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化学性质:
规格 | 5mg 10mg 50mg 500mg 1g |
CAS | 303162-79-0 |
别名 | N/A |
化学名 | N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]pyridin-2-yl]benzamide |
分子式 | C24H21N3OS |
分子量 | 399.52 |
溶解度 | ≥ 40mg/mL in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
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].
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原创作者:上海莼试生物技术有限公司
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