COH000

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

COH000  纯度: ≥98.0%

COH000 是共价的、不可逆的泛素样激活酶1 (E1) 的变构抑制剂，体外测得对 SUMO 化修饰的 IC50 值为 0.2 μM。

COH000

COH000 Chemical Structure

CAS No. : 1534358-79-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥6500 In-stock
5 mg ￥5900 In-stock
10 mg ￥8000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

COH000 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Oxygen Sensing Compound Library
  • Ubiquitination Compound Library
  • Anti-Liver Cancer Compound Library

生物活性

COH000 is an allosteric, covalent and irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) (E1), with an IC50 of 0.2 μM for SUMOylation in vitro[1].

IC50 & Target

IC50: 0.2 μM (SUMO-activating enzyme)[1].
体外研究
(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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

419.47

Formula

C25H25NO5
CAS 号

1534358-79-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 35.71 mg/mL (85.13 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3840 mL 11.9198 mL 23.8396 mL
5 mM 0.4768 mL 2.3840 mL 4.7679 mL
10 mM 0.2384 mL 1.1920 mL 2.3840 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务