303162-79-0 Usage
Uses
TAK 715 is a p38 MAPK inhibitor for p38α and p38β but not for p38γ and p38δ.
Biological Activity
tak-715 is a selective inhibitor of p38 mapk with ic50 value of 7.1 nm [1].p38 mitogen-activated protein (map) kinases (p38 mapks) are a class of mitogen-activated protein kinases and play an important role in controlling cellular responses to cytokines and stress. four p38 mapks contain members, p38-α (mapk14), p38-β (mapk11), p38-γ (mapk12/erk6), and p38-δ (mapk13/sapk4), have been identified. abnormal expression of p38 mapks are correlated with a variety of chronic inflammatory diseases and their inhibitors are regarded as promising targets in clinical [1] [2].tak-715 is a potent p38 mapk inhibitor and has a different selectivity with the reported p38 mapk inhibitor vx-745. when tested with human monocytic thp-1 cells, administration of tak-715 exhibited inhibition on p38mapkα with ic50 value of 7.1 nm [1]. in hek293t, u2os, and f9 cells, tak-715 was used to inhibit p38 mapk activity and concluded that p38 mapk had no function in wnt/β-catenin signaling pathway [2].in adjuvant-induced rheumatoid arthritis rat model, administration of tak-715 at dose of 10 mg/kg significantly decreased lps-induced stimulated release of tnf-α (87.6%) by inhibiting p38 mapk activity [1].
references
[1]. 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 chem, 2005. 48(19): p. 5966-79. [2]. verkaar, f., et al., inhibition of wnt/beta-catenin signaling by p38 map kinase inhibitors is explained by cross-reactivity with casein kinase idelta/varepsilon. chem biol, 2011. 18(4): p. 485-94.
Check Digit Verification of cas no
The CAS Registry Mumber 303162-79-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,0,3,1,6 and 2 respectively; the second part has 2 digits, 7 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 303162-79:
(8*3)+(7*0)+(6*3)+(5*1)+(4*6)+(3*2)+(2*7)+(1*9)=100
100 % 10 = 0
So 303162-79-0 is a valid CAS Registry Number.
303162-79-0Relevant articles and documents
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
Miwatashi, Seiji,Arikawa, Yasuyoshi,Kotani, Etsuo,Miyamoto, Maki,Naruo, Ken-Ichi,Kimura, Hiroyuki,Tanaka, Toshimasa,Asahi, Satoru,Ohkawa, Shigenori
, p. 5966 - 5979 (2007/10/03)
The p38 mitogen-activated protein (MAP) kinase has been implicated in the proinflammatory cytokine signal pathway, and its inhibitors are potentially useful for the treatment of chronic inflammatory diseases such as rheumatoid arthritis (RA) and inflammat
