General Description
A cell-permeable biphenylylpentanoic acid compound that acts as a selective allosteric inhibitor of E2 ubiquitin-conjugating enzyme Cdc34 (IC
50 = 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 EC
50 value of 267 μM, but in the presence of ubiquitin, this affinity is significantly increased (EC
50 = 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 (IC
50 = 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.
