COH000 is an inhibitor of SUMO-activating enzyme (SAE; IC50 = 0.2 ?M), a heterodimer composed of SAE1 and SAE2.1 It is selective for SAE over ubiquitin-activating enzyme (UAE) and NEDD8-activating enzyme (NAE) at 10 ?M. COH000 induces degradation of SAE2 in HCT116 human colon cancer cells. COH000 (10 mg/kg) induces intratumoral apoptosis, decreases intratumoral c-Myc expression, and reduces tumor growth in an HCT116 mouse xenograft model.
1.Li, Y.-J., Du, L., Wang, J., et al.Allosteric inhibition of ubiquitin-like modifications by a class of inhibitor of SUMO-activating enzymeCell Chem. Biol.26(2)278-288(2019)
















