COH000是共价的、不可逆的泛素样激活酶1的变构抑制剂，体外测得对SUMO化修饰的IC50值为0.2μM。
货号:ajcx12868
CAS:1534358-79-6
分子式:C25H25NO5
分子量：419.47
溶解度:DMSO : 35.71 mg/mL (85.13 mM);H2O :< 0.1 mg/mL (insoluble)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

COH000 is an allosteric, covalent and irreversible inhibitor of Ubiquitin-like 1-activating enzyme (SUMO-activating enzyme), with an IC50 of 0.2 μM for SUMOylation in vitro[1].

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[1].

[1]. Li YJ, et al. Allosteric Inhibition of Ubiquitin-like Modifications by a Class of Inhibitor of SUMO-Activating Enzyme. Cell Chem Biol. 2018 Dec 5. pii: S2451-9456(18)30386-6.