| Description | PI5P4Ks-IN-2 is an inhibitor of the phosphatidylinositol 5-phosphate 4-kinase PI5P4Kγ. Targeting the PI5P4K isoforms, PI5P4Ks-IN-2 inhibited PI5P4Kα, PI5P4Kβ, PI5P4Kγ, and PI5P4Kγ+, with IC50 values of <4.3, <4.6, 6.2, and 0.32, respectively. |
| In vitro | PI5P4Ks-IN-2(10 μM)对一组140种蛋白激酶和15种脂激酶显示出选择性,与PI5P4Kγ-WT(Ki=68 nM)或PI5P4Kβ(Ki >30,000 nM)结合。[1] |
| In vivo | PI5P4Ks-IN-2 (10 μM) 展现了对140种蛋白激酶和15种脂激酶的选择性,特别是与PI5P4Kγ-WT (Ki=68 nM) 或PI5P4Kβ (Ki >30,000 nM) 的结合。[1] |
| Target activity | PI5P4Kα:<4.3(pIC50), PI5P4Kβ:<4.6(pIC50), PI5P4Kγ:6.2(pIC50), PI5P4Kγ+:0.32(pIC50), PI5P4Kγ (WT):68 nM(Ki), PI5P4Kβ:>30 μM(Ki) |
| molecular weight | 357.45 |
| Molecular formula | C22H23N5 |
| CAS | 2766854-03-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 27.5 mg/mL (72.08 mM) |
| References | 1. Boffey HK, et al. Development of Selective Phosphatidylinositol 5-Phosphate 4-Kinase γ Inhibitors with a Non-ATP-competitive, Allosteric Binding Mode. J Med Chem. 2022;65(4):3359-3370. |