PeptideDB

UbcH5c-IN-1

CAS: 2123480-72-6 F: C22H21BrO3 W: 413.30

UbcH5c-IN-1 (compound 6d) is a potent and selective small-molecule inhibitor of Ubiquitin-conjugating enzyme UbcH5c, wit
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Bioactivity 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].
Target Kd: 283 nM (E2 UbcH5c).
In Vivo 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:
Name UbcH5c-IN-1
CAS 2123480-72-6
Formula C22H21BrO3
Molar Mass 413.30
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]. 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.