HBX 41108

HBX 41108 is an uncompetitive, reversible inhibitor of ubiquitin-specific protease 7 (USP7) activity (IC50 = 424 nM). 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.Formal Name: 7-chloro-9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile. CAS Number: 924296-39-9. Molecular Formula: C13H3ClN4O. Formula Weight: 266.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 33 mg/ml, DMSO:PBS (pH 7.2) (1:40): 0.2 mg/ml. lambdamax: 312 nm. SMILES: O=C1C2=NC(C#N)=C(C#N)N=C2C3=C1C=C(Cl)C=C3. InChi Code: InChI=1S/C13H3ClN4O/c14-6-1-2-7-8(3-6)13(19)12-11(7)17-9(4-15)10(5-16)18-12/h1-3H. InChi Key: BIGPXXAUSQLTQR-UHFFFAOYSA-N.