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编 号:F757016
分子式:C23H20Cl2N2O3S
分子量:475.39
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生物活性:
USP28-IN-2 is a USP28 inhibitor (IC50=0.3 μM) with high selectivity over USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-2 shows cytotoxicity against cancer cells, down-regulates the cellular level of c-Myc through ubiquitin-proteasome system. USP28-IN-2 also decreases the ankyrase-1/2 level in vitro. USP28-IN-2 enhance the sensitivity of colorectal cancer cells to Regorafenib (HY-10331).

体外研究:
USP28-IN-2 (compound 9l) (15 μM,17.5 μM;3 d) 抑制人结直肠癌细胞 HCT116 (17.5 μM) 和 Ls174T (15 μM) 的集落形成。USP28-IN-2 (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。
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