| 产品描述： | 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. |
| 靶点： |
c-Kit JNK;JNK;c-Kit |
| 体内研究： |
JNK-IN-8（10 mM）对IL-1R细胞中IL-1β刺激的c-Jun磷酸化有抑制作用。与伊马替尼相比,JNK-IN-8有明显的1,4-双苯胺和1,3-氨基苯甲酸结构区域选择性,且以N,N-二甲基丁烯乙酰胺共价结合Cys154靶点。JNK-IN-8抑制HeLa（EC50：486 nM）和A375（EC50：338 nM）细胞中c-Jun的磷酸化。JNK-IN-8与PIK3C3,IRAK1,PIP5K3和PIP4K2C结合可使选择性和消除率显著提高。JNK-IN-8经Cys116抑制JNK2 |
| 细胞实验： |
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 |
| 参考文献： |
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 |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
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： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京