| 产品描述： | MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM |
| 靶点： |
IC50: 0.23 to 44 μM (IRE1α);IRE1 |
| 体外研究： |
At 10 μM concentration, MKC9989 completely inhibits both basal and thapsigargin induced splicing of XBP1 mRNA. These effects are observed even in cells pre-treated with thapsigargin, indicating that MKC9989 can fully reverse the onset of XPB1 splicing after the UPR is initiated. In parallel analysis, MKC9989, significantly stabilizes the RIDD target CD59 mRNA when co-administered with thapsigargin relative to thapsigargin treatment alone and modestly increases levels of CD59 mRNA in non-stressed cells, the latter likely reflects the inhibition of baseline RIDD activity. In contrast to effects on XBP1 splicing, MKC9989 moderately stabilizes CD59 levels when administered 2 hour post treatment with thapsigargin. Finally, the potency of MKC9989 against the splicing of XBP1 mRNA (EC50=0.33 μM) is comparable to its potency against RNA cleavage in vitro |
| 参考文献： |
1. Sanches M, et al. Structure and mechanism of action of the hydroxy-aryl-aldehyde class of IRE1 endoribonuclease inhibitors. Nat Commun. 2014 Aug 28;5:4202. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.973 ml |
14.866 ml |
29.732 ml |
| 5 mM |
0.595 ml |
2.973 ml |
5.946 ml |
| 10 mM |
0.297 ml |
1.487 ml |
2.973 ml |
| 50 mM |
0.059 ml |
0.297 ml |
0.595 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