COH000 |
رقم الكتالوجGC33039 |
COH000 هو مثبط خيفي وتساهمي ولا رجوع فيه من إنزيم منشط 1 يشبه يوبيكويتين (إنزيم تنشيط SUMO) (E1) ، مع IC 50 من 0.2 ميكرومتر من أجل SUMOylation في المختبر
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Cas No.: 1534358-79-6
Sample solution is provided at 25 µL, 10mM.
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.
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