Background
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).
Molecular Formula
C17H14ClF2IN2O22
Molecular Weight
478.66 g/mol
Purity
>99%
CAS
212631-79-3
Solubility
Soluble in DMSO at 50mg/ml and EtOH at 8.3mg/ml.
Storage
Directions for Use
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.
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
Trademarks and Patents
Limited Uses
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