| Description | PI-828 is a phosphatidylinositol 3-kinase (PI3K) inhibitor, which is widely used to study the physiological function of PI3K and also promotes stem cell differentiation into mesoderm. |
| In vitro | PI-828 (0.78-3.12 µM; 48 hours) reduces caspase 3 activation. However, higher concentrations of PI-828 (6.25-12.5 μM) alone causes apoptosis[2].The sensitivity to PI-828 is a key feature of PI3K-C2β that shows a different sensitivity to this inhibitor compared to class I PI3Ks. Of note, 1 μM PI-828 has no effect on the activity of PI3K-C2β, while it significantly inhibits class I PI3Ks. In particular, a concentration of 10 μM PI-828 completely blocks class I PI3Ks, whereas it has only a partial inhibitory effect on PI3K-C2β[4] |
| Target activity | CK2:149 nM, p110α:173 nM, CK2α2:1.127 μM |
| Synonyms | LY 294002, 4gamma-NH2 |
| molecular weight | 322.36 |
| Molecular formula | C19H18N2O3 |
| CAS | 942289-87-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 11.2 mg/mL (34.9 mM) |
| References | 1. Gharbi SI, et al. Exploring the specificity of the PI3K family inhibitor LY294002. Biochem J. 2007 May 15;404(1):15-21. 2. Kulkarni AA, et al. Supramolecular nanoparticles that target phosphoinositide-3-kinase overcome insulin resistance and exert pronounced antitumor efficacy. Cancer Res. 2013 Dec 1;73(23):6987-97. 3. McLean AB, et al. Activin a efficiently specifies definitive endoderm from human embryonic stem cells only when phosphatidylinositol 3-kinase signaling is suppressed. Stem Cells. 2007 Jan;25(1):29-38. 4. Falasca M, Maffucci T. Emerging roles of phosphatidylinositol 3-monophosphate as a dynamic lipid second messenger. Arch Physiol Biochem. 2006 Oct-Dec;112(4-5):274-84. |