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CC0651

Catalog No. T14896   CAS 1319207-44-7

CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. CC0651 potently inhibits the ubiquitination of p27Kip1 (IC50: 1.72 μM).

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CC0651 Chemical Structure
CC0651, CAS 1319207-44-7
Pack Size Availability Price/USD Quantity
25 mg 8-10 weeks $ 1,820.00
50 mg 8-10 weeks $ 2,380.00
100 mg 8-10 weeks $ 3,100.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. CC0651 potently inhibits the ubiquitination of p27Kip1 (IC50: 1.72 μM).
Targets&IC50 p27Kip1 ubiquitination:1.72 μM
In vitro CC0651 acts by trapping a weak interaction between ubiquitin and the E2 donor ubiquitin-binding site. 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 the production of diubiquitin [1]. CC0651 strongly impairs the rate of ubiquitin chain initiation on the substrate by SCFCdc4, 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. 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 the effective concentrations observed in the NMR and TR-FRET assays [2].
Molecular Weight 442.29
Formula C20H21Cl2NO6
CAS No. 1319207-44-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 56 mg/mL (126.61 mM)

TargetMolReferences and Literature

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.

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Keywords

CC0651 1319207-44-7 Others CC-0651 CC 0651 inhibitor inhibit

 

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