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COH000
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
COH000图片
CAS NO:1534358-79-6
包装与价格:
包装价格(元)
250mg电议
500mg电议

产品介绍
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。
Cas No.1534358-79-6
别名(1R,4S)-二甲基1-((R)-1-(苯基氨基)-2-(对甲苯基)乙基)-7-氧杂二环[2.2.1]庚-2,5-二烯-2,3-二羧酸
Canonical SMILESCC(C=C1)=CC=C1C[C@@H](NC2=CC=CC=C2)[C@]34C(C(OC)=O)=C(C(OC)=O)[C@@H](O4)C=C3
分子式C25H25NO5
分子量419.47
溶解度DMSO : 35.71 mg/mL (85.13 mM);Water :< 0.1 mg/mL (insoluble)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.