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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:23499 - 1 mg

    Available 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:
    Cayman
    SKU:23499 - 10 mg

    Available 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:
    Cayman
    SKU:23499 - 25 mg

    Available 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:
    Cayman
    SKU:23499 - 5 mg

    Available 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:
    Cayman
    SKU:-

    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:
    Cayman
    SKU:-

    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:
    Cayman
    SKU:-

    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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:29226 - 1 mg

    Available 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:
    Cayman
    SKU:29226 - 10 mg

    Available 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:
    Cayman
    SKU:29226 - 5 mg

    Available 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU: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:
    Cayman
    SKU: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:
    Cayman
    SKU: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:
    Cayman
    SKU: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:
    Cayman
    SKU:26166 - 1 mg

    Available 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:
    Cayman
    SKU:26166 - 5 mg

    Available 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU: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:
    Cayman
    SKU: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:
    Cayman
    SKU: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:
    Cayman
    SKU: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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-

    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:
    Cayman
    SKU:-

    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:
    Cayman
    SKU:-

    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:
    Cayman
    SKU:-

    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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:9003247 - 1 mg

    Available 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:
    Cayman
    SKU:9003247 - 10 mg

    Available 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:
    Cayman
    SKU:9003247 - 5 mg

    Available 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:
    Cayman
    SKU:25178 - 10 mg

    Available 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:
    Cayman
    SKU:25178 - 25 mg

    Available 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:
    Cayman
    SKU:25178 - 5 mg

    Available 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:
    Cayman
    SKU:30363 - 10 mg

    Available 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:
    Cayman
    SKU:30363 - 25 mg

    Available 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:
    Cayman
    SKU:30363 - 5 mg

    Available 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:
    Cayman
    SKU:30363 - 50 mg

    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:
    Cayman
    SKU: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:
    Cayman
    SKU: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:
    Cayman
    SKU: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:
    Cayman
    SKU: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:
    Cayman
    SKU:-

    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:
    Cayman
    SKU:-

    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:
    Cayman
    SKU:-

    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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:30622 - 1 mg

    Available 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:
    Cayman
    SKU:30622 - 10 mg

    Available 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:
    Cayman
    SKU:30622 - 25 mg

    Available 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:
    Cayman
    SKU:30622 - 5 mg

    Available 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:
    Cayman
    SKU:23458 - 1 mg

    Available 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:
    Cayman
    SKU:23458 - 10 mg

    Available 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:
    Cayman
    SKU:23458 - 5 mg

    Available 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:
    Cayman
    SKU:-

    Available 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:
    Cayman
    SKU:-

    Available 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:
    Cayman
    SKU:-

    Available 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:
    Cayman
    SKU:-

    Available on backorder

  • Hsp90 is a molecular chaperone of many different kinases, transcription factors, and hormone receptors involved in signal transduction, cell cycle regulation, and apoptosis. In addition to its important function in normal cell homeostasis, a high affinity form of Hsp90 is prevalent in tumor cells. Hsp90 inhibition has been associated with the degradation of oncogenic client proteins. NVP-AUY922 is a Hsp90 inhibitor (IC50 = 21 nM in a FP binding assay) that prevents the proliferation of a range of human cancer cell lines in vitro with GI50s averaging 9 nM.{15809} In a human colon cancer xenograft model, 50 mg/kg NVP-AUY922 inhibits tumor growth by ~50% compared to vehicle controls.{15809} Unlike some first generation Hsp90 inhibitors that are quickly glucuronidated, NVP-AUY922 is retained in tumors in vivo when administered at 4 mg/kg i.p. by cassette dosing in tumor-bearing mice.{15809}  

     

    Brand:
    Cayman
    SKU:10012698 - 10 mg

    Available on backorder

  • Hsp90 is a molecular chaperone of many different kinases, transcription factors, and hormone receptors involved in signal transduction, cell cycle regulation, and apoptosis. In addition to its important function in normal cell homeostasis, a high affinity form of Hsp90 is prevalent in tumor cells. Hsp90 inhibition has been associated with the degradation of oncogenic client proteins. NVP-AUY922 is a Hsp90 inhibitor (IC50 = 21 nM in a FP binding assay) that prevents the proliferation of a range of human cancer cell lines in vitro with GI50s averaging 9 nM.{15809} In a human colon cancer xenograft model, 50 mg/kg NVP-AUY922 inhibits tumor growth by ~50% compared to vehicle controls.{15809} Unlike some first generation Hsp90 inhibitors that are quickly glucuronidated, NVP-AUY922 is retained in tumors in vivo when administered at 4 mg/kg i.p. by cassette dosing in tumor-bearing mice.{15809}  

     

    Brand:
    Cayman
    SKU:10012698 - 5 mg

    Available on backorder

  • NVP-BAG956 is a dual inhibitor of 3-phosphoinositide-dependent protein kinase 1 (PDK1; IC50 = 245 nM) and class I phosphatidylinositol 3-kinase catalytic subunits (PI3Ks; IC50s = 56, 446, 35, and 117 nM for p110α, p110β, p110δ, and p110γ, respectively).{36931} It inhibits phosphorylation of T308-PKB (IC50 = 45 nM) in and proliferation of U87MG cells (EC50 = 143 nM). NVP-BAG956 decreases cell viability in a panel of human leukemia cell lines (IC50s = 1 phase in MOLM-14 cells and reduces colony formation by patient-derived acute myeloid leukemia (AML) cells. NVP-BAG956 (75 mg/kg) reduces tumor burden in mice injected with 32D.p210-luc+cells when administered in combination with everolimus (Item No. 11597).  

     

    Brand:
    Cayman
    SKU:24195 - 1 mg

    Available on backorder

  • NVP-BAG956 is a dual inhibitor of 3-phosphoinositide-dependent protein kinase 1 (PDK1; IC50 = 245 nM) and class I phosphatidylinositol 3-kinase catalytic subunits (PI3Ks; IC50s = 56, 446, 35, and 117 nM for p110α, p110β, p110δ, and p110γ, respectively).{36931} It inhibits phosphorylation of T308-PKB (IC50 = 45 nM) in and proliferation of U87MG cells (EC50 = 143 nM). NVP-BAG956 decreases cell viability in a panel of human leukemia cell lines (IC50s = 1 phase in MOLM-14 cells and reduces colony formation by patient-derived acute myeloid leukemia (AML) cells. NVP-BAG956 (75 mg/kg) reduces tumor burden in mice injected with 32D.p210-luc+cells when administered in combination with everolimus (Item No. 11597).  

     

    Brand:
    Cayman
    SKU:24195 - 10 mg

    Available on backorder

  • NVP-BAG956 is a dual inhibitor of 3-phosphoinositide-dependent protein kinase 1 (PDK1; IC50 = 245 nM) and class I phosphatidylinositol 3-kinase catalytic subunits (PI3Ks; IC50s = 56, 446, 35, and 117 nM for p110α, p110β, p110δ, and p110γ, respectively).{36931} It inhibits phosphorylation of T308-PKB (IC50 = 45 nM) in and proliferation of U87MG cells (EC50 = 143 nM). NVP-BAG956 decreases cell viability in a panel of human leukemia cell lines (IC50s = 1 phase in MOLM-14 cells and reduces colony formation by patient-derived acute myeloid leukemia (AML) cells. NVP-BAG956 (75 mg/kg) reduces tumor burden in mice injected with 32D.p210-luc+cells when administered in combination with everolimus (Item No. 11597).  

     

    Brand:
    Cayman
    SKU:24195 - 5 mg

    Available on backorder

  • NVP-BEP800 is an inhibitor of heat shock protein 90 (Hsp90; IC50 = 58 nM for recombinant human Hsp90β).{29919} It is selective for Hsp90 over the chaperones GRP94 and TRAP1 (IC50s = 4.1 and 5.5 µM, respectively). NVP-BEP800 inhibits the growth of BT474, SK-BR-3, MCF-7, MDA-MB-157, MDA-MB-231, MDA-MB-468, and BT-20 breast cancer cells (GI50s = 53, 56, 118, 89, 190, 173, and 162 nM, respectively). It reduces levels of the Hsp90 target proteins HER2 and Raf-1 in MCF-7 cells. NVP-BEP800 induces apoptosis and attenuates X-ray-induced increases in Hsp70 levels in T98G glioblastoma cells.{29922} NVP-BEP800 (15-50 mg/kg) reduces tumor volume in A375 melanoma and BT474 breast cancer mouse xenograft models.{29919} It also reduces tumor volume in an L1T2 Kaposi sarcoma mouse xenograft model.{29918}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • NVP-BEP800 is an inhibitor of heat shock protein 90 (Hsp90; IC50 = 58 nM for recombinant human Hsp90β).{29919} It is selective for Hsp90 over the chaperones GRP94 and TRAP1 (IC50s = 4.1 and 5.5 µM, respectively). NVP-BEP800 inhibits the growth of BT474, SK-BR-3, MCF-7, MDA-MB-157, MDA-MB-231, MDA-MB-468, and BT-20 breast cancer cells (GI50s = 53, 56, 118, 89, 190, 173, and 162 nM, respectively). It reduces levels of the Hsp90 target proteins HER2 and Raf-1 in MCF-7 cells. NVP-BEP800 induces apoptosis and attenuates X-ray-induced increases in Hsp70 levels in T98G glioblastoma cells.{29922} NVP-BEP800 (15-50 mg/kg) reduces tumor volume in A375 melanoma and BT474 breast cancer mouse xenograft models.{29919} It also reduces tumor volume in an L1T2 Kaposi sarcoma mouse xenograft model.{29918}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • NVP-BEP800 is an inhibitor of heat shock protein 90 (Hsp90; IC50 = 58 nM for recombinant human Hsp90β).{29919} It is selective for Hsp90 over the chaperones GRP94 and TRAP1 (IC50s = 4.1 and 5.5 µM, respectively). NVP-BEP800 inhibits the growth of BT474, SK-BR-3, MCF-7, MDA-MB-157, MDA-MB-231, MDA-MB-468, and BT-20 breast cancer cells (GI50s = 53, 56, 118, 89, 190, 173, and 162 nM, respectively). It reduces levels of the Hsp90 target proteins HER2 and Raf-1 in MCF-7 cells. NVP-BEP800 induces apoptosis and attenuates X-ray-induced increases in Hsp70 levels in T98G glioblastoma cells.{29922} NVP-BEP800 (15-50 mg/kg) reduces tumor volume in A375 melanoma and BT474 breast cancer mouse xenograft models.{29919} It also reduces tumor volume in an L1T2 Kaposi sarcoma mouse xenograft model.{29918}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • NVP-BEP800 is an inhibitor of heat shock protein 90 (Hsp90; IC50 = 58 nM for recombinant human Hsp90β).{29919} It is selective for Hsp90 over the chaperones GRP94 and TRAP1 (IC50s = 4.1 and 5.5 µM, respectively). NVP-BEP800 inhibits the growth of BT474, SK-BR-3, MCF-7, MDA-MB-157, MDA-MB-231, MDA-MB-468, and BT-20 breast cancer cells (GI50s = 53, 56, 118, 89, 190, 173, and 162 nM, respectively). It reduces levels of the Hsp90 target proteins HER2 and Raf-1 in MCF-7 cells. NVP-BEP800 induces apoptosis and attenuates X-ray-induced increases in Hsp70 levels in T98G glioblastoma cells.{29922} NVP-BEP800 (15-50 mg/kg) reduces tumor volume in A375 melanoma and BT474 breast cancer mouse xenograft models.{29919} It also reduces tumor volume in an L1T2 Kaposi sarcoma mouse xenograft model.{29918}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Phosphatidylinositol 3-kinase (PI3K) signaling through Akt/PKB and the mammalian target of rapamycin (mTOR) controls gene expression related to cell proliferation, differentiation, and apoptosis. Increased activity of this pathway is important in many types of cancer. NVP-BEZ235 is a potent dual inhibitor of PI3K and mTOR that is well tolerated, displays disease stasis when administered orally, and enhances the efficacy of other anticancer agents when used in in vivo combination studies.{18570,18573} It inhibits PI3K isoforms and mutants with low nanomolar IC50 values, leading to growth arrest in the G1 phase.{18570,18572} Through its effects on PI3K, NVP-BEZ235 inhibits VEGF-induced angiogenesis.{18571} By directly blocking cell growth and indirectly inhibiting angiogenesis, it has potential in both solid tumors and in metastatic melanoma therapy.{18574,18575}  

     

    Brand:
    Cayman
    SKU:10565 - 100 mg

    Available on backorder

  • Phosphatidylinositol 3-kinase (PI3K) signaling through Akt/PKB and the mammalian target of rapamycin (mTOR) controls gene expression related to cell proliferation, differentiation, and apoptosis. Increased activity of this pathway is important in many types of cancer. NVP-BEZ235 is a potent dual inhibitor of PI3K and mTOR that is well tolerated, displays disease stasis when administered orally, and enhances the efficacy of other anticancer agents when used in in vivo combination studies.{18570,18573} It inhibits PI3K isoforms and mutants with low nanomolar IC50 values, leading to growth arrest in the G1 phase.{18570,18572} Through its effects on PI3K, NVP-BEZ235 inhibits VEGF-induced angiogenesis.{18571} By directly blocking cell growth and indirectly inhibiting angiogenesis, it has potential in both solid tumors and in metastatic melanoma therapy.{18574,18575}  

     

    Brand:
    Cayman
    SKU:10565 - 25 mg

    Available on backorder

  • Phosphatidylinositol 3-kinase (PI3K) signaling through Akt/PKB and the mammalian target of rapamycin (mTOR) controls gene expression related to cell proliferation, differentiation, and apoptosis. Increased activity of this pathway is important in many types of cancer. NVP-BEZ235 is a potent dual inhibitor of PI3K and mTOR that is well tolerated, displays disease stasis when administered orally, and enhances the efficacy of other anticancer agents when used in in vivo combination studies.{18570,18573} It inhibits PI3K isoforms and mutants with low nanomolar IC50 values, leading to growth arrest in the G1 phase.{18570,18572} Through its effects on PI3K, NVP-BEZ235 inhibits VEGF-induced angiogenesis.{18571} By directly blocking cell growth and indirectly inhibiting angiogenesis, it has potential in both solid tumors and in metastatic melanoma therapy.{18574,18575}  

     

    Brand:
    Cayman
    SKU:10565 - 250 mg

    Available on backorder

  • Phosphatidylinositol 3-kinase (PI3K) signaling through Akt/PKB and the mammalian target of rapamycin (mTOR) controls gene expression related to cell proliferation, differentiation, and apoptosis. Increased activity of this pathway is important in many types of cancer. NVP-BEZ235 is a potent dual inhibitor of PI3K and mTOR that is well tolerated, displays disease stasis when administered orally, and enhances the efficacy of other anticancer agents when used in in vivo combination studies.{18570,18573} It inhibits PI3K isoforms and mutants with low nanomolar IC50 values, leading to growth arrest in the G1 phase.{18570,18572} Through its effects on PI3K, NVP-BEZ235 inhibits VEGF-induced angiogenesis.{18571} By directly blocking cell growth and indirectly inhibiting angiogenesis, it has potential in both solid tumors and in metastatic melanoma therapy.{18574,18575}  

     

    Brand:
    Cayman
    SKU:10565 - 50 mg

    Available on backorder

  • NVP-BGT226 is an orally bioavailable dual inhibitor of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR).{35140} It inhibits class I PI3Ks with EC50 values of 4, 63, and 38 nM for PI3Kα, β, and γ isoforms, respectively, in a filter binding assay. It binds to both class I and class III PI3Ks in a quantitative ELISA assay with EC50 values of 55.8 and 7.03 nM, for HsPI3Kβ and HsVps34, respectively.{35142} It decreases protein levels of phosphorylated mTOR and Akt, a downstream target of PI3K signaling.{36351} NVP-BGT226 inhibits the growth of squamous cell carcinoma cell lines, HONE-1, and a variant of HONE-1 resistant to cisplatin (Item No. 13119) with IC50 values of 7.4-27.8, 22.6, and 30.1 nM, respectively.{35138} It halts the cell cycle at the G0/G1 phase and induces autophagy. NVP-BGT226 (2.5 and 5 mg/kg daily for three weeks) inhibits tumor growth in a FaDu head and neck cancer mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:22142 -

    Out of stock

  • NVP-BGT226 is an orally bioavailable dual inhibitor of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR).{35140} It inhibits class I PI3Ks with EC50 values of 4, 63, and 38 nM for PI3Kα, β, and γ isoforms, respectively, in a filter binding assay. It binds to both class I and class III PI3Ks in a quantitative ELISA assay with EC50 values of 55.8 and 7.03 nM, for HsPI3Kβ and HsVps34, respectively.{35142} It decreases protein levels of phosphorylated mTOR and Akt, a downstream target of PI3K signaling.{36351} NVP-BGT226 inhibits the growth of squamous cell carcinoma cell lines, HONE-1, and a variant of HONE-1 resistant to cisplatin (Item No. 13119) with IC50 values of 7.4-27.8, 22.6, and 30.1 nM, respectively.{35138} It halts the cell cycle at the G0/G1 phase and induces autophagy. NVP-BGT226 (2.5 and 5 mg/kg daily for three weeks) inhibits tumor growth in a FaDu head and neck cancer mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:22142 -

    Out of stock

  • NVP-BGT226 is an orally bioavailable dual inhibitor of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR).{35140} It inhibits class I PI3Ks with EC50 values of 4, 63, and 38 nM for PI3Kα, β, and γ isoforms, respectively, in a filter binding assay. It binds to both class I and class III PI3Ks in a quantitative ELISA assay with EC50 values of 55.8 and 7.03 nM, for HsPI3Kβ and HsVps34, respectively.{35142} It decreases protein levels of phosphorylated mTOR and Akt, a downstream target of PI3K signaling.{36351} NVP-BGT226 inhibits the growth of squamous cell carcinoma cell lines, HONE-1, and a variant of HONE-1 resistant to cisplatin (Item No. 13119) with IC50 values of 7.4-27.8, 22.6, and 30.1 nM, respectively.{35138} It halts the cell cycle at the G0/G1 phase and induces autophagy. NVP-BGT226 (2.5 and 5 mg/kg daily for three weeks) inhibits tumor growth in a FaDu head and neck cancer mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:22142 -

    Out of stock

  • NVP-BGT226 is an orally bioavailable dual inhibitor of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR).{35140} It inhibits class I PI3Ks with EC50 values of 4, 63, and 38 nM for PI3Kα, β, and γ isoforms, respectively, in a filter binding assay. It binds to both class I and class III PI3Ks in a quantitative ELISA assay with EC50 values of 55.8 and 7.03 nM, for HsPI3Kβ and HsVps34, respectively.{35142} It decreases protein levels of phosphorylated mTOR and Akt, a downstream target of PI3K signaling.{36351} NVP-BGT226 inhibits the growth of squamous cell carcinoma cell lines, HONE-1, and a variant of HONE-1 resistant to cisplatin (Item No. 13119) with IC50 values of 7.4-27.8, 22.6, and 30.1 nM, respectively.{35138} It halts the cell cycle at the G0/G1 phase and induces autophagy. NVP-BGT226 (2.5 and 5 mg/kg daily for three weeks) inhibits tumor growth in a FaDu head and neck cancer mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:22142 -

    Out of stock

  • The EphB4 receptor tyrosine kinase (cloned from erythropoietin-producing hepatocellular carcinoma) and its ligand ephrinB2 play an important role in embryonic vessel development and vascular remodeling. Signaling from this pair is also involved in tumor angiogenesis. NVP-BHG712 is an orally bioavailable inhibitor of EphB4 kinase autophosphorylation (ED50 = 25 nM).{29822} It is selective for EphB4, demonstrating an ED50 value of 4.2 µM at the related VEGFR2 receptor and ED50 values >10 µM against a panel of 40 additional kinases.{29822} At 3-30 mg/kg, NVP-BHG712 dose dependently inhibits VEGF-directed vessel formation in an in vivo mouse model of angiogenesis.{29822}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • The EphB4 receptor tyrosine kinase (cloned from erythropoietin-producing hepatocellular carcinoma) and its ligand ephrinB2 play an important role in embryonic vessel development and vascular remodeling. Signaling from this pair is also involved in tumor angiogenesis. NVP-BHG712 is an orally bioavailable inhibitor of EphB4 kinase autophosphorylation (ED50 = 25 nM).{29822} It is selective for EphB4, demonstrating an ED50 value of 4.2 µM at the related VEGFR2 receptor and ED50 values >10 µM against a panel of 40 additional kinases.{29822} At 3-30 mg/kg, NVP-BHG712 dose dependently inhibits VEGF-directed vessel formation in an in vivo mouse model of angiogenesis.{29822}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • The EphB4 receptor tyrosine kinase (cloned from erythropoietin-producing hepatocellular carcinoma) and its ligand ephrinB2 play an important role in embryonic vessel development and vascular remodeling. Signaling from this pair is also involved in tumor angiogenesis. NVP-BHG712 is an orally bioavailable inhibitor of EphB4 kinase autophosphorylation (ED50 = 25 nM).{29822} It is selective for EphB4, demonstrating an ED50 value of 4.2 µM at the related VEGFR2 receptor and ED50 values >10 µM against a panel of 40 additional kinases.{29822} At 3-30 mg/kg, NVP-BHG712 dose dependently inhibits VEGF-directed vessel formation in an in vivo mouse model of angiogenesis.{29822}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • The EphB4 receptor tyrosine kinase (cloned from erythropoietin-producing hepatocellular carcinoma) and its ligand ephrinB2 play an important role in embryonic vessel development and vascular remodeling. Signaling from this pair is also involved in tumor angiogenesis. NVP-BHG712 is an orally bioavailable inhibitor of EphB4 kinase autophosphorylation (ED50 = 25 nM).{29822} It is selective for EphB4, demonstrating an ED50 value of 4.2 µM at the related VEGFR2 receptor and ED50 values >10 µM against a panel of 40 additional kinases.{29822} At 3-30 mg/kg, NVP-BHG712 dose dependently inhibits VEGF-directed vessel formation in an in vivo mouse model of angiogenesis.{29822}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • NVP-BKM120 is an orally bioavailable inhibitor of the class I PI3K isoforms p110α (IC50 = 52 nM) and p110β (IC50 = 166 nM).{23146} It is selective for these isoforms over the class III PI3K Vps34 (IC50 = 2,410 nM), the mammalian target of rapamycin (mTOR; IC50 = 2,866 nM), PI4Kβ (IC50 = >25,000 nM), and a variety of kinases (IC50s = >10,000 nM). NVP-BKM120 inhibits proliferation of human tumor and glioma cell lines, with p53 wild-type glioma cells being more sensitive than p53 mutant/deleted glioma cells (IC50s = 1.28 and 2.08 µM, respectively).{23147,23145} It halts the cell cycle in the G2/M phase in both p53 wild-type and p53 mutant/deleted glioma cells, but p53 mutant/deleted cells reenter the cell cycle, progress into mitosis, and die via mitotic catastrophic cell death. NVP-BKM120 (1-5 mg/kg) crosses the blood brain barrier and selectively decreases phosphorylation of the PI3K target protein Akt.{36845} It increases survival in a U87 glioma mouse xenograft intracranial tumor model when administered orally at doses of 20 and 40 mg/kg once per week.{23147}  

     

    Brand:
    Cayman
    SKU:11587 - 1 mg

    Available on backorder

  • NVP-BKM120 is an orally bioavailable inhibitor of the class I PI3K isoforms p110α (IC50 = 52 nM) and p110β (IC50 = 166 nM).{23146} It is selective for these isoforms over the class III PI3K Vps34 (IC50 = 2,410 nM), the mammalian target of rapamycin (mTOR; IC50 = 2,866 nM), PI4Kβ (IC50 = >25,000 nM), and a variety of kinases (IC50s = >10,000 nM). NVP-BKM120 inhibits proliferation of human tumor and glioma cell lines, with p53 wild-type glioma cells being more sensitive than p53 mutant/deleted glioma cells (IC50s = 1.28 and 2.08 µM, respectively).{23147,23145} It halts the cell cycle in the G2/M phase in both p53 wild-type and p53 mutant/deleted glioma cells, but p53 mutant/deleted cells reenter the cell cycle, progress into mitosis, and die via mitotic catastrophic cell death. NVP-BKM120 (1-5 mg/kg) crosses the blood brain barrier and selectively decreases phosphorylation of the PI3K target protein Akt.{36845} It increases survival in a U87 glioma mouse xenograft intracranial tumor model when administered orally at doses of 20 and 40 mg/kg once per week.{23147}  

     

    Brand:
    Cayman
    SKU:11587 - 10 mg

    Available on backorder

  • NVP-BKM120 is an orally bioavailable inhibitor of the class I PI3K isoforms p110α (IC50 = 52 nM) and p110β (IC50 = 166 nM).{23146} It is selective for these isoforms over the class III PI3K Vps34 (IC50 = 2,410 nM), the mammalian target of rapamycin (mTOR; IC50 = 2,866 nM), PI4Kβ (IC50 = >25,000 nM), and a variety of kinases (IC50s = >10,000 nM). NVP-BKM120 inhibits proliferation of human tumor and glioma cell lines, with p53 wild-type glioma cells being more sensitive than p53 mutant/deleted glioma cells (IC50s = 1.28 and 2.08 µM, respectively).{23147,23145} It halts the cell cycle in the G2/M phase in both p53 wild-type and p53 mutant/deleted glioma cells, but p53 mutant/deleted cells reenter the cell cycle, progress into mitosis, and die via mitotic catastrophic cell death. NVP-BKM120 (1-5 mg/kg) crosses the blood brain barrier and selectively decreases phosphorylation of the PI3K target protein Akt.{36845} It increases survival in a U87 glioma mouse xenograft intracranial tumor model when administered orally at doses of 20 and 40 mg/kg once per week.{23147}  

     

    Brand:
    Cayman
    SKU:11587 - 25 mg

    Available on backorder

  • NVP-BKM120 is an orally bioavailable inhibitor of the class I PI3K isoforms p110α (IC50 = 52 nM) and p110β (IC50 = 166 nM).{23146} It is selective for these isoforms over the class III PI3K Vps34 (IC50 = 2,410 nM), the mammalian target of rapamycin (mTOR; IC50 = 2,866 nM), PI4Kβ (IC50 = >25,000 nM), and a variety of kinases (IC50s = >10,000 nM). NVP-BKM120 inhibits proliferation of human tumor and glioma cell lines, with p53 wild-type glioma cells being more sensitive than p53 mutant/deleted glioma cells (IC50s = 1.28 and 2.08 µM, respectively).{23147,23145} It halts the cell cycle in the G2/M phase in both p53 wild-type and p53 mutant/deleted glioma cells, but p53 mutant/deleted cells reenter the cell cycle, progress into mitosis, and die via mitotic catastrophic cell death. NVP-BKM120 (1-5 mg/kg) crosses the blood brain barrier and selectively decreases phosphorylation of the PI3K target protein Akt.{36845} It increases survival in a U87 glioma mouse xenograft intracranial tumor model when administered orally at doses of 20 and 40 mg/kg once per week.{23147}  

     

    Brand:
    Cayman
    SKU:11587 - 5 mg

    Available on backorder

  • Janus kinases (JAKs) are non-receptor tyrosine kinases that mediate signaling through cytokine receptors, often to members of the signal transducer and activator of transcription (STAT) family.{20362} A point mutation of JAK2, V617F, activates signaling through STAT5 and drives certain forms of cancer.{27443} NVP-BSK805 is a potent inhibitor of JAK2 that also inhibits the JAK2V617F mutant enzyme (IC50s for both enzymes ~ 0.5 nM). It displays at least 20-fold selectivity against other JAK enzymes and a panel of serine/threonine and tyrosine kinases.{27443} This ATP-competitive inhibitor is orally bioavailable and has a long half-life in vivo, suppressing leukemic cell spreading and splenomegaly in JAK2V617F cell-driven disease in mice.{27443} NVP-BSK805 suppresses recombinant human erythropoietin-induced polycythemia and extramedullary erythropoiesis in mice and rats.{27443} NVP-BSK805 can be used to study the molecular mechanisms involved in JAK2V617F signaling in cells.{27444}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Janus kinases (JAKs) are non-receptor tyrosine kinases that mediate signaling through cytokine receptors, often to members of the signal transducer and activator of transcription (STAT) family.{20362} A point mutation of JAK2, V617F, activates signaling through STAT5 and drives certain forms of cancer.{27443} NVP-BSK805 is a potent inhibitor of JAK2 that also inhibits the JAK2V617F mutant enzyme (IC50s for both enzymes ~ 0.5 nM). It displays at least 20-fold selectivity against other JAK enzymes and a panel of serine/threonine and tyrosine kinases.{27443} This ATP-competitive inhibitor is orally bioavailable and has a long half-life in vivo, suppressing leukemic cell spreading and splenomegaly in JAK2V617F cell-driven disease in mice.{27443} NVP-BSK805 suppresses recombinant human erythropoietin-induced polycythemia and extramedullary erythropoiesis in mice and rats.{27443} NVP-BSK805 can be used to study the molecular mechanisms involved in JAK2V617F signaling in cells.{27444}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Janus kinases (JAKs) are non-receptor tyrosine kinases that mediate signaling through cytokine receptors, often to members of the signal transducer and activator of transcription (STAT) family.{20362} A point mutation of JAK2, V617F, activates signaling through STAT5 and drives certain forms of cancer.{27443} NVP-BSK805 is a potent inhibitor of JAK2 that also inhibits the JAK2V617F mutant enzyme (IC50s for both enzymes ~ 0.5 nM). It displays at least 20-fold selectivity against other JAK enzymes and a panel of serine/threonine and tyrosine kinases.{27443} This ATP-competitive inhibitor is orally bioavailable and has a long half-life in vivo, suppressing leukemic cell spreading and splenomegaly in JAK2V617F cell-driven disease in mice.{27443} NVP-BSK805 suppresses recombinant human erythropoietin-induced polycythemia and extramedullary erythropoiesis in mice and rats.{27443} NVP-BSK805 can be used to study the molecular mechanisms involved in JAK2V617F signaling in cells.{27444}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • NVP-CGM097 is an inhibitor of the protein-protein interaction between murine double minute 2 (MDM2) and p53 (IC50 = 1.7 nM for human MDM2 in a TR-FRET assay).{53380} It is selective for human MDM2 (Ki = 1.3 nM) over dog, mouse, and rat Mdm2 (Kis = 20.5, 65.9, and 47.4 nM, respectively).{53381} NVP-CGM097 selectively inhibits proliferation of acute myeloid leukemia (AML) cells expressing wild-type p53 (IC50s = 50-1,000 nM) over AML cells expressing mutant p53 (IC50s = >1,000 nM).{53380} It induces tumor regression in a patient-derived xenograft (PDX) mouse model of AML when administered at a dose of 100 mg/kg per day.{53380}  

     

    Brand:
    Cayman
    SKU:29519 - 1 mg

    Available on backorder

  • NVP-CGM097 is an inhibitor of the protein-protein interaction between murine double minute 2 (MDM2) and p53 (IC50 = 1.7 nM for human MDM2 in a TR-FRET assay).{53380} It is selective for human MDM2 (Ki = 1.3 nM) over dog, mouse, and rat Mdm2 (Kis = 20.5, 65.9, and 47.4 nM, respectively).{53381} NVP-CGM097 selectively inhibits proliferation of acute myeloid leukemia (AML) cells expressing wild-type p53 (IC50s = 50-1,000 nM) over AML cells expressing mutant p53 (IC50s = >1,000 nM).{53380} It induces tumor regression in a patient-derived xenograft (PDX) mouse model of AML when administered at a dose of 100 mg/kg per day.{53380}  

     

    Brand:
    Cayman
    SKU:29519 - 10 mg

    Available on backorder

  • NVP-CGM097 is an inhibitor of the protein-protein interaction between murine double minute 2 (MDM2) and p53 (IC50 = 1.7 nM for human MDM2 in a TR-FRET assay).{53380} It is selective for human MDM2 (Ki = 1.3 nM) over dog, mouse, and rat Mdm2 (Kis = 20.5, 65.9, and 47.4 nM, respectively).{53381} NVP-CGM097 selectively inhibits proliferation of acute myeloid leukemia (AML) cells expressing wild-type p53 (IC50s = 50-1,000 nM) over AML cells expressing mutant p53 (IC50s = >1,000 nM).{53380} It induces tumor regression in a patient-derived xenograft (PDX) mouse model of AML when administered at a dose of 100 mg/kg per day.{53380}  

     

    Brand:
    Cayman
    SKU:29519 - 5 mg

    Available on backorder

  • NVP-TAE226 is an inhibitor of focal adhesion kinase (FAK; IC50 = 5.5 nM) and the related proline-rich tyrosine kinase 2-β (PYK2β; IC50 = 5 nM).{32642} It can also inhibit the insulin-like growth factor 1 receptor (IC50 = 0.16 µM) as well as the activity of its downstream target genes such as MAPK and Akt.{32642} NVP-TAE226 has been shown to inhibit glioma and ovarian tumor growth in in vivo tumor models.{15631}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • NVP-TAE226 is an inhibitor of focal adhesion kinase (FAK; IC50 = 5.5 nM) and the related proline-rich tyrosine kinase 2-β (PYK2β; IC50 = 5 nM).{32642} It can also inhibit the insulin-like growth factor 1 receptor (IC50 = 0.16 µM) as well as the activity of its downstream target genes such as MAPK and Akt.{32642} NVP-TAE226 has been shown to inhibit glioma and ovarian tumor growth in in vivo tumor models.{15631}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • NVP-TAE226 is an inhibitor of focal adhesion kinase (FAK; IC50 = 5.5 nM) and the related proline-rich tyrosine kinase 2-β (PYK2β; IC50 = 5 nM).{32642} It can also inhibit the insulin-like growth factor 1 receptor (IC50 = 0.16 µM) as well as the activity of its downstream target genes such as MAPK and Akt.{32642} NVP-TAE226 has been shown to inhibit glioma and ovarian tumor growth in in vivo tumor models.{15631}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • NVP-TAE226 is an inhibitor of focal adhesion kinase (FAK; IC50 = 5.5 nM) and the related proline-rich tyrosine kinase 2-β (PYK2β; IC50 = 5 nM).{32642} It can also inhibit the insulin-like growth factor 1 receptor (IC50 = 0.16 µM) as well as the activity of its downstream target genes such as MAPK and Akt.{32642} NVP-TAE226 has been shown to inhibit glioma and ovarian tumor growth in in vivo tumor models.{15631}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • NVP-TNKS656 is an orally bioavailable inhibitor of tankyrase 2 (TNKS2; IC50 = 6 nM).{40669} It is selective for TNKS2 over poly(ADP-ribose) polymerase (PARP) 1 and 2 (IC50s = >19 and 32 nM, respectively). NVP-TNKS656 inhibits Wnt ligand-induced signaling with an IC50 value of 3.5 nM in an HEK293 cell reporter assay. In vivo, NVP-TNKS656 (350 mg/kg) reduces Axin 2 mRNA expression, a Wnt/β-catenin target gene, in MMTV-Wnt1 tumor bearing mice.  

     

    Brand:
    Cayman
    SKU:19930 -

    Available on backorder

  • NVP-TNKS656 is an orally bioavailable inhibitor of tankyrase 2 (TNKS2; IC50 = 6 nM).{40669} It is selective for TNKS2 over poly(ADP-ribose) polymerase (PARP) 1 and 2 (IC50s = >19 and 32 nM, respectively). NVP-TNKS656 inhibits Wnt ligand-induced signaling with an IC50 value of 3.5 nM in an HEK293 cell reporter assay. In vivo, NVP-TNKS656 (350 mg/kg) reduces Axin 2 mRNA expression, a Wnt/β-catenin target gene, in MMTV-Wnt1 tumor bearing mice.  

     

    Brand:
    Cayman
    SKU:19930 -

    Available on backorder

  • NVP-TNKS656 is an orally bioavailable inhibitor of tankyrase 2 (TNKS2; IC50 = 6 nM).{40669} It is selective for TNKS2 over poly(ADP-ribose) polymerase (PARP) 1 and 2 (IC50s = >19 and 32 nM, respectively). NVP-TNKS656 inhibits Wnt ligand-induced signaling with an IC50 value of 3.5 nM in an HEK293 cell reporter assay. In vivo, NVP-TNKS656 (350 mg/kg) reduces Axin 2 mRNA expression, a Wnt/β-catenin target gene, in MMTV-Wnt1 tumor bearing mice.  

     

    Brand:
    Cayman
    SKU:19930 -

    Available on backorder

  • NVP-TNKS656 is an orally bioavailable inhibitor of tankyrase 2 (TNKS2; IC50 = 6 nM).{40669} It is selective for TNKS2 over poly(ADP-ribose) polymerase (PARP) 1 and 2 (IC50s = >19 and 32 nM, respectively). NVP-TNKS656 inhibits Wnt ligand-induced signaling with an IC50 value of 3.5 nM in an HEK293 cell reporter assay. In vivo, NVP-TNKS656 (350 mg/kg) reduces Axin 2 mRNA expression, a Wnt/β-catenin target gene, in MMTV-Wnt1 tumor bearing mice.  

     

    Brand:
    Cayman
    SKU:19930 -

    Available on backorder

  • NVS-CECR2-1 is a potent inhibitor of CECR2 (cat eye syndrome chromosome region, candidate 2), a component of chromatin complexes that regulate gene expression controlling development. It binds CECR2 with high affinity (IC50 = 0.047 µM by Alpha screen, Kd = 0.80 µM by ITC). NVS-CECR2-1 demonstrates no crossreactivity in a panel of 48 bromodomains and has no major activity in kinase, protease, and receptor panels. It shows robust activity in cells by FRAP assay, due to its slow off-rate, and has no acute toxicity. See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • NVS-CECR2-1 is a potent inhibitor of CECR2 (cat eye syndrome chromosome region, candidate 2), a component of chromatin complexes that regulate gene expression controlling development. It binds CECR2 with high affinity (IC50 = 0.047 µM by Alpha screen, Kd = 0.80 µM by ITC). NVS-CECR2-1 demonstrates no crossreactivity in a panel of 48 bromodomains and has no major activity in kinase, protease, and receptor panels. It shows robust activity in cells by FRAP assay, due to its slow off-rate, and has no acute toxicity. See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • NVS-CECR2-1 is a potent inhibitor of CECR2 (cat eye syndrome chromosome region, candidate 2), a component of chromatin complexes that regulate gene expression controlling development. It binds CECR2 with high affinity (IC50 = 0.047 µM by Alpha screen, Kd = 0.80 µM by ITC). NVS-CECR2-1 demonstrates no crossreactivity in a panel of 48 bromodomains and has no major activity in kinase, protease, and receptor panels. It shows robust activity in cells by FRAP assay, due to its slow off-rate, and has no acute toxicity. See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • NVS-CECR2-1 is a potent inhibitor of CECR2 (cat eye syndrome chromosome region, candidate 2), a component of chromatin complexes that regulate gene expression controlling development. It binds CECR2 with high affinity (IC50 = 0.047 µM by Alpha screen, Kd = 0.80 µM by ITC). NVS-CECR2-1 demonstrates no crossreactivity in a panel of 48 bromodomains and has no major activity in kinase, protease, and receptor panels. It shows robust activity in cells by FRAP assay, due to its slow off-rate, and has no acute toxicity. See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • NVS-PAK1-1 is an allosteric inhibitor of p21-activated kinase 1 (PAK1), a non-receptor serine/threonine kinase involved in tumorigenesis (Kd = 7 nM).{39819} It has an IC50 value of 5.2 nM in a PAK1 dephosphorylation assay. NVS-PAK1-1 is selective for PAK1 over PAK2 (Kd = 400 nM) and over a panel of 442 kinases, where it did not inhibit any other kinases by greater than 80%.{39819,39820} It inhibits phosphorylation of MEK Ser289 when used at concentrations ranging from 6 to 20 µM but does not inhibit proliferation of Su86.86 cells at concentrations lower than 2 µM.{39819} See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:19964 -

    Available on backorder

  • NVS-PAK1-1 is an allosteric inhibitor of p21-activated kinase 1 (PAK1), a non-receptor serine/threonine kinase involved in tumorigenesis (Kd = 7 nM).{39819} It has an IC50 value of 5.2 nM in a PAK1 dephosphorylation assay. NVS-PAK1-1 is selective for PAK1 over PAK2 (Kd = 400 nM) and over a panel of 442 kinases, where it did not inhibit any other kinases by greater than 80%.{39819,39820} It inhibits phosphorylation of MEK Ser289 when used at concentrations ranging from 6 to 20 µM but does not inhibit proliferation of Su86.86 cells at concentrations lower than 2 µM.{39819} See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:19964 -

    Available on backorder

  • NVS-PAK1-1 is an allosteric inhibitor of p21-activated kinase 1 (PAK1), a non-receptor serine/threonine kinase involved in tumorigenesis (Kd = 7 nM).{39819} It has an IC50 value of 5.2 nM in a PAK1 dephosphorylation assay. NVS-PAK1-1 is selective for PAK1 over PAK2 (Kd = 400 nM) and over a panel of 442 kinases, where it did not inhibit any other kinases by greater than 80%.{39819,39820} It inhibits phosphorylation of MEK Ser289 when used at concentrations ranging from 6 to 20 µM but does not inhibit proliferation of Su86.86 cells at concentrations lower than 2 µM.{39819} See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:19964 -

    Available on backorder

  • NXY-059 is a nitrone free radical spin trap with neuroprotective properties.{37428,37429,37430} It inhibits transport of tissue plasminogen activator (tPA) from the luminal to the abluminal compartment in an in vitro model of the blood-brain barrier (BBB) under ischemic conditions at a concentration of 250 μM.{37431} NXY-059 (10 mg/kg per h) decreases infarct volume by 59% in a rat model of transient ischemia induced by occlusion of the middle cerebral artery (MCA).{37429} It decreases functional disability in the hemiparetic arm of marmosets in the Hill-and-Valley staircase, two-tube choice, and six-tube search tests following MCA occlusion-induced ischemia when administered at a dose of 16 mg/kg per hour.{37430}  

     

    Brand:
    Cayman
    SKU:22109 -

    Out of stock

  • NXY-059 is a nitrone free radical spin trap with neuroprotective properties.{37428,37429,37430} It inhibits transport of tissue plasminogen activator (tPA) from the luminal to the abluminal compartment in an in vitro model of the blood-brain barrier (BBB) under ischemic conditions at a concentration of 250 μM.{37431} NXY-059 (10 mg/kg per h) decreases infarct volume by 59% in a rat model of transient ischemia induced by occlusion of the middle cerebral artery (MCA).{37429} It decreases functional disability in the hemiparetic arm of marmosets in the Hill-and-Valley staircase, two-tube choice, and six-tube search tests following MCA occlusion-induced ischemia when administered at a dose of 16 mg/kg per hour.{37430}  

     

    Brand:
    Cayman
    SKU:22109 -

    Out of stock

  • NXY-059 is a nitrone free radical spin trap with neuroprotective properties.{37428,37429,37430} It inhibits transport of tissue plasminogen activator (tPA) from the luminal to the abluminal compartment in an in vitro model of the blood-brain barrier (BBB) under ischemic conditions at a concentration of 250 μM.{37431} NXY-059 (10 mg/kg per h) decreases infarct volume by 59% in a rat model of transient ischemia induced by occlusion of the middle cerebral artery (MCA).{37429} It decreases functional disability in the hemiparetic arm of marmosets in the Hill-and-Valley staircase, two-tube choice, and six-tube search tests following MCA occlusion-induced ischemia when administered at a dose of 16 mg/kg per hour.{37430}  

     

    Brand:
    Cayman
    SKU:22109 -

    Out of stock

  • NXY-059 is a nitrone free radical spin trap with neuroprotective properties.{37428,37429,37430} It inhibits transport of tissue plasminogen activator (tPA) from the luminal to the abluminal compartment in an in vitro model of the blood-brain barrier (BBB) under ischemic conditions at a concentration of 250 μM.{37431} NXY-059 (10 mg/kg per h) decreases infarct volume by 59% in a rat model of transient ischemia induced by occlusion of the middle cerebral artery (MCA).{37429} It decreases functional disability in the hemiparetic arm of marmosets in the Hill-and-Valley staircase, two-tube choice, and six-tube search tests following MCA occlusion-induced ischemia when administered at a dose of 16 mg/kg per hour.{37430}  

     

    Brand:
    Cayman
    SKU:22109 -

    Out of stock

  • Nybomycin is a fungal metabolite originally isolated from Streptomyces sp. A717 and has antibacterial activity.{48308} It is active against B. subtilis, B. cereus, B. mycoides, M. smegmatis, and K. pneumoniae (MICs = 0.025, 2, 0.8, 0.2, and 0.003 μg/ml, respectively). Nybomycin is also active against M. tuberculosis and M. bovis (MICs = 4.5 and 1 μg/ml, respectively).{48309}  

     

    Brand:
    Cayman
    SKU:28099 - 2.5 mg

    Available on backorder

  • Nybomycin is a fungal metabolite originally isolated from Streptomyces sp. A717 and has antibacterial activity.{48308} It is active against B. subtilis, B. cereus, B. mycoides, M. smegmatis, and K. pneumoniae (MICs = 0.025, 2, 0.8, 0.2, and 0.003 μg/ml, respectively). Nybomycin is also active against M. tuberculosis and M. bovis (MICs = 4.5 and 1 μg/ml, respectively).{48309}  

     

    Brand:
    Cayman
    SKU:28099 - 500 µg

    Available on backorder

  • Nα-Boc-D-Histidine is an amino acid building block.{52500,52502,52501} It has been used in the synthesis of antimicrobial peptides, thyrotropin-releasing hormone enantiomers, and proteolysis-resistant peptide renin inhibitors.  

     

    Brand:
    Cayman
    SKU:30501 - 1 g

    Available on backorder

  • Nα-Boc-D-Histidine is an amino acid building block.{52500,52502,52501} It has been used in the synthesis of antimicrobial peptides, thyrotropin-releasing hormone enantiomers, and proteolysis-resistant peptide renin inhibitors.  

     

    Brand:
    Cayman
    SKU:30501 - 500 mg

    Available on backorder

  • Nω-Propyl-L-Arginine is a potent and selective inhibitor of neuronal nitric oxide synthase (nNOS). Nω-Propyl-L-Arginine is a competitive inhibitor of bovine nNOS having a Ki value of 57 nM.{5453} The Ki values for eNOS (bovine) and iNOS (murine) are 8.5 and 180 µM, respectively. Nω-propyl-L-Arginine therefore exhibits 3,000-fold and 150-fold selectivity for the neuronal isoform versus the inducible (murine) and endothelial (bovine) isoforms of NOS, respectively.{5453}  

     

    Brand:
    Cayman
    SKU:80587 - 10 mg

    Available on backorder

  • Nω-Propyl-L-Arginine is a potent and selective inhibitor of neuronal nitric oxide synthase (nNOS). Nω-Propyl-L-Arginine is a competitive inhibitor of bovine nNOS having a Ki value of 57 nM.{5453} The Ki values for eNOS (bovine) and iNOS (murine) are 8.5 and 180 µM, respectively. Nω-propyl-L-Arginine therefore exhibits 3,000-fold and 150-fold selectivity for the neuronal isoform versus the inducible (murine) and endothelial (bovine) isoforms of NOS, respectively.{5453}  

     

    Brand:
    Cayman
    SKU:80587 - 100 mg

    Available on backorder

  • Nω-Propyl-L-Arginine is a potent and selective inhibitor of neuronal nitric oxide synthase (nNOS). Nω-Propyl-L-Arginine is a competitive inhibitor of bovine nNOS having a Ki value of 57 nM.{5453} The Ki values for eNOS (bovine) and iNOS (murine) are 8.5 and 180 µM, respectively. Nω-propyl-L-Arginine therefore exhibits 3,000-fold and 150-fold selectivity for the neuronal isoform versus the inducible (murine) and endothelial (bovine) isoforms of NOS, respectively.{5453}  

     

    Brand:
    Cayman
    SKU:80587 - 5 mg

    Available on backorder

  • Nω-Propyl-L-Arginine is a potent and selective inhibitor of neuronal nitric oxide synthase (nNOS). Nω-Propyl-L-Arginine is a competitive inhibitor of bovine nNOS having a Ki value of 57 nM.{5453} The Ki values for eNOS (bovine) and iNOS (murine) are 8.5 and 180 µM, respectively. Nω-propyl-L-Arginine therefore exhibits 3,000-fold and 150-fold selectivity for the neuronal isoform versus the inducible (murine) and endothelial (bovine) isoforms of NOS, respectively.{5453}  

     

    Brand:
    Cayman
    SKU:80587 - 50 mg

    Available on backorder

  • O-11 is an analog of the fully saturated, 14-carbon fatty acid myristic acid, in which the methylene group at position 11 is replaced with oxygen. It is highly effective and selective at killing Trypanosoma brucei, the protozoan parasite responsible for African sleeping sickness, exhibiting an LD50 of less than 1 µM in a cell culture assay.{7752,11965} The toxic effects of O-11 appear to be caused by its ability to inhibit the incorporation of a single myristate into the GPI anchor of the variant surface glycoprotein (VSG), a protein critical for evading the host immune response.{7752} O-11 exhibits essentially no anti-fungal activity when assayed using C. neoformans, but does have a minor inhibitory effect on HIV-1 replication in T-lymphocytes.{2338}  

     

    Brand:
    Cayman
    SKU:90510 - 1 mg

    Available on backorder

  • O-11 is an analog of the fully saturated, 14-carbon fatty acid myristic acid, in which the methylene group at position 11 is replaced with oxygen. It is highly effective and selective at killing Trypanosoma brucei, the protozoan parasite responsible for African sleeping sickness, exhibiting an LD50 of less than 1 µM in a cell culture assay.{7752,11965} The toxic effects of O-11 appear to be caused by its ability to inhibit the incorporation of a single myristate into the GPI anchor of the variant surface glycoprotein (VSG), a protein critical for evading the host immune response.{7752} O-11 exhibits essentially no anti-fungal activity when assayed using C. neoformans, but does have a minor inhibitory effect on HIV-1 replication in T-lymphocytes.{2338}  

     

    Brand:
    Cayman
    SKU:90510 - 10 mg

    Available on backorder

  • O-11 is an analog of the fully saturated, 14-carbon fatty acid myristic acid, in which the methylene group at position 11 is replaced with oxygen. It is highly effective and selective at killing Trypanosoma brucei, the protozoan parasite responsible for African sleeping sickness, exhibiting an LD50 of less than 1 µM in a cell culture assay.{7752,11965} The toxic effects of O-11 appear to be caused by its ability to inhibit the incorporation of a single myristate into the GPI anchor of the variant surface glycoprotein (VSG), a protein critical for evading the host immune response.{7752} O-11 exhibits essentially no anti-fungal activity when assayed using C. neoformans, but does have a minor inhibitory effect on HIV-1 replication in T-lymphocytes.{2338}  

     

    Brand:
    Cayman
    SKU:90510 - 5 mg

    Available on backorder

  • O-1602 is an agonist of GPR55 (EC50 = 13 nM in a GTPγS binding assay) and a derivative of the GPR55 agonist abnormal cannabidiol (Item No. 10004259).{17583} It is selective for GPR55 over cannabinoid (CB) receptor 1 (CB1) and CB2 (EC50s = >30 µM for both in GTPγS binding assays). O-1602 (50 µM) reduces growth of Mz-ChA-1, HuCCT-1, CC-LP-1, and SG231 cholangiocarcinoma cells and reduces tumor growth in a Mz-ChA-1 mouse xenograft model when administered at a dose of 10 mg/kg per day.{38346} O-1602 increases calcium mobilization and lipogenesis in 3T3-L1 adipocytes in a concentration-dependent manner and increases food intake and fat mass in rats; however, this effect was also observed in mice lacking GPR55.{38347} O-1602 reduces movement-induced firing of nociceptive C fibers in a rat model of inflammatory joint pain.{38344} It also decreases IL-6 and TNF-α levels and myeloperoxidase activities in the plasma, lungs, and pancreas in a mouse model of acute pancreatitis.{38345}  

     

    Brand:
    Cayman
    SKU:10006803 - 1 mg

    Available on backorder

  • O-1602 is an agonist of GPR55 (EC50 = 13 nM in a GTPγS binding assay) and a derivative of the GPR55 agonist abnormal cannabidiol (Item No. 10004259).{17583} It is selective for GPR55 over cannabinoid (CB) receptor 1 (CB1) and CB2 (EC50s = >30 µM for both in GTPγS binding assays). O-1602 (50 µM) reduces growth of Mz-ChA-1, HuCCT-1, CC-LP-1, and SG231 cholangiocarcinoma cells and reduces tumor growth in a Mz-ChA-1 mouse xenograft model when administered at a dose of 10 mg/kg per day.{38346} O-1602 increases calcium mobilization and lipogenesis in 3T3-L1 adipocytes in a concentration-dependent manner and increases food intake and fat mass in rats; however, this effect was also observed in mice lacking GPR55.{38347} O-1602 reduces movement-induced firing of nociceptive C fibers in a rat model of inflammatory joint pain.{38344} It also decreases IL-6 and TNF-α levels and myeloperoxidase activities in the plasma, lungs, and pancreas in a mouse model of acute pancreatitis.{38345}  

     

    Brand:
    Cayman
    SKU:10006803 - 10 mg

    Available on backorder

  • O-1602 is an agonist of GPR55 (EC50 = 13 nM in a GTPγS binding assay) and a derivative of the GPR55 agonist abnormal cannabidiol (Item No. 10004259).{17583} It is selective for GPR55 over cannabinoid (CB) receptor 1 (CB1) and CB2 (EC50s = >30 µM for both in GTPγS binding assays). O-1602 (50 µM) reduces growth of Mz-ChA-1, HuCCT-1, CC-LP-1, and SG231 cholangiocarcinoma cells and reduces tumor growth in a Mz-ChA-1 mouse xenograft model when administered at a dose of 10 mg/kg per day.{38346} O-1602 increases calcium mobilization and lipogenesis in 3T3-L1 adipocytes in a concentration-dependent manner and increases food intake and fat mass in rats; however, this effect was also observed in mice lacking GPR55.{38347} O-1602 reduces movement-induced firing of nociceptive C fibers in a rat model of inflammatory joint pain.{38344} It also decreases IL-6 and TNF-α levels and myeloperoxidase activities in the plasma, lungs, and pancreas in a mouse model of acute pancreatitis.{38345}  

     

    Brand:
    Cayman
    SKU:10006803 - 25 mg

    Available on backorder

  • O-1602 is an agonist of GPR55 (EC50 = 13 nM in a GTPγS binding assay) and a derivative of the GPR55 agonist abnormal cannabidiol (Item No. 10004259).{17583} It is selective for GPR55 over cannabinoid (CB) receptor 1 (CB1) and CB2 (EC50s = >30 µM for both in GTPγS binding assays). O-1602 (50 µM) reduces growth of Mz-ChA-1, HuCCT-1, CC-LP-1, and SG231 cholangiocarcinoma cells and reduces tumor growth in a Mz-ChA-1 mouse xenograft model when administered at a dose of 10 mg/kg per day.{38346} O-1602 increases calcium mobilization and lipogenesis in 3T3-L1 adipocytes in a concentration-dependent manner and increases food intake and fat mass in rats; however, this effect was also observed in mice lacking GPR55.{38347} O-1602 reduces movement-induced firing of nociceptive C fibers in a rat model of inflammatory joint pain.{38344} It also decreases IL-6 and TNF-α levels and myeloperoxidase activities in the plasma, lungs, and pancreas in a mouse model of acute pancreatitis.{38345}  

     

    Brand:
    Cayman
    SKU:10006803 - 5 mg

    Available on backorder

  • Abnormal cannabidiol is a synthetic regioisomer of cannabidiol that fails to elicit either central cannabinoid (CB1) or peripheral cannabinoid (CB2) receptors responsiveness and is without psychotropic activity. It induces endothelium-dependent vasodilation via a CB1/CB2/nitric oxide-independent mechanism.{11092} O-1821 is a cannabidiol analog with close structural similarity to O-1918 which is a selective antagonist of abnormal cannabidiol at the non-central cannabinoid (CB1)/peripheral cannabinoid (CB2) receptors endothelial receptor.{11761} O-1918 does not bind to CB1 or CB2 receptors at concentrations up to 30 µM and inhibits the vasorelaxant effects of abnormal cannabidiol in vitro and in whole animals.{11761} The biological activity of O-1821 has not been reported.  

     

    Brand:
    Cayman
    SKU:10006804 - 1 mg

    Available on backorder