COH000

Research use only, not for human use.

COH000 (COH-000) is a highly selective, first-in-class, irreversible, allosteric, covalent inhibitor of SUMO-Activating Enzyme E1.

COH000 (COH-000) is a highly selective, first-in-class, irreversible, allosteric, covalent inhibitor of SUMO-Activating Enzyme E1, inhibits SUMOylation in vitro with IC50 of 0.2 uM, displays >500-fold selectivity for SUMOylation over ubiquitylation; increased the degradation of SAE2, increases the expression of miR-34b and reduces c-Myc levels in lymphoma and colorectal cancer cell lines and a colorectal cancer xenograft mouse model.(In Vitro):COH000 has over 500-fold selectivity for SUMOylation than ubiquitylation. COH000 inhibits SUMO adenylation without directly competing with ATP or SUMO1 binding. COH000 has an extremely slow off-rate and is consistent with it being covalently bound to the enzyme.

COH000 has over 500-fold selectivity for SUMOylation than ubiquitylation. COH000 inhibits SUMO adenylation without directly competing with ATP or SUMO1 binding. COH000 has an extremely slow off-rate and is consistent with it being covalently bound to the enzyme.

——

COH-000 | COH 000 | CID 46835111 | SID 99212997

Proteasome/Ubiquitin

E1

SUMO-activatingenzyme

——

——

1534358-79-6

419.477

C25H25NO5

>98% (HPLC)

DMSO: Soluble （ < 1 mg/ml refers to the product slightly soluble or insoluble )

O=C(C1=C(C(OC)=O)C2C=CC1([C@H](NC3=CC=CC=C3)CC4=CC=C(C)C=C4)O2)OC

dimethyl 1-((R)-1-(phenylamino)-2-(p-tolyl)ethyl)-7-oxabicyclo[2.2.1]hepta-2,5-diene-2,3-dicarboxylate

(-20℃)

With Ice Pack

≥ 2 years