Other
CN
EU
USA
Description: TAK-715 is a novel, potent and selective p38 MAPK (p38 mitogen-activated protein) inhibitor with potential anti-inflammatory activity. It inhibits p38α with an IC50 of 7.1 nM, and is 28-fold more selective for p38α over p38β, it shows no/little inhibition against p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1. TAK-715 is currently under clinical investigation for the treatment of Rheumatoid arthritis-RA.
References: J Med Chem. 2005 Sep 22;48(19):5966-79; Chem Biol. 2011 Apr 22;18(4):485-94.
Synonym: TAK 715, TAK715, TAK-715
Chemical Name: N-(4-(2-ethyl-4-(m-tolyl)thiazol-5-yl)pyridin-2-yl)benzamide
InChi Key: HEKAIDKUDLCBRU-UHFFFAOYSA-N
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)
SMILES Code: O=C(NC1=NC=CC(C2=C(C3=CC=CC(C)=C3)N=C(CC)S2)=C1)C4=CC=CC=C4
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
In vitro activity: TAK 715 inhibits LPS-stimulated release of TNF-alpha from THP-1 with IC50 of 48 nM. TAK 715 (10 μM) inhibits Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift in U2OS-EFC cells. The amide NH of TAK 715 is hydrogen bonded to the main-chain carbonyl of Met109 of p38 alpha. TAK 715 binds relatively high in the ATP pocket, occupying the hydrophobic back pocket, the adenine region and the front pocket of p38 as well as extending to most of the length of the Gly-rich loop.
Kinase Assay: TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1.
Cell Assay: TAK 715 inhibits LPS-stimulated release of TNF-alpha from THP-1 with IC50 of 48 nM. TAK 715 (10 μM) inhibits Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift in U2OS-EFC cells. The amide NH of TAK 715 is hydrogen bonded to the main-chain carbonyl of Met109 of p38 alpha. TAK 715 binds relatively high in the ATP pocket, occupying the hydrophobic back pocket, the adenine region and the front pocket of p38 as well as extending to most of the length of the Gly-rich loop.
Purity ≥98%
COA
MSDS