HBX 41108

HBX 41108 is an uncompetitive, reversible inhibitor of ubiquitin-specific protease 7 (USP7) activity (IC₅₀ = 424 nM).¹ 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.

WARNING This product is not for human or veterinary use.

1. Colland, F., Formstecher, E., Jacq, X., et al. Small-molecule inhibitor of USP7/HAUSP ubiquitin protease stabilizes and activates p53 in cells. Mol. Cancer Ther. 8(8), 2286-2295 (2009).