UbcH5c-IN-1 |
| カタログ番号GC33885 |
UbcH5c-IN-1 (化合物 6d) は、Cys85 との共有結合による E2 UbcH5c-IN-1 の Kd が 283 nM である、ユビキチン結合酵素 UbcH5c の強力かつ選択的な低分子阻害剤です。
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Cas No.: 2123480-72-6
Sample solution is provided at 25 µL, 10mM.
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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.
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