An inhibitor of USP7 (IC50 = 424 nM); dose-dependently inhibits USP7-mediated p53 deubiquitination in a cell-free assay (IC50 = ~0.8 µM) and in vitro; selective for USP7 over a panel of proteases including aspartic

HBX 41108 – 1 mg

Brand:
Cayman
CAS:
924296-39-9
Storage:
-20
UN-No:
Non-Hazardous - /

HBX 41108 is an uncompetitive, reversible inhibitor of ubiquitin-specific protease 7 (USP7) activity (IC50 = 424 nM).{41377} It dose-dependently inhibits USP7-mediated p53 deubiquitination in a cell-free assay, with an IC50 value of approximately 0.8 µM, as well as in HEK293 cells. It is selective for USP7 over a panel of proteases including aspartic, serine, and metalloproteases (IC50s = >10 µM), several cysteine proteases (IC50s = >1 and >10 µM), and the deubiquitinating enzymes UCH-L1 (IC50 = >1 µM) and SENP1 (IC50 = >10 µM). HBX 41108 increases the levels of p53 and p21/WAF1, a p53 target gene. It also dose-dependently inhibits proliferation of HCT116 cells with an IC50 value of approximately 1 µM and induces apoptosis.  

 

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Description

An inhibitor of USP7 (IC50 = 424 nM); dose-dependently inhibits USP7-mediated p53 deubiquitination in a cell-free assay (IC50 = ~0.8 µM) and in vitro; selective for USP7 over a panel of proteases including aspartic, serine, and metalloproteases (IC50s = >10 µM), several cysteine proteases (IC50s = >1 and >10 µM), and the deubiquitinating enzymes UCH-L1 (IC50 = >1 µM) and SENP1 (IC50 = >10 µM; increases p53 levels; inhibits proliferation of HCT116 cells (IC50 = ~1 µM); induces apoptosis in HCT116 cells

Formal name: 7-chloro-9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile

Synonyms: 

Molecular weight: 266.6

CAS: 924296-39-9

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|p53 Signaling||Research Area|Cancer|Transcription Factors|p53||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System

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