An inhibitor of p38α MAPK (IC50 = 7.1 nM); selective for p38α over p38β (IC50 = 200 nM)

TAK-715 – 50 mg

Brand:
Cayman
CAS:
303162-79-0
Storage:
-20
UN-No:
Non-Hazardous - /

TAK-715 is an inhibitor of p38α MAPK (IC50 = 7.1 nM).{45144} 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.{45144,27226} 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.{45144} 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.{27226}  

 

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SKU: 26170 - 50 mg Category:

Description

An inhibitor of p38α MAPK (IC50 = 7.1 nM); 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 CK1δ and CK1ε; inhibits LPS-induced TNF-α release from THP-1 cells (IC50 = 48 nM); LPS-induced TNF-α production by 87.6% in mice at 10 mg/kg; reduces adjuvant-induced paw swelling in a rat model of rheumatoid arthritis at 30 mg/kg; inhibits Wnt3a-induced phosphorylation of hDvl2 in a p38α-independent manner

Formal name: N-[4-[2-ethyl-4-(3-methylphenyl)-5-thiazolyl]-2-pyridinyl]-benzamide

Synonyms: 

Molecular weight: 399.5

CAS: 303162-79-0

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|p38 MAPK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Immunology & Inflammation|Innate Immunity

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