UbcH5c-IN-1(compound6d)是一种有效的、选择性的小分子泛素结合酶UbcH5c抑制剂，其与E2UbcH5c-IN-1活性位点Cys85共价结合的Kd值为283nM，是开发新型类风湿性关节炎药物的先导化合物。
UbcH5c-IN-1 (compound 6d) is a potent and selective small-molecule inhibitor of Ubiquitin-conjugating enzyme UbcH5c, with a Kd of 283 nM for E2 UbcH5c-IN-1 by covalent binding with Cys85. A promising lead compound for the development of new antirheumatoid arthritis (RA) agent[1].
UbcH5c-IN-1 (compound 6d) (5 and 20 mg/kg, p.o., daily, 10-20 days) treatment in Freund's adjuvant (CFA)-induced adjuvant arthritis (AA) rat model results in appreciable decreases in the arthritis index score and hind paw swelling rate compared with those of the vehicle-treated AA model control group[1].|| Animal Model:|Freund's adjuvant (CFA)-induced adjuvant arthritis (AA) rat model[1].|Dosage:|5 and 20 mg/kg|Administration:|Oral administration daily between day 10-20 postimmunization.|Result:|Resulted in appreciable decreases in the arthritis index score and hind paw swelling rate compared with those of the vehicle-treated AA model control group.
[1]. Chen H, et al. Discovery of Potent Small-Molecule Inhibitors of Ubiquitin-Conjugating Enzyme UbcH5c from α-Santonin Derivatives. J Med Chem. 2017 Aug 24;60(16):6828-6852.
动态评分
0.0