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Technical Resources
Technical Information
Calbiochem Information
Interactive Pathways
MAPK Family
MAPK Signaling Pathway: MAPK Inhibitors
 
 
Selected Cell-Permeable Inhibitors of MAP Kinase and MAP Kinase Kinase (MEK):
Product
Cat. No.
M.W.
Comments
ERK Activation Inhibitor I,
Cell-Permeable
1757.3
A stearated 13-amino acids peptide corresponding to the N-terminal of MEK1. Acts as a specific inhibitor of ERK activation and the transcriptional activity of ELK1. Selectively binds to ERK2 and prevents its interaction with MEK (IC50 = 2.5 µM).
ERK Activation Inhibitor II,
Cell-Permeable
3146.8
A 13-amino acids peptide corresponding to the N-terminal of MEK1 that is fused to the HIV-TAT membrane translocating peptide (MTP) sequence via a glycine linker. Acts as a specific inhibitor of ERK activation and the transcriptional activity of ELK1 by binding to ERK2, and prevents its interaction with MEK (IC50 = 210 nM).
ML3163
423.5
A potent and specific p38 MAP kinase inhibitor (IC50 = 4 µM). Acts by occupying the ATP binding site of p38 MAP kinase.
p38 MAP Kinase Inhibitor
365.8
A potent p38 MAP kinase inhibitor (IC50 = 35 nM).
PD 98059
267.3
A potent and selective MEK inhibitor. It selectively blocks the activation of MEK, thus preventing its phosphorylation by cRaf or MEK kinase (IC50 = 2 – 7 µM).
PD 169316
360.3
A potent, and selective p38 MAP kinase inhibitor (IC50 = 89 nM).
SB 202474
279.3
A negative control for MAP kinase inhibition studies.
SB 202190
331.3
A potent, and selective p38 MAP kinase inhibitor (IC50 = 50 nM for SAPK2a/p38 and 100 nM for SAPK2b/p38b2).
SB 203580
377.4
A potent and selective p38 MAP kinase inhibitor (IC50 = 50 nM for SAPK2a/p38 and 500 nM for SAPK2b/p38b2).
SB 203580, Sulfone
393.4
The sulfone analog of SB 203580 (Cat. No. 559389). Potently inhibits MAP kinase (IC50 = 30 nM).
SB 220025
338.4
A potent and specific inhibitor of human p38 MAP kinase (IC50 = 60 nM). Displays 2000-fold greater selectivity for p38 MAPK over ERK (p42/p44 MAP kinase).
SB 239063
368.4
A potent MAP kinase inhibitor (IC50 = 44 nM for inhibition of recombinant purified human p38a).
SC 68376
236.3
A potent and selective inhibitor of p38 MAP kinase (IC50 = 2 – 5 µM).
U0124
226.3
A useful negative control for MEK inhibitors U0125 (Cat. No. 662008) and U0126 (Cat. No. 662005).
U0125
350.5
A potent and specific inhibitor of MEK1 and MEK2. About 10-fold less potent than U0126 (Cat. No. 662005).
U0126
380.5
A potent and specific inhibitor of MEK1 (IC50 = 72 nM) and MEK2 (IC50 = 58 nM).
 
 
MAP Kinases (and related) Inhibitors: