Formulation: A solid
Formal Name: (1R,4S)-1-[(1R)-2-(4-methylphenyl)-1-(phenylamino)ethyl]-7-oxabicyclo[2.2.1]hepta-2,5-diene-2,3-dicarboxylic acid, 2,3-dimethyl ester
Purity: ≥98%
Formula Markup: C25H25NO5
Formula Weight: 419,5
Shelf life (days): 1460
CAS Number: 1534358-79-6
Notes: COH000 is an inhibitor of SUMO-activating enzyme (SAE; IC50 = 0.2 µM), a heterodimer composed of SAE1 and SAE2.{58874} It is selective for SAE over ubiquitin-activating enzyme (UAE) and NEDD8-activating enzyme (NAE) at 10 µM. 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.