491871-58-0
TCS PIM-1 1
CAS: 491871-58-0
Molecular Formula: C18H11BrN2O2
491871-58-0 - Names and Identifiers
491871-58-0 - Physico-chemical Properties
| Molecular Formula | C18H11BrN2O2 |
| Molar Mass | 367.2 |
| Density | 1.63±0.1 g/cm3(Predicted) |
| Boling Point | 592.6±50.0 °C(Predicted) |
| Solubility | DMSO: ≥ 52 mg/mL |
| pKa | 6.93±0.10(Predicted) |
| Storage Condition | Store at +4°C |
| In vitro study | 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. |
491871-58-0 - Preparation solution concentration reference
| 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 |
| 5 mM | 0.054 ml | 0.272 ml | 0.545 ml |
Last Update：2024-01-02 23:10:35
491871-58-0 - Reference Information
| biological activity | TCS PIM-1 1 (SC 204330) is an effective and selective ATP-competitive Pim-1 kianse inhibitor with an IC50 value of 50 nM and good selectivity for Pim-2 and MEK1/MEK2 (IC50> 20000 nM). |
| target | TargetValue Pim1 (Cell-free say) 50 nM |
| Target | Value |
| Pim1 (Cell-free assay) | 50 nM |
| in vitro study | 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. |
Last Update：2024-04-09 21:04:16
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