Identification | Back Directory | [Name]
UbcH5c-IN-6d | [CAS]
2123480-72-6 | [Synonyms]
UbcH5c-IN-1 UbcH5c-IN-6d Naphtho[1,2-b]furan-2(3H)-one, 8-[(2-bromophenyl)methoxy]-3a,4,5,9b-tetrahydro-6,9-dimethyl-3-methylene-, (3aS,9bR)- | [Molecular Formula]
C22H21BrO3 | [MDL Number]
MFCD31813615 | [MOL File]
2123480-72-6.mol | [Molecular Weight]
413.3 |
Chemical Properties | Back Directory | [Boiling point ]
559.8±50.0 °C(Predicted) | [density ]
1.41±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [color ]
White to off-white |
Hazard Information | Back Directory | [Uses]
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]. | [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. |
| [storage]
Store at -20°C | [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. DOI:10.1021/acs.jmedchem.6b01829 |
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MedChemExpress
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021-58955995 |
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www.medchemexpress.com |
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