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MEK Inhibitor U0126
Block the ERK Pathway with a
Novel and Potent Inhibitor
MEK Inhibitor U0126 is a
chemically synthesized organic compound that inhibits the kinase
activity of MAP kinase kinase, MEK.
Features:
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U0126 Inhibits both active and
inactive MEK1,2 unlike PD098059 which ony inhibits
activation of inactive MEK (1,2).
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Suitable for use in in vitro and cellular
investigations (1-6).
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Downstream inhibition of ERK 1 and ERK 2
mediated responses.
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More potent and less toxic than PD098059
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Compatible reagents available:
Anti-ACTIVE® MAPK pAb, Rabbit
(pTEpY) (Cat.#
V8031)
Anti-ERK 1/2 pAb, Rabbit "pan" (Cat.#
V1141)
Application Data:
U0126 inhibits NGF-induced
activation of ERK 1/2 in PC12 cells. PC12 cells were grown
in serum-free RPMI medium for 16 hours. The inhibitor U0126 was
added to the medium at 10µM in 0.2% DMSO for 15 minutes. NGF was
then added at a final concentration of 50ng/ml, and the cells were
incubated for either 5 or 30 minutes before harvesting and lysing.
Protein samples (20µg) were analyzed by SDS-PAGE and Western blot.
Detection was performed with Anti-ERK 1/2 pAb and Anti-ACTIVE®
MAPK pAb using chemiluminescence detection (Tropix). Panel
A: The amount of total ERK 1/2 shows little change with the
various treatments, as detected by the Anti-ERK 1/2 pAb. Panel
B: Using Anti-ACTIVE® MAPK pAb, which
recognizes only the active ERK 1/2, U0126 completely inhibited the
activation of ERK 1/2 in NGF-treated PC12 cells at both 5 and 30
minutes. Lane 1, no NGF; lane 2, NGF for 5 minutes; lane 3, NGF for
30 minutes; lane 4, U0126; lane 5, U0126 + NGF for 5 minutes; lane
6, U0126 + NGF for 30 minutes (7).
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