COH000 - SUMO E1 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECOH000Cat. No.: HY-114304CAS No.: 1534358-79-6分式: CHNO分量: 419.47作靶点: E1/E2/E3 Enzyme作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 35.71 mg/mL (85.13 mM; Need

2、 ultrasonic)H2O : 0.1 mg/mL (insoluble)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3840 mL 11.9198 mL 23.8396 mL5 mM 0.4768 mL 2.3840 mL 4.7679 mL10 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，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 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 SU

3、MO 化修饰的 IC50 值为 0.2 M 1。IC50 & Target IC50: 0.2 M (SUMO-activating enzyme) 1.体外研究COH000 has over 500-fold selectivity for SUMOylation than ubiquitylation. COH000 inhibits SUMO1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEadenylation without directly competing with ATP or SUMO1 binding. COH000 has

4、 an extremely slow off-rateand is consistent with it being covalently bound to the enzyme 1.REFERENCES1. Li YJ, et al. Allosteric Inhibition of Ubiquitin-like Modifications by a Class of Inhibitor of SUMO-Activating Enzyme. Cell Chem Biol. 2018Dec 5. pii: S2451-9456(18)30386-6.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792;Fax: 0