COH000

COH000 is an inhibitor of SUMO-activating enzyme (SAE, IC50 = 0.2 µM), a heterodimer composed of SAE1 and SAE2. 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.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. CAS Number: 1534358-79-6. Molecular Formula: C25H25NO5. Formula Weight: 419.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 11 mg/mL, DMSO: 13 mg/mL, Ethanol: Slightly Soluble, PBS (pH 7.2): 0.04 mg/mL. lambdamax: 244 nm. SMILES: CC(C=C1)=CC=C1C[C@H]([C@@]23C(C(OC)=O)=C([C@H](C=C3)O2)C(OC)=O)NC4=CC=CC=C4. InChi Code: InChI=1S/C25H25NO5/c1-16-9-11-17(12-10-16)15-20(26-18-7-5-4-6-8-18)25-14-13-19(31-25)21(23(27)29-2)22(25)24(28)30-3/h4-14,19-20,26H,15H2,1-3H3/t19-,20+,25-/m0/s1. InChi Key: UFPINDDCTUCUSA-DFIYOIEZSA-N.