Chemical structure of PD184352.
Western blot analysis of extracts from HeLa cells, serum-starved overnight and untreated or treated with TPA #4174 (200 nM, 20 min) either with or without PD184352 pretreatment (1 hr) at the indicated concentrations, using Phospho-p44/42 MAPK (Erk1/2) (Thr202/Tyr204) (D13.14.4E) XP® Rabbit mAb #4370 (upper) or p44/42 MAPK (Erk1/2) (137F5) Rabbit mAb #4695 (lower).
PD184352 is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 5 mg in 1044.6 µl DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used as a pretreatment at 0.1-10 µM for 0.5-1 hr prior to treating with a stimulator or is used alone with varying treatment times lasting up to 24 hr. Soluble in DMSO at 25 mg/ml and ethanol at 8 mg/ml with warming; poorly soluble in water with maximum solubility in water at ~5-10 µM.
Store lyophilized or in solution at -20ºC, desiccated. Protect from light. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
PD184352 (CI-1040) is a highly potent and selective noncompetitive MEK inhibitor with an IC50 of 17 nM for MEK1 (1). Treatment of cells with PD184352 leads to suppression of MAPK activation (1-4) and potently inhibits the proliferation of cells harboring the B-Raf mutation V600E (2,3). Researchers have shown that PD184352 effectively inhibits MEK5, although not as potently as MEK1 (4).
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