| 产品描述： | SMI-4a (TCS-PIM-1-4a) is a pan-Pim kinases inhibitor that blocks mTORC1 activity via activation of AMPK. SMI-4a kills a wide range of both myeloid and lymphoid cell lines (IC50 values ranging from 0.8 μM to 40 μM) |
| 靶点： |
Pim;Apoptosis;Pim |
| 体外研究： |
SMI-4a（10 μM；24-48 小时；6812/2 细胞和 Jurkat 细胞）使 6812/2 细胞和 Jurkat 的 G1 期细胞数量从 44.3% 增加到 68.4%，从 56.2% 增加到 67.1%。 在 6812/2 细胞中S 期细胞减少，而在 Jurkat 细胞中仅观察到与较小的 G1 阻滞一致的微小变化。 SMI-4a（5 μM；6 小时；6812/2 细胞和 Jurkat 细胞）通过诱导细胞凋亡诱导细胞死亡。 SMI-4a（5 μM；4-8 小时；6812/2 细胞和 Jurkat 细胞）可防止 4E-BP1 蛋白水平升高并抑制 Thr37/46 上 mTOR 定向磷酸化。 Cell Cycle Analysis Cell Line: 6812/2 cells and Jurkat cells Concentration: 10 μM Incubation Time: 24 hours, 48 hours Result: Induced cell-cycle arrest. Apoptosis Analysis Cell Line: 6812/2 cells and Jurkat cells Concentration: 5 μM Incubation Time: 6 hours Result: Led to an increase in the number of the cells positive for annexin V and negative for PI from 8.25% in the control to 21.85%. Western Blot Analysis Cell Line: 6812/2 cells and Jurkat cells Concentration: 10 μM Incubation Time: 4 hours, 8 hours Result: Prevented the increase in 4E-BP1 protein levels and inhibited mTOR-directed phosphorylation on Thr3 |
| 体内研究： |
SMI-4a (SMI-4a; 60 mg/kg; oral gavage; twice daily; for 21 days; nu/nu nude mice) treatment causes a significant delay in the tumor growth without any change in the weight, blood counts, or chemistries. Animal Model: 18 Nu/nu nude mice with 6812/2 murine pre–T-LBL cells Dosage: 60 mg/kg Administration: Oral gavage; twice daily; for 21 days Result: Caused a significant delay in the tumor growth. |
| 参考文献： |
1. Lin YW, Beharry ZM, Hill EG, et al. A small molecule inhibitor of Pim protein kinases blocks the growth of precursor T-cell lymphoblastic leukemia/lymphoma. Blood. 2010 ;115(4):824-33. 2. Beharry Z, Mahajan S, Zemskova M,et al. The Pim protein kinases regulate energy metabolism and cell growth. Proc Natl Acad Sci U S A. 2011;108(2):528-33. |
| 溶解性： |
Soluble in DMSO |
| 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 |
3.66 ml |
18.3 ml |
36.599 ml |
| 5 mM |
0.732 ml |
3.66 ml |
7.32 ml |
| 10 mM |
0.366 ml |
1.83 ml |
3.66 ml |
| 50 mM |
0.073 ml |
0.366 ml |
0.732 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