TAK-715

TAK-715 is an inhibitor of p38α MAPK (IC₅₀ = 7.1 nM).¹ It is selective for p38α over p38β (IC₅₀ = 200 nM), as well as over p38γ/δ, JNK, ERK1, IKKβ, MEKK1, and TAK1 (IC₅₀ = >10 µM for all) but also inhibits casein kinase Iδ (CK1δ) and CK1ε.^1,2 It inhibits TNF-α release induced by LPS from THP-1 cells (IC₅₀ = 48 nM) and inhibits LPS-induced TNF-α production by 87.6% in mice when administered at a dose of 10 mg/kg.¹ TAK-715 (30 mg/kg) reduces adjuvant-induced paw swelling in a rat model of rheumatoid arthritis. It also inhibits phosphorylation of human Disheveled 2 (hDvl2) by Wnt3a in a p38α-independent manner.²

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1. Miwatashi, S., Arikawa, Y., Kotani, E., et al. Novel inhibitor of p38 MAP kinase as an anti-TNF-α 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. Chem. 48(19), 5966-5979 (2005).

2. Verkaar, F., van der Stelt, M., Blankesteijn, W.M., et al. Discovery of novel small molecule activators of β-catenin signaling. PLoS One 6(4), e19185 (2011).