Biological descriptionPotent p38 MAPK inhibitor (IC50 = 7.1 nM at p38 MAPKα). Additionally inhibits Wnt-3a stimulated β-catenin signaling and shows cross-reactivity with casein kinase Iδ and ε. Antirheumatic. Active in vivo.
Storage instructionsStore at +4°C. The product can be stored for up to 12 months.
Solubility overviewSoluble in DMSO to 100 mM and in ethanol to 25 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Verkaar F et al. Inhibition of Wnt/ß-catenin signaling by p38 MAP kinase inhibitors is explained by cross-reactivity with casein kinase Id/?. Chem Biol18:485-94 (2011).
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Roberts PJ & Der CJ Targeting the Raf-MEK-ERK mitogen-activated protein kinase cascade for the treatment of cancer. Oncogene26:3291-310 (2007).
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Miwatashi S et al. Novel inhibitor of p38 MAP kinase as an anti-TNF-alpha drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent. J Med Chem48:5966-79 (2005).
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