[HTML][HTML] The protein kinase C inhibitors Ro 318220 and GF 109203X are equally potent inhibitors of MAPKAP kinase-1β (Rsk-2) and p70 S6 kinase
DR Alessi - FEBS letters, 1997 - Elsevier
FEBS letters, 1997•Elsevier
The protein kinase C (PKC) inhibitors Ro318220 and GF109203X have been used in over
350 published studies to investigate the physiological roles of PKC. Here we demonstrate
that these inhibitors are not selective for PKC isoforms as was previously assumed.
Ro318220 inhibited MAPKAP kinase-1β (also known as Rsk-2) in vitro (IC50 3 nM) more
potently than it inhibited mixed PKC isoforms (IC50 5 nM), and it also inhibited p70S6 kinase
(IC50 15 nM). GF109203X also potently inhibited MAPKAP kinase-1β (IC50 50 nM) and …
350 published studies to investigate the physiological roles of PKC. Here we demonstrate
that these inhibitors are not selective for PKC isoforms as was previously assumed.
Ro318220 inhibited MAPKAP kinase-1β (also known as Rsk-2) in vitro (IC50 3 nM) more
potently than it inhibited mixed PKC isoforms (IC50 5 nM), and it also inhibited p70S6 kinase
(IC50 15 nM). GF109203X also potently inhibited MAPKAP kinase-1β (IC50 50 nM) and …
The protein kinase C (PKC) inhibitors Ro318220 and GF109203X have been used in over 350 published studies to investigate the physiological roles of PKC. Here we demonstrate that these inhibitors are not selective for PKC isoforms as was previously assumed. Ro318220 inhibited MAPKAP kinase-1β (also known as Rsk-2) in vitro (IC50 3 nM) more potently than it inhibited mixed PKC isoforms (IC50 5 nM), and it also inhibited p70S6 kinase (IC50 15 nM). GF109203X also potently inhibited MAPKAP kinase-1β (IC50 50 nM) and p70S6 kinase (IC50 100 nM) with similar potency to PKC isoforms (IC50 30 nM). The inhibition of MAPKAP kinase-1β, p70S6 kinase, and probably other protein kinases, may explain many of the effects previously attributed to PKC.
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