| 產品描述： | JNK-IN-8 is an irreversible JNK1/2/4 inhibitor (IC50: 4.7/18.7/1 nM). The selectivity is higher 10-fold than MNK2, Fms and no inhibition of Met, c-Kit, PDGFRβ in A375 cell line. |
| 靶點： |
c-Kit JNK;JNK;c-Kit |
| 體內研究： |
JNK-IN-8（10 mM）對IL-1R細胞中IL-1β刺激的c-Jun磷酸化有抑制作用。與伊馬替尼相比,JNK-IN-8有明顯的1,4-雙苯胺和1,3-氨基苯甲酸結構區(qū)域選擇性,且以N,N-二甲基丁烯乙酰胺共價結合Cys154靶點。JNK-IN-8抑制HeLa（EC50：486 nM）和A375（EC50：338 nM）細胞中c-Jun的磷酸化。JNK-IN-8與PIK3C3,IRAK1,PIP5K3和PIP4K2C結合可使選擇性和消除率顯著提高。JNK-IN-8經Cys116抑制JNK2 |
| 細胞實驗： |
JNK-IN-8 is dissolved in DMSO and stored, and then diluted with appropriate media before use. HEK-293 cells stably expressing Interleukin Receptor 1 (HEK293-IL1R) are cultured in Dulbecco's Modified Eagle's medium (DMEM) supplemented with 10% FBS, 2 mM glutamine and 1×antimycotic/antibiotic solution. Cells are serum starved for 18 h before incubation with DMSO or JNK-IN-8, stimulated with 2 μM Anisomycin for 1h and lysates are clarified by centrifugation for 10 min at 16000 g and 4°C |
| 參考文獻： |
1.Liu Q, et al. Chem Biol, 2013, 20(2), 146-159. 2.Zhang T, et al. Chem Biol, 2012, 19(1), 140-154. 3.Goh ET, et al. Biochem J, 2012, 441(1), 339-346. |
| 溶解性： |
Ethanol:<1 mg/mL DMSO:93 mg/mL (183.2 mM) H2O:<1 mg/mL |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.97 ml |
9.85 ml |
19.701 ml |
| 5 mM |
0.394 ml |
1.97 ml |
3.94 ml |
| 10 mM |
0.197 ml |
0.985 ml |
1.97 ml |
| 50 mM |
0.039 ml |
0.197 ml |
0.394 ml |
|
| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京