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Background: The p38 MAPK (mitogen-activated protein kinase) pathway contains protein kinases which engage in respond to various extracellular stimuli an intracellular signalling cascade, coordinating the activation of gene transcription, protein synthesis, cell cycle machinery, cell death, and differentiation. The different p38 MAPK family members (p38α, p38β, p38γ, p38δ) encoded by different genes show an approximately 60% identical in their amino acid sequence but have different tissue expression patterns. p38 MAPKs being activated by dual phosphorylation of the Thr-Gly-Tyr in the activation loop sequence by MKKs/MAP2Ks (MKK6 and MKK3). Down-regulation of p38 MAPK is achieved for instance by Wip1, a phosphatase of the PP2C family that can be transcriptionally up-regulated by p53 or by MKPs, a family of dual-specificity protein phosphatases. Upon activation p38 MAP kinases can phosphorylate substrates on Ser-Pro or Thr-Pro motifs on MSK1 and 2, which directly phosphorylate the transcription factors CREB, ATF1, or cytosolic proteins such as phospholipase A2, Bcl-2 family proteins and cyclins. Because of the important role of p38α in inflammatory diseases it is also an interesting pharmaceutical target. Based on SB203580, one of the first discovered p38α inhibitors structurally diverse p38α and p38β inhibitors have been developed with both enhanced potency and specificity.
Human p38a/SAPK2a, recombinantly expressed in E. coli. Active form of p38alpha kinase produced by phosphorylation of the purified p38alpha with MKK6.
Expression system: E.coli
Molecular weight: 42.7 kDa
Protein concentration: 1.19 mg/ml (Bradford with BSA as standard)
Storage buffer: 25 mM Tris-HCl, 150 mM NaCl, 1 mM DTT, 50 % glycerol, pH 8.5
Purity: > 95% by SDS PAGE
Specific activity: 2,357,900 U*/mg (*1 U = 1 pmol/min transferred to myelin basic protein at 30 degree C). No protease activity detectable.
Entrez Gene ID: 1432
Ordering information: shipped on dry ice
Figure: Real-time kinetic analysis of kinase inhibitor SB203580 binding to p38α using surface plasmon resonance.
We provide our Kinascreen services to kinetically characterize small molecule kinase inhibitors for all p38 isoforms (p38α, p38β, p38γ and p38δ) in their phosphorylated (activated) and unphosphorylated (non-activated) state.
Please contact our application specialists to obtain more information and an individual quote tailored to your specific needs.
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Laferriere J, Houle F, Taher MM, Valerie K, Huot J (2001) "Transendothelial migration of colon carcinoma cells requires expression of E-selectin by endothelial cells and activation of stress-activated protein kinase-2 (SAPK2/p38) in the tumor cells" J Biol Chem. 276(36):33762-72
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Saklatvala J (2004) "The p38 MAP kinase pathway as a therapeutic target in inflammatory disease" Curr Opin Pharmacol. 4(4):372-7
SB203580, 1 mg - 100,00 €
MAPK Inhibitor Set, 5x 50 µl - 245,00 €
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