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PI5P4Ks-IN-2

CAS No.: 2766854-03-7

PI5P4Ks-IN-2 is an inhibitor of the phosphatidylinositol 5-phosphate 4-kinase PI5P4Kγ. Targeting the PI5P4K isoforms, P
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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.