CC0651 是一种人Cdc34泛素结合酶变构抑制剂。CC0651 有效抑制 p27^Kip1的泛素化，IC₅₀ 为 1.72 μM。

CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. CC0651 potently (IC 50 =1.72 μM) inhibits the ubiquitination of p27, as confirmed by dose-response analysis.

Solid

IC50: 1.72 μM (p27 ubiquitination)

CC0651 strongly impairs the rate of ubiquitin chain initiation on substrate by SCF, as measured by the monoubiquitination of Sic1 by K0 ubiquitin. CC0651 actually potentiates the formation of both ubiquitin dimers and monoubiquitinated hCdc34, concordant with the observed accumulation of the hCdc34 conjugate in cells treated with the ester derivative of CC0651. CC0651 completely inhibits the assembly of polyubiquitin chains and decreased formation of free triubiquitin and, to a lesser extent, hCdc34 monoubiquitin, but has no effect on production of diubiquitin. CC0651 is an inhibitor of the E2 ubiquitin conjugating enzyme Cdc34A, acts by trapping a weak interaction between ubiquitin and the E2 donor ubiquitin binding site. A quantitative SCF ubiquitination assay with a β-Catenin substrate peptide yields a value of IC50 of 18±1 μM for CC0651 inhibition, similar to th

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[1]. Ceccarelli DF, et al. An allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. Cell. 2011 Jun 24;145(7):1075-87.
[2]. Huang H, et al. E2 enzyme inhibition by stabilization of a low-affinity interface with ubiquitin. Nat Chem Biol. 2014 Feb;10(2):156-63.

In Vitro: DMSO : ≥ 56 mg/mL (126.61 mM)配制储备液