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-SCFCdc4 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 p27Kip1 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.
