HBX41108, USP7 Inhibitor

HBX41108 is a potent and selective ubiquitin-specific protease 7 (USP7) inhibitor with IC50 ~424 nM. Kinetics data indicate it is an uncompetitive reversible inhibition mechanism. It inhibits USP7-mediated p53 deubiquitination (IC50 ~0.8 μM). It can also stabilize p53 and activate the transcription of a p53 target gene without inducing genotoxic stress. HBX41108 inhibits cancer cell growth, and induces p53-dependent apoptosis in p53 wild type and null isogenic cancer cell lines.

Product information

CAS Number: 924296-39-9

Molecular Weight: 266.64

Formula: C13H3ClN4O

Chemical Name: HBX41108, USP7 Inhibitor

Smiles: N#CC1=NC2=C(N=C1C#N)C(=O)C1=CC(Cl)=CC=C12

InChiKey: BIGPXXAUSQLTQR-UHFFFAOYSA-N

InChi: 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

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

HBX41108 was used at 10 µM final concentration in various in vitro assays.

References:

1. Colland F, et al. Small-molecule inhibitor of USP7/HAUSP ubiquitin protease stabilizes and activates p53 in cells. (2009) Mol Cancer Ther. 8(8):2286-95.
2. Colombo M, et al. Synthesis and biological evaluation of 9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile analogues as potential inhibitors of deubiquitinating enzymes. (2010) ChemMedChem. 5(4):552-8.

Products are for research use only. Not for human use.

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