CC0651 Chemical Properties

Boiling point:

755.7±60.0 °C(Predicted)

Density 

1.410±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO: ≥ 56 mg/mL (126.61 mM)

pka

3.37±0.34(Predicted)

form 

Powder

color 

White to off-white

CC0651 Usage And Synthesis

Uses

CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. CC0651 potently (IC50=1.72 μM) inhibits the ubiquitination of p27Kip1, as confirmed by dose-response analysis.

General Description

A cell-permeable biphenylylpentanoic acid compound that acts as a selective allosteric inhibitor of E2 ubiquitin-conjugating enzyme Cdc34 (IC₅₀ = 2.5 μM in a Sic1-SCF^Cdc4 assay) without affecting the activities of E1 or E3 ligases. Reported to act by trapping a weak interaction between ubiquitin and the E2 donor ubiquitin-binding site and may serve as a molecular bridge between Cdc34A and ubiquitin. Binds to Cdc34ACAT alone with an EC₅₀ value of 267 μM, but in the presence of ubiquitin, this affinity is significantly increased (EC₅₀ = 19 μM). Does not disrupt the interaction of Cdc34A with the RING domain of Rbx1 and is suggested to even moderately stabilize this interaction. Shown to inhibit p27^Kip1 ubiquitination (IC₅₀ = 1.72 μM) and reduce PC-3 cancer cells proliferation (~30 μM).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/physiol Actions

Cell permeable: yes

References

[1] Ceccarelli DF, et al. An allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. Cell. 2011 Jun 24;145(7):1075-87. DOI:10.1016/j.cell.2011.05.039
[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. DOI:10.1038/nchembio.1412

CC0651(1319207-44-7)Related Product Information

• CHLOROETHANE
• TDZD-8
• 4SC-202
• CEP-32496
• N2-[2-Methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-1,3,5-triazine-2,4-diamine
• PURVALANOL A
• Testolactone
• GDC-0077
• AGI6780
• 6-Amino-8-[(6-iodo-1,3-benzodioxol-5-yl)thio]-N-(1-methylethyl)-9H-purine-9-propanamine
• IDO-IN-7
• UNC 0631
• XL 228
• N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea