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CAY10682

CAT: 0931-T36192-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0931-T36192-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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CAS Number
1542066-74-9
Target
NF-κB, MDM-2/p53, Others
Related Pathways
NF-κB, Others, Apoptosis
Bioactivity
(±) -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.
Smiles
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
Molecular Formula
C30H25BrFN5O
Molecular Weight
570.45
Shipping Conditions
Ice Packs
Storage Temperature
-20°C

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