DUBs-IN-1 是一种泛素特异性蛋白酶 (USP) 的活性抑制剂,对于 USP8 的 IC50 为 0.85 μM。
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DUBs-IN-1 is an active inhibitor of ubiquitin-specific proteases (USPs), with an IC50 of 0.24 μM for USP8. IC50: 0.24 μM (USP8)[1]
DUBs-IN-1 (22 f) is an active inhibitor of ubiquitin-specific proteases, with an IC50 of 0.24 μM for USP8. DUBs-IN-1 is inactive toward USP7 (IC50, >100 μM). DUBs-IN-1 and its analogs reduce the viability of HCT116 colon and PC-3 prostate cancer cell lines with IC50s ranging from 0.5 μM to 1.5 μM[1].
[1]. Colombo M, et al. Synthesis and biological evaluation of 9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile analogues as potential inhibitors of deubiquitinating enzymes. ChemMedChem. 2010 Apr 6;5(4):552-8.
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