USP28-IN-3 is a USP28 inhibitor (IC50=0.1 μM) with high selectivity over USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-3 shows cytotoxicity against cancer cells, down-regulates the cellular level of c-Myc through ubiquitin-proteasome system. USP28-IN-3 also decreases the ankyrase-1/2 level in vitro. USP28-IN-3 enhance the sensitivity of colorectal cancer cells to Regorafenib (HY-10331)[1].
IC 50
USP28: 0.1 μM (IC50)
References
[1] Zhou D, et al. Structure-based discovery of potent USP28 inhibitors derived from Vismodegib. Eur J Med Chem. 2023 Jun 5;254:115369. DOI:10.1016/j.ejmech.2023.115369
