CC0651

CC0651 is an allosteric inhibitor of the human cdc34 ubiquitin-conjugating enzyme that potently (IC50 = 1.72 uM) inhibited the ubiquitination of p27 Kip1.

CC0651 that potently (IC50 = 1.72 uM) inhibited the ubiquitination of p27 Kip1, as confrmed by dose-response analysis. CC0651 corresponds to (2R,3S,4S)-5-(3,5-dichlorobiphenyl-4-yl)-2,3-dihydroxy-4-(2-methoxyacetamido) pentanoic acid and has a molecular mass of 442.3 g/mol.The calculated Log P and Log D values for CC0651 were 2.46 and 0.985, with an aqueous solubility of 1 mg/ml at pH 7.4. CC0651 had no effect on ubiquitination of
the yeast CDK inhibitor Sic1 in the yeast Cdc34-SCF Cdc4 reaction. However, substitution of yeast Cdc34 with hCdc34 in this reaction caused CC0651 to robustly inhibit Sic1 ubiquitination.