S85536 |
TCS PIM-1 1 |
| 源叶(MedMol) | 97% |
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- 产品描述： TCS PIM-1 1 (SC 204330) is a potent, selective and ATP-competitive Pim-1 kianse inhibitor with an IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2 (IC50s >20000 nM)
- 靶点： PIM1:50 nM (IC50)
- 体外研究： TCS PIM-1 1 (compound 1), a substituted pyridone scaffold, binds convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism. Preliminary data further suggests that TCS PIM-1 1 lacked in vitro inhibitory activity toward related serine/threonine kinases Pim-2 and MEK1/2. Hence, small molecules similar to TCS PIM-1 1 may serve as useful starting scaffolds for the development of other improved yet selective Pim-1 inhibitors. TCS PIM-1 1 serves both as a starting point for SAR chemical syntheses and was used for co-crystallization with Pim-1 protein
- 参考文献：
1. Cheney IW, et al. Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1679-83.
- 溶解性： soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 2.723 ml 13.617 ml 27.233 ml 5 mM 0.545 ml 2.723 ml 5.447 ml 10 mM 0.272 ml 1.362 ml 2.723 ml 50 mM 0.054 ml 0.272 ml 0.545 ml
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