Western blot analysis of extracts from HeLa cells, untreated (-) or treated with TPA #4174 (200 nM, 20 min; +) with or without pretreating the cells with Trametinib for 1 hour at the indicated concentrations, using Phospho-p44/42 MAPK (Erk1/2) (Thr202/Tyr204) (D13.14.4E) XP® Rabbit mAb #4370 (upper), p44/42 MAPK (Erk1/2) (137F5) Rabbit mAb #4695 (middle), and β-Actin (D6A8) Rabbit mAb #8457 (lower).
Chemical structure of Trametinib.
Trametinib is supplied as a lyophilized powder. For a 15 mM stock, reconstitute 10 mg of powder in 1.08 ml of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.
Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
Molecular Weight: 615.4 g/mol
Molecular Formula: C26H23FIN5O4
Solubility: Soluble in DMSO at 20 mg/ml with slight warming.
Trametinib, also known as GSK1120212, is a potent and selective inhibitor of MEK with an IC50 of 0.7 nM for u-MEK1 and 14.9 nM for pp-MEK1 (1). When compared to several tyrosine kinase inhibitors (TKIs) and MEK inhibitors (MEKIs) in endothelial cells, Trametinib displays the highest level of antiangiogenic activity and is the most effective ERK1/2 inhibitor (IC50 = 1.3 nM) (2). Trametinib has also been shown to be the most effective at reducing proliferation in low-grade serous ovarian cancers (LGSCs) when compared to other MEKIs (3).
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