()-Nutlin-3 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. 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-kappaB pathway. It specifically prevents phosphorylation of IkappaBalpha by the kinases IKKalpha, IKKbeta, and IKK (IC50s = 80.5, 78.2, and 57.1 µM, respectively). 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.
Molekulargewicht:
570.45
CAS Nummer:
[1542066-74-9]
Formel:
C30H25BrFN5O
Target-Kategorie:
Others|||MDM-2/p53|||NF-kappaB
T36192
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