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Submit ReviewPI 828
Description: PI 3-kinase inhibitor, more potent than LY 294002 (Cat. No. 1130)
Chemical Name: 2-(4-Morpholinyl)-8-(4-aminopheny)l-4H-1-benzopyran-4-one
Purity: ≥99% (HPLC)
Biological Activity
PI 3-Kinase inhibitor (IC50 values are 0.098, 0.183, 0.227 and 1.967 μM for p110β, p110α, p110δ and p110γ respectively) that displays higher potency than LY 294002 (Cat No. 1130). Can be immobilized onto a solid phase.
Compound Libraries
PI 828 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 322.36 |
| Formula | C19H18N2O3 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 942289-87-4 |
| PubChem ID | 25181195 |
| InChI Key | WUKMIBOGGXMBAC-UHFFFAOYSA-N |
| Smiles | O=C2C=C(N3CCOCC3)OC1=C(C4=CC=C(N)C=C4)C=CC=C12 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 32.24 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 322.36. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.1 mL | 15.51 mL | 31.02 mL |
| 5 mM | 0.62 mL | 3.1 mL | 6.2 mL |
| 10 mM | 0.31 mL | 1.55 mL | 3.1 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.62 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Gharbi et al (2007) Exploring the specificity of the PI3K family inhibitor LY294002. Biochem.J. 404 15 PMID: 17302559
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Keywords: PI 828, PI 828 supplier, PI, 3-kinase, inhibitors, inhibits, potent, LY, 294002, PI3K, Phosphoinositide, 3-Kinases, PI828, 3-Kinase, Inositol, Lipids, 2814, Tocris Bioscience
5 Citations for PI 828
Citations are publications that use Tocris products. Selected citations for PI 828 include:
Moser et al (2014) Functional kinomics identifies candidate therapeutic targets in head and neck cancer. Clin Cancer Res 20 4274 PMID: 25125259
Liddell et al (2016) Pyrrolidine dithiocarbamate activates the Nrf2 pathway in astrocytes. J Neuroinflammation 13 49 PMID: 26920699
Grassin-Delyle et al (2013) The expression and relaxant effect of bitter taste receptors in human bronchi. Respir Res 14 134 PMID: 24266887
Rogers and Gahring (2015) Upregulation of Nicotinic Acetylcholine Receptor α4+β2 through a Ligand-Independent PI3Kβ Mechanism That Is Enhanced by TNFα and the Jak2/p38Mapk Pathways. J Neurosci 10 e0143319 PMID: 26619345
Li et al (2011) TRPV4-mediated calcium influx into human bronchial epithelia upon exposure to diesel exhaust particles. Environ Health Perspect 119 784 PMID: 21245013
Do you know of a great paper that uses PI 828 from Tocris? Please let us know.
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