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50's for JNK3 and p38 were determined using HTRF. Briefly, final assay concentrations of JNK3, biotinylated-ATF2 and ATP were 0.3 nM, 0.4 nM, and 1 μM, respectively. Final assay concentrations of p38, biotinylated-ATF2, and ATP were 1 nM, 0.4 nM, and 11.5 μM, respectively. In both assays, the phospho-Thr71-ATF-2 product was detected by a Europiumcryptate-labeled anti-phospho-Thr71-ATF-2 antibody. Streptavidin-allophycocyanin-XL was used as the acceptor. A 10-point dose-response curve for each compound was generated in duplicate and data were fit to a four parameter logistic.
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note
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1/2), clearance (CL), and volume of distribution (Vd) were calculated. CNS exposure was evaluated in C57Bl6 mice (n = 3). Compounds were dosed at 10 mg/kg intraperitoneally and after 2 h blood and brain were collected. Plasma was generated and the samples were frozen at -80 °C. The plasma and brain were mixed with acetonitrile (1:5 v/v or 1:5 w/v, respectively). The brain sample was sonicated with a probe tip sonicator to break up the tissue, and samples were analyzed for drug levels by LC-MS/MS. Plasma drug levels were determined against standards made in plasma and brain levels against standards made in blank brain matrix. All procedures were approved by the Scripps Florida IACUC.
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