| 產(chǎn)品描述： | JNK Inhibitor VIII (TCS JNK 6o) 是一種 c-Jun N-terminal kinases 的抑制劑，對JNK-1和JNK-2的IC50值分別為45 nM和160 nM。JNK Inhibitor VIII (TCS JNK 6o) 可抑制JNK-1、JNK-2和JNK-3，對應(yīng)的Ki值分別為2 nM、4 nM和52 nM |
| 靶點： |
JNK1(Cell-free assay):2 nM(Ki); JNK2(Cell-free assay):4 nM(Ki); JNK1(Cell-free assay):45 nM; JNK3(Cell-free assay):52 nM(Ki); JNK2(Cell-free assay):160 nM;JNK |
| 體內(nèi)研究： |
Pharmacokinetic profiles are determined for JNK Inhibitor VIII (TCS-JNK-6o) in Sprague-Dawley rats. JNK Inhibitor VIII (TCS-JNK-6o) showes a short half-life of roughly 1 h, with rapid clearance and barely measurable bioavailability. Microsomal incubation studies revealed that oxidative metabolism is very rapid with this compound |
| 細(xì)胞實驗： |
Cell lines: hepG2 cells Concentrations: Serial concentrations Incubation Time: 1 h Method: HepG2 human hepatoma cells (ATCC) are cultured in low glucose MEM supplemented with 1×NEAA, 1×sodium pyruvate, and 10% FBS. For P-c-Jun assays, cells are plated at 5×104 cells/well in 500 μL of complete media on 24-well collagen-coated plates and incubated overnight. Serial compound dilutions are made in DMSO at 100×, and then 5 μL is added directly to the media on the cells to provide the final inhibitor concentrations. After 1 h, cells are stimulated with vehicle control or TNFR for 30 min and harvested in 70μL of lysis buffer (TBS (54 mM Tris-HCl, pH 7.6, 150 mM NaCl), 1% TritonX-100,0.5% Nonidet P-40, 0.25% sodium deoxycholate, 1 mM EDTA, 1 mM EGTA, 0.5 mM sodium fluoride, 1 mM pervanadate, 1 μM microcystin, 1 mM AEBSF, 1 tablet of complete EDTA Free-Mini inhibitor cocktail) and frozen at -80 °C prior to use in the P-c-Jun assay. |
| 動物實驗： |
Animal Models: Sprague-Dawley rat Dosages: 5 mg/kg Administration: IV, Oral gavage |
| 參考文獻(xiàn)： |
1. Bruce G Szczepankiewicz, et al. J Med Chem. 2006 Jun 15;49(12):3563-80. |
| 溶解性： |
Soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.806 ml |
14.03 ml |
28.06 ml |
| 5 mM |
0.561 ml |
2.806 ml |
5.612 ml |
| 10 mM |
0.281 ml |
1.403 ml |
2.806 ml |
| 50 mM |
0.056 ml |
0.281 ml |
0.561 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。 |
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危險品化學(xué)品經(jīng)營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京