FR180204 inhibited the kinase activity of ERK1 and ERK2, with K(i) values 0.31 and 0.14microM, respectively. FR180204 inhibited TGFbeta-induced luciferase-expression. FR180204 inhibited in vitro CII-induced proliferation of lymph node cells prepared from CII-immunized mice, in which CII-specific T cells are known to undergo specific proliferation.
|Cell lines||Met5A, MSTO-211H, NCI-H28, NCI-H2052, and NCIH2452 cell lines|
|Preparation method||Using MTT to assay cell viability . Using a micro-plate reader to quantify MTT-reactive cells at an absorbance of 570 nm.|
|Incubation time||48 hours|
|Animal models||Collagen-induced arthritis mouse model|
|Formulation||Suspended in 0.1% methylcellulose solution|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex.
Ohori M, et al. Biochem Biophys Res Commun. 2005 Oct 14;336(1):357-63. PMID: 16139248.
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VX-11e is a potent, selective, and orally bioavailable ERK2 inhibitor with Ki of <2 nM, over 200-fold selective over other kinases tested.
XMD8-92 is a potent and selective BMK1/ERK5 inhibitor with Kd of 80 nM.
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