CAY10682

CAY10682

CAT N°: 15574
Price:

From 176.00 149.60

(±)-Nutlin-3 (Item No. 10004372) blocks the interaction of p53 with its negative regulator Mdm2 (IC50 = 90 nM), inducing the expression of p53-regulated genes and blocking the growth of tumor xenografts in vivo.{11628} CAY10682 is a pyrrolo[3,4c]pyrazole derivative that inhibits the p53-Mdm2 interaction as potently as (±)-nutlin-3 (Ki = 83 nM) and also dose-dependently reduces activation of the NF-?B pathway.{25314} It specifically prevents phosphorylation of I?B? by the kinases IKK?, IKK?, and IKK? (IC50s = 80.5, 78.2, and 57.1 µM, respectively).{25314} CAY10682 blocks the growth of cancer cells in vitro (IC50s = 2-6 µM) and inhibits the growth of A549 cell xenografts in mice without significantly reducing body weight.{25314}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 4-(4-bromophenyl)-1-[(4-fluorophenyl)methyl]-4,5-dihydro-5-[3-(1H-imidazol-1-yl)propyl]-3-phenyl-pyrrolo[3,4-c]pyrazol-6(1H)-one
  • Correlated keywords
    • biochemicals cancer intracellular signaling dual interaction inhibitors inhibit gene regulation NF-?B NF?B pathyway p53-Mdm2 p53Mdm2 interaction pyrrolo[3,4c]pyrazole derivative (+)-nutlin-3 phosphorylation of I?B? kinase IKK? IKK? IKK? A549 cell xenograft CAY 10682
  • Product Overview:
    (±)-Nutlin-3 (Item No. 10004372) blocks the interaction of p53 with its negative regulator Mdm2 (IC50 = 90 nM), inducing the expression of p53-regulated genes and blocking the growth of tumor xenografts in vivo.{11628} CAY10682 is a pyrrolo[3,4c]pyrazole derivative that inhibits the p53-Mdm2 interaction as potently as (±)-nutlin-3 (Ki = 83 nM) and also dose-dependently reduces activation of the NF-?B pathway.{25314} It specifically prevents phosphorylation of I?B? by the kinases IKK?, IKK?, and IKK? (IC50s = 80.5, 78.2, and 57.1 µM, respectively).{25314} CAY10682 blocks the growth of cancer cells in vitro (IC50s = 2-6 µM) and inhibits the growth of A549 cell xenografts in mice without significantly reducing body weight.{25314}

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