A dual modulator of p53-MDM2 interaction and NF-κB signaling; binds MDM2 (Ki = 250 nM)

CAY10681 – 25 mg

Brand:
Cayman
CAS:
1542066-69-2
Storage:
-20
UN-No:
Non-Hazardous - /

Inactivation of the tumor suppressor p53 commonly coincides with increased signaling through NF-κB in cancer. CAY10681 is a dual modulator of p53-MDM2 interaction and NF-κB signaling.{25314} It potently binds MDM2 (Ki = 250 nM), reducing MDM2-mediated turnover of p53.{25314} CAY10681 also inhibits phosphorylation of IκBα and dose-dependently reduces nuclear accumulation of p65.{25314} It blocks the proliferation of cancer cell lines (IC50s range from 33 to 37 µM).{25314} CAY10681 exhibits excellent oral bioavailability and inhibits tumor growth in A549 xenografts in nude mice.{25314}  

 

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Description

A dual modulator of p53-MDM2 interaction and NF-κB signaling; binds MDM2 (Ki = 250 nM), reducing MDM2-mediated turnover of p53; inhibits phosphorylation of IκBα and dose-dependently reduces nuclear accumulation of p65; inhibits cancer cell growth in vitro and in vivo

Formal name: 4-(4-bromophenyl)-4,5-dihydro-5-[3-(1H-imidazol-1-yl)propyl]-3-phenyl-1-(phenylmethyl)-pyrrolo[3,4-c]pyrazol-6(1H)-one

Synonyms: 

Molecular weight: 552.5

CAS: 1542066-69-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|TNF-α/NF-κB Signaling||Product Type|Biochemicals|Small Molecule Inhibitors|Ubiquitin Ligase System||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||Research Area|Immunology & Inflammation

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