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COH000
- Soluble in DMSO
- MF: C25H25NO5
- MW: 419.47
Description
COH000 is a first-in-class, highly specific, covalent allosteric inhibitor of the SUMO E1 activating enzyme. COH000 has been demonstrated to induce strong anti-tumor effects in colorectal cancer cells as well as mouse and patient-derived xenograft models.
More Information
| Parent CAS No. | 1534358-79-6 |
|---|---|
| Chemical Name | Dimethyl 1-(1-(phenylamino)-2-p-tolylethyl)-7-oxabicyclo[2.2.1]hepta-2,5-diene-2,3-dicarboxylate |
| SMILES | C1(C(=O)OC)C2OC(C(NC3C=CC=CC=3)CC3C=CC(C)=CC=3)(C=C2)C=1C(=O)OC |
| MFCD | N.A. |
| InChi | InChI=1S/C25H25NO5/c1-16-9-11-17(12-10-16)15-20(26-18-7-5-4-6-8-18)25-14-13-19(31-25)21(23(27)29-2)22(25)24(28)30-3/h4-14,19-20,26H,15H2,1-3H3 |
| InChiKey | UFPINDDCTUCUSA-UHFFFAOYSA-N |
| CID | 75216152 |
| Short Description | SUMO E1 inhibitor |
References
- Z Lv et al. Molecular mechanism of a covalent allosteric inhibitor of SUMO E1 activating enzyme. Nat Commun. 2018 Dec 4;9(1):5145.
- YJ Li 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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