| Description |
A cell-permeable cyclohexylamino-indenone compound that acts as an allosteric inhibitor against substrate binding-induced MAPK phosphatase activity of Dusp1/CL100/HVH1/MKP1/PTPN10 and Dusp6/MKP3/PYST1 (57% and 30% reduction, respectively, of 0.21 and 2.1 µg Erk2-induced OMFP dephosphorylation by 0.21 µg Dusp6) by locking Dusp1 and Dusp6 in their low-activity conformation, while exhibiting little activity toward Cdc25B, DUSP3/VHR, DUSP5, or PTP1B. Shown to effectively enhance cellular Erk phosphorylation in HeLa cells overexpressing human Dusp1 and Dusp6 (EC 50 = 11.5 and 12.3 µM, respectively)
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