Bioactivity | USP28-IN-4 is a USP28 inhibitor (IC50=0.04 μM) with high selectivity over USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-4 shows cytotoxicity against cancer cells, down-regulates the cellular level of c-Myc through ubiquitin-proteasome system. USP28-IN-4 also decreases the ankyrase-1/2 level in vitro. USP28-IN-4 enhance the sensitivity of colorectal cancer cells to Regorafenib (HY-10331)[1]. |
Invitro | USP28-IN-4 (compound 9p) (12.5 μM,15 μM;3 d) 抑制人结直肠癌细胞 HCT116 (15 μM) 和 Ls174T (12.5 μM) 的集落形成[1]。USP28-IN-4 (20-80 μM;24 小时) 通过泛素-蛋白酶体系统 (UPS) 增强其降解,从而下调 c-Myc 的水平[1]。 Western Blot Analysis[1] Cell Line: |
Name | USP28-IN-4 |
Formula | C22H18Cl2N2O3S |
Molar Mass | 461.36 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Zhou D, et al. Structure-based discovery of potent USP28 inhibitors derived from Vismodegib. Eur J Med Chem. 2023 Jun 5;254:115369. |