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COH000

Chemical Structure : COH000

CAS No.: 1534358-79-6

COH000 (COH-000;COH 000;CID 46835111;SID 99212997)

Catalog No.: PC-35900Not For Human Use, Lab Use Only.

COH000 (COH-000) is a highly selective, first-in-class, irreversible, allosteric, covalent inhibitor of SUMO-Activating Enzyme E1, inhibits SUMOylation in vitro with IC50 of 0.2 uM, displays >500-fold selectivity for SUMOylation over ubiquitylation.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

COH000 (COH-000) is a highly selective, first-in-class, irreversible, allosteric, covalent inhibitor of SUMO-Activating Enzyme E1, inhibits SUMOylation in vitro with IC50 of 0.2 uM, displays >500-fold selectivity for SUMOylation over ubiquitylation.
COH000 increased the degradation of SAE2, increases the expression of miR-34b and reduces c-Myc levels in lymphoma and colorectal cancer cell lines and a colorectal cancer xenograft mouse model.

Physicochemical Properties

M.Wt 419.477
Formula C25H25NO5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

dimethyl 1-((R)-1-(phenylamino)-2-(p-tolyl)ethyl)-7-oxabicyclo[2.2.1]hepta-2,5-diene-2,3-dicarboxylate

References

1. Li YJ, et al. Cell Chem Biol. 2018 Dec 5. pii: S2451-9456(18)30386-6. doi: 10.1016/j.chembiol.2018.10.026.

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