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HOIPIN 11a
- GSK11a - HOIP inhibitor 11a
- Soluble in DMSO
- MF: C15H18N2O4
- MW: 290.31
Description
Selective, cell-permeable and covalent inhibitor of the RBR E3 ubiquitin ligase HOIP. Biochemical characterization of HOIPIN 11a demonstrated that this compound labels HOIP with promising proteome-wide selectivity and effectively inhibits linear polyubiquitin chain formation in vitro and in a cellular environment. Treating HEK293T cells overexpressing full length HOIP, HOIL-1L, and SHARPIN with compound 11a overnight led to inhibition of NF-κB activation in a concentration-dependent manner, with an estimated IC50 value of 37 μM.
More Information
| Parent CAS No. | 1610800-91-3 |
|---|---|
| Chemical Name | (E)-Methyl 4-(2-oxo-1,2,5,6,7,8-hexahydroquinoline-3-carboxamido)but-2-enoate |
| SMILES | C12CCCCC=1NC(=O)C(C(=O)NC/C=C/C(=O)OC)=C2 |
| MFCD | N.A. |
| InChi | InChI=1S/C15H18N2O4/c1-21-13(18)7-4-8-16-14(19)11-9-10-5-2-3-6-12(10)17-15(11)20/h4,7,9H,2-3,5-6,8H2,1H3,(H,16,19)(H,17,20)/b7-4+ |
| InChiKey | NHQZASSXPZNVQW-QPJJXVBHSA-N |
| CID | 129179200 |
| Short Description | HOIP inhibitor |
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