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Biological Activity:
Selective, cell permeable and ATP-competitive ERK inhiitor; 30-fold selective on ERK over p38α MAPK; FR180204 was shown to inhibit ERK1 (Ki=0.31μM), ERK2 (Ki=0.14 μM) and TGFβ-induced AP-1 activation.
References:
M Ohori et al. Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex. Biochem Biophys Res Commun. 2005, 336(1), 357-363. [online]
M Ohori. ERK inhibitors as a potential new therapy for rheumatoid arthritis. Drug News Perspect. 2008, 21(5), 245-250. [online]
Chemical Name: 3-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-7H-pyrazolo[3,4-c]pyridazin-5-amine
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