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CAS No.: 1534358-79-6

COH000 is an irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) with IC50 of 0.2 μM for SUMOylation in vitro.

规格	价格	促销价格	库存	数量

400-920-2911

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描述COH000 is a highly specific covalent allosteric inhibitor of SUMO E1 with little ability to inhibit other canonical Ubl E1s, including Uba1, Uba6, Nedd8 E1 or the noncanonical Ubl E1, Uba5. COH000 inhibited the ATP-dependent step of SUMO E1 catalysis and inhibited SUMOylation with an average IC50 of approximately 0.2μM in vitro, but did not inhibit ubiquitylation in a Ubc13-mediated poly-ubiquitylation assay tested under the same condition at concentrations up to 100μM, with over 500-fold selectivity for SUMOylation than ubiquitylation. COH000 at concentration ranging in 2-16μM inhibited SUMO E1-catalyzed Ubc9-SUMO thioester formation in a dose-dependent manner. It increased the degradation of SAE2 in pulse-chase assays, likely because the inactive conformation enhanced ubiquitin-proteasome-mediated degradation. COH000 at concentration of 10 and 20μM inhibited SUMOylation in HCT-116 cells in a dose-dependent manner upon 18-hour treatment.
作用机制COH000 targets a cryptic binding pocket on SUMO E1 and exploits conformational coupling of SUMO E1 domains.^[1]
参考文献

实验方案

技术信息

CAS号

1534358-79-6

储存条件

分子式

C25H25NO5

运输

蓝冰

分子量

419.47

别名

溶解度

DMSO	32.5 mg/mL (77.5 mM)
Water	insoluble

动物实验配方

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