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COH000

Names

[ CAS No. ]:
1534358-79-6

[ Name ]:
COH000

Biological Activity

[Description]:

COH000 is an inhibitor of Ubiquitin-like 1-activating enzyme (SUMO-activating enzyme), with an IC50 of 0.2 μM for SUMOylation in vitro[1].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> E1/E2/E3 Enzyme
Research Areas >> Cancer

[Target]

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


[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].

[References]

[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.


[Related Small Molecules]

Ginkgolic acid C15:1 | PYR-41 | NSC232003 | CC122 | SZL P1-41 | TAK-243(MLN7243) | 2-Chloro-N-(3,4-dimethoxybenzyl)acetamide | PRT 4165 | SKPin C1 | TZ9 | CC 0651 | 2-D08 | PYZD 4409 | CC-885

Chemical & Physical Properties

[ Molecular Formula ]:
C25H25NO5

[ Molecular Weight ]:
419.47

[ Storage condition ]:
2-8℃

Related Compounds