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. |