CAY10682 - CAS 1542066-74-9

(±) -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-κB pathway. It specifically prevents phosphorylation of IκBα by the kinases IKKα, IKKβ, 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.

NF-κB, MDM-2/p53, Others

NF-κB, Others, Apoptosis

1541983

C30H25BrFN5O

570.45

C(CCN1C=CN=C1)N2C(C3=C(N(CC4=CC=C(F)C=C4)N=C3C5=CC=CC=C5)C2=O)C6=CC=C(Br)C=C6

-20°C

Ice Packs

Small Compound