TAK-715

TAK-715 is an inhibitor of p38alpha MAPK (IC50 = 7.1 nM). It is selective for p38alpha over p38beta (IC50 = 200 nM), as well as over p38gamma/delta, JNK, ERK1, IKKbeta, MEKK1, and TAK1 (IC50 = >10 µM for all) but also inhibits casein kinase Idelta (CK1delta) and CK1epsilon. It inhibits TNF-alpha release induced by LPS from THP-1 cells (IC50 = 48 nM) and inhibits LPS-induced TNF-alpha production by 87.6% in mice when administered at a dose of 10 mg/kg. 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 p38alpha-independent manner.Formal Name: N-[4-[2-ethyl-4-(3-methylphenyl)-5-thiazolyl]-2-pyridinyl]-benzamide. CAS Number: 303162-79-0. Molecular Formula: C24H21N3OS. Formula Weight: 399.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 80 mg/mL, Ethanol: 15 mg/mL. lambdamax: 236, 296 nm. SMILES: O=C(NC1=NC=CC(C2=C(C3=CC(C)=CC=C3)N=C(CC)S2)=C1)C4=CC=CC=C4. InChi Code: InChI=1S/C24H21N3OS/c1-3-21-27-22(18-11-7-8-16(2)14-18)23(29-21)19-12-13-25-20(15-19)26-24(28)17-9-5-4-6-10-17/h4-15H,3H2,1-2H3,(H,25,26,28). InChi Key: HEKAIDKUDLCBRU-UHFFFAOYSA-N.