FMK is a potent, highly specific and irreversible ribosomal s6 kinase (RSK) inhibitor that covalently modifies the C-terminal kinase domain of RSK. Its IC50 value is 15 nM. It could prevent the activation of the N-terminal kinase domain of RSK by the C-terminal kinase domain, but does not affect the activity of the N-terminal domain. It binds in the CTKD ATP-binding site and inhibits RSK autophosphorylation at Ser386. It induces significant apoptosis in human FGFR3-expressing, t(4;14)-positive multiple myeloma cells. It is used to determine the role of RSK as a direct regulator of NHE1 phosphorylation and sarcolemmal NHE activity in this cell type, in response to 1-adrenergic stimulation.
Products > Drug Discovery > Inhibitor | Products > Drug Discovery > Inhibitor | Cancer | Ribosomal S6 Kinase (RSK)
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