Inhibits the p53-Mdm2 interaction (Ki = 83 nM) and also dose-dependently reduces activation of the NF-κB pathway; prevents phosphorylation of IκBα by IKKα

CAY10682 – 1 mg

Brand:
Cayman
CAS:
1542066-74-9
Storage:
-20
UN-No:
Non-Hazardous - /

(±)-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-κB pathway.{25314} It specifically prevents phosphorylation of IκBα by the kinases IKKα, IKKβ, and IKKɛ (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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Description

Inhibits the p53-Mdm2 interaction (Ki = 83 nM) and also dose-dependently reduces activation of the NF-κB pathway; prevents phosphorylation of IκBα by IKKα, IKKβ, and IKKɛ (IC50s = 80.5, 78.2, and 57.1 µM, respectively); inhibits the growth of A549 cell xenografts in mice

Formal name: 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

Synonyms: 

Molecular weight: 570.5

CAS: 1542066-74-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|TNF-α/NF-κB Signaling||Research Area|Cancer|Cell Signaling|NF-κB Signaling||Research Area|Cancer|Cell Signaling|p53 Signaling||Research Area|Cancer|Transcription Factors|NF-κB||Research Area|Cancer|Transcription Factors|p53||Research Area|Cell Biology|Cell Signaling|NF-κB Signaling||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors

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