COH000
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; 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. (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.
Product Specifications
CAS Number
1534358-79-6
Product Name Alternative
COH-000 | COH 000 | CID 46835111 | SID 99212997
Purity
>98% (HPLC)
Solubility
DMSO: Soluble (< 1 mg/ml refers to the product slightly soluble or insoluble)
Smiles
O=C (C1=C (C (OC) =O) C2C=CC1 ([C@H] (NC3=CC=CC=C3) CC4=CC=C (C) C=C4) O2) OC
Molecular Formula
C25H25NO5
Molecular Weight
419.477
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
Dimethyl 1- ((R) -1- (phenylamino) -2- (p-tolyl) ethyl) -7-oxabicyclo[2.2.1]hepta-2,5-diene-2,3-dicarboxylate
Available Sizes
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