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Beschreibung

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 microg Erk2-induced OMFP dephosphorylation by 0.21 microg 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 (EC50 = 11.5 and 12.3 microM, respectively). FGF signaling activation by BCI treatment (5 to 10 microM) during zebrafish embryo development is reported to expand myocardial progenitors population at the expense of other progenitor cell types, resulting in enlarged heart size.