 receptor (IGF-1R) inhibitor with an IC50 value of 0.17 µM.{31811} It exhibits 6-fold greater selectivity for IGF-1R over the insulin receptor (InsR) kinase and minimal inhibitory activity against c-Kit, HER1, PDGFR, VEGFR2, or Bcr-Abl p210.{31811} NVP-ADW742 has been shown to inhibit tumor proliferation both in vitro and in a mouse model of multiple myeloma.{31811}
Brand:CaymanSKU:-Available on backorder