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编 号:F329941
分子式:C20H16N6S
分子量:372.45
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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生物活性:
AS601245 is an orally active, selective, ATP competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. AS601245 exhibits 10- to 20-fold selectivity over c-src, CDK2, and c-Raf and more than 50- to 100-fold selectivity over a range of Ser/Thr- and Tyr-protein kinases. Neuroprotective properties.

体内研究:
AS601245 (40、60 和 80 mg/kg;腹腔注射) 在短暂性全脑缺血的沙鼠模型中提供显著保护,防止海马 CA1 神经元延迟丢失。 AS601245 (0.3-10 mg/kg;po) 是小鼠体内 LPS 诱导的 TNF-α 释放的有效抑制剂。Animal Model:C3H/HEN mice
Dosage:0.3, 1, 3, or 10 mg/kg
Administration:P.o.
Result:Decreased the TNF-α release in a dose-dependent manner.

体外研究:
抗炎 JNK 抑制剂 AS601245 和 Clofibrate 在诱导细胞反应和影响 CaCo-2 结肠癌细胞的基因表达谱方面具有协同作用。
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