- 提示:详情请下载说明书。
- 产品描述: M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM
- 靶点: Pim
- 体外研究:
M-110 (0.01-10 μM; 72 hours) inhibiting the growth of DU-145 cells with an IC50 value of 0.9 μM. M-110 has no activity on normal human peripheral blood mononuclear cells up to 40 μM. M-110 (10 μM; 18 hours) inhibits STAT3 Tyr705 phosphorylation. M-110 inhibits the expression of active STAT3 through inhibition of PIM-3. M-110 also inhibits the proliferation of 22Rv1, PC3, and SW480 cells, with IC50 values of 0.6 to 0.8 μM. Cell Viability Assay Cell Line: DU-145 cells Concentration: 0.01, 0.1, 1, 10 μM Incubation Time: 72 hours Result: Inhibiting the growth of DU-145 cells with an IC50 value of 0.9 μM. Western Blot Analysis Cell Line: DU-145 cells Concentration: 10 μM Incubation Time: 18 hours Result: Reduced the expression of p-STAT3 Tyr705 to 23.5%, compared with untreated cells without affecting the expression of STAT3.
- 参考文献:
1. Chang M, et al.PIM kinase inhibitors downregulate STAT3(Tyr705) phosphorylation.Mol Cancer Ther. 2010 Sep;9(9):2478-87. 2. He Y, et al. Schisantherin A suppresses osteoclast formation and wear particle-induced osteolysis via modulating RANKL signaling pathways. Biochem Biophys Res Commun. 2014 Jul 4;449(3):344-50. 3. Zhou E, et al. Schisantherin A protects lipopolysaccharide-induced acute respiratory distress syndrome in mice through inhibiting NF-κB and MAPKs signaling pathways. Int Immunopharmacol. 2014 Sep;22(1):133-40. 4. Sa F, et al. Discovery of novel anti-parkinsonian effect of schisantherin A in in vitro and in vivo. Neurosci Lett. 2015 Apr 23;593:7-12. 5. Zhang LQ, et al. Schisantherin A protects against 6-OHDA-induced dopaminergic neuron damage in zebrafish and cytotoxicity in SH-SY5Y cells through the ROS/NO and AKT/GSK3β pathways. J Ethnopharmacol. 2015 Apr 29. pii: S0378-8741(15)00306-2.
- 溶解性: soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.242 ml 11.212 ml 22.424 ml 5 mM 0.448 ml 2.242 ml 4.485 ml 10 mM 0.224 ml 1.121 ml 2.242 ml 50 mM 0.045 ml 0.224 ml 0.448 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。
输入产品批号:
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)