USP28-IN-2 is a selective USP28 inhibitor (IC50 = 0.3 μM), demonstrating high specificity compared to USP2, USP7, USP8, USP9x, UCHL3, and UCHL5. This compound exhibits cytotoxic effects on cancer cells and induces the degradation of c-Myc via the ubiquitin-proteasome pathway. Additionally, USP28-IN-2 reduces ankyrin-1/2 levels in vitro and potentiates the responsiveness of colorectal cancer cells to Regorafenib [1].

USP28:0.3 μM

USP28-IN-2（化合物9l）以15 μM和17.5 μM的浓度并作用3天，有效抑制了人类结直肠癌细胞株HCT116（17.5 μM）和Ls174T（15 μM）的集落形成[1]。此外，USP28-IN-2在20-80 μM浓度下，持续作用24小时，能够通过泛素-蛋白酶体系统（UPS）促进蛋白质的降解，进而降低c-Myc水平[1]。