Description
FMK is a potent and selective inhibitor of p90 ribosomal protein S6 kinaseRSK2 (wt) with IC50 of 15 nM, >600- and 200-fold selectivity for RSK2 than the C436V and T493M mutants.
Storage
2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO.
Molecular Formula
C18H19FN4O2
Chemical Name
Ethanone, 1-[4-amino-7-(3-hydroxypropyl)-5-(4-methylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-2-fluoro-
Solubility
DMSO mg/mL; Water mg/mL; Ethanol mg/mL
In vitro
FMK inhibits the activity of RSK2 with IC50 of 15 nM. FMK suppresses EGF induced Ser386 phosphorylation of endogenous RSK2 in serum-starved COS-7 cells with EC50 of ~200 nM. Pretreatment of myocytes with FMK before exposure to the α1-adrenoceptor agonist phenylephrine inhibited RSK C-terminal kinase activity and thereby RSK N-terminal kinase activation, without affecting MEK or ERK activation. Pretreatment of myocytes with fmk also inhibited phenylephrine-induced increases in NHE1 phosphorylation and the rate of NHE1-mediated H+ efflux under conditions of intracellular acidosis.
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