Western blot analysis of extracts from SK-MEL-28 cells, untreated (-) or treated with Vemurafenib (24 hr) at the indicated concentrations, using Phospho-p44/42 MAPK (Erk1/2) (Thr202/Tyr204) (D13.14.4E) XP® Rabbit mAb #4370,
p44/42 MAPK (Erk1/2) (137F5) Rabbit mAb #4695, Phospho-MEK1/2 (Ser217/221) (41G9) Rabbit mAb #9154, and
MEK1/2 (D1A5) Rabbit mAb #8727.Learn more about how we get our images
Chemical structure of Vemurafenib.Learn more about how we get our images
Vemurafenib is supplied as a lyophilized powder. For a 50 mM stock, reconstitute the 5 mg of powder in 204.12 μl of DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used between 0.5-50 μM for 24 hrs.
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.
Vemurafenib, also known as PLX4032, is an inhibitor of mutated BRAF (V600E) (1,2). The BRAF kinase is responsible for the activation of MEK and in turn, activating ERK and other downstream transcription factors involved in cell differentiation, proliferation, growth and apoptosis (1). The V600E mutation elevates the catalytic activity of BRAF which in turn renders it insensitive to negative feedback, thus causing hyperactivation of ERK signaling (2). Ultimately, the inhibition of mutated BRAF will cause a cascade of inhibitory actions against downstream targets, such as ERK and MEK1/2 (1,2).
Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc. XP is a registered trademark of Cell Signaling Technology, Inc.
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