Description
An inhibitor of SUMO-activating enzyme (IC50s = 0.003 and 0.011 µM with SUMO1 or SUMO2, respectively, as the ubiquitin-like proteins); selective for SAE over NAE and UAE (IC50s = 32 and >100 µM, respectively); decreases global SUMOylation in HCT116 cells (EC50 = 0.019 µM), as well as decreases the viability of MDA-MB-468 and A375 cells (EC50s = 0.06 and 0.45 µM, respectively); reduces tumor growth in an HCT116 mouse xenograft model at 150 and 200 mg/kg twice per day