| 产品描述: | IRE1 抑制剂;IRE1 Inhibitors;;InformationMKC8866 MKC8866 (IRE1-IN-8866), a salicylaldehyde analog, is a specific IRE1α RNase inhibitor with IC50 of 0.29 μM for human IRE1α in vitro.TargetshIRE1α (Cell-free assay) 0.29 μMIn vitroMKC8866 is optimized and refined from a family of IRE1α-specific endoribonuclease inhibitors obtained from a chemical library screen. MKC8866 effectively represses IRE1α-mediated XBP1 splicing in PCa cells and has favorable pharmacokinetic and pharmacodynamic properties.In vivoMKC8866 is an IRE1α RNase-specific inhibitor molecule that displays significant therapeutic activity in various preclinical models of PCa in vivo. MKC8866 synergizes with clinical PCa drugs in vivo.Cell Research(from reference)Cell lines:human PCa cell lines LNCaP and 22Rv1, VCaP cell line, C4-2B cell line Concentrations:0.2-10 μM Incubation Time:0.25-24 h |
| 靶点: |
IC50: 0.29 μM (IRE1 RNase) |
| 体内研究: |
MKC8866 (口服;300 mg/kg;持续 28 天)可减少 NSC 125973 停药后的肿瘤再生。 |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.767 ml |
13.837 ml |
27.674 ml |
| 5 mM |
0.553 ml |
2.767 ml |
5.535 ml |
| 10 mM |
0.277 ml |
1.384 ml |
2.767 ml |
| 50 mM |
0.055 ml |
0.277 ml |
0.553 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。 |