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2123480-72-6

2123480-72-6 structure
2123480-72-6 structure
  • Name: UbcH5c-IN-1
  • Chemical Name: UbcH5c-IN-1
  • CAS Number: 2123480-72-6
  • Molecular Formula: C22H21BrO3
  • Molecular Weight: 413.30
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease E1/E2/E3 Enzyme
  • Create Date: 2019-03-30 18:54:34
  • Modify Date: 2024-01-08 18:44:35
  • 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].

Name UbcH5c-IN-1
Description 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].
Related Catalog
Target

Kd: 283 nM (E2 UbcH5c)[1].

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: 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.
References

[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.

Molecular Formula C22H21BrO3
Molecular Weight 413.30
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