| 產(chǎn)品描述： | 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 |
| 靶點(diǎn)： |
hJNK1:150 nM (IC50);hJNK2:220 nM (IC50);hJNK3:70 nM (IC50);JNK |
| 體外研究： |
AS601245, an anti-Inflammatory JNK inhibitor, and Clofibrate have a synergistic effect in inducing cell responses and in affecting the gene expression profile in CaCo-2 colon cancer cells |
| 體內(nèi)研究： |
AS601245 (40, 60, and 80 mg/kg; i.p.) provides significant protection against the delayed loss of hippocampal CA1 neurons in a gerbil model of transient global ischemia. AS601245 (0.3-10 mg/kg; p.o.) is a potent inhibitor of LPS-induced TNF-α release in mice. 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. |
| 參考文獻(xiàn)： |
1. Carboni S, et al. AS601245 (1,3-benzothiazol-2-yl (2-[[2-(3-pyridinyl) ethyl] amino]-4 pyrimidinyl) acetonitrile): a c-Jun NH2-terminal protein kinase inhibitor with neuroprotective properties. J Pharmacol Exp Ther. 2004;310(1):25-32. |
| 溶解性： |
Soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.685 ml |
13.425 ml |
26.85 ml |
| 5 mM |
0.537 ml |
2.685 ml |
5.37 ml |
| 10 mM |
0.268 ml |
1.342 ml |
2.685 ml |
| 50 mM |
0.054 ml |
0.268 ml |
0.537 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險(xiǎn)品化學(xué)品經(jīng)營(yíng)許可證（不帶存儲(chǔ)）
營(yíng)業(yè)執(zhí)照(三證合一)
北京