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PI828
- Development stage
- Unknown
- Lead developer
- Roche
- Modality
- Small Molecules
- Administration
- Intraperitoneal, Intrathecal, Intravenous
01
Overview
PI828 (also known as PI-828) is a small molecule phosphoinositide 3-kinase (PI3K) inhibitor originally synthesized by Piramed (later acquired by Roche). It is a structural analogue of the widely used PI3K inhibitor LY294002, modified with an aminophenyl group to allow for immobilization or conjugation. PI828 acts as a dual inhibitor of class I PI3K isoforms (with preference for PI3Kβ and PI3Kα) and casein kinase 2 (CK2). It is primarily utilized as a research tool to study PI3K/Akt signaling pathways, respiratory motor plasticity, and the development of targeted supramolecular nanoparticles for cancer therapy.
- Other names
- 2-(4-morpholinyl)-8-(4-aminophenyl)-4H-1-benzopyran-4-one8-(4-aminophenyl)-2-morpholin-4-ylchromen-4-one
02
Targets
BRD4 (Bromodomain-containing protein 4)mTOR (Mammalian target of rapamycin kinase)CK2 (Casein kinase II subunit alpha)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)H (Histamine receptors)PIK3CA (Phosphoinositide 3-kinase alpha)GSK3 (Glycogen synthase kinase 3 beta)ALDH1A1 (Aldehyde dehydrogenase 1 family member A1)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)mAChR (Muscarinic acetylcholine receptors)5-HT (Serotonin receptors)PIK3CD (Phosphatidylinositol 3-kinase delta)
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