PI-103
PI3K, mTOR and DNA-PK inhibitor / A potent inhibitor of PI-3 kinase, mTOR and DNA-PK, IC50 = 8, 88, 150, 48, 20, 83 and 2 nM for p110α, p110ß, p110γ, p110δ, mTORC1, mTORC2 and DNA-PK respectively.1,2 Synergizes with arsenic disulfide to eradicate AML stem cells by induction of differentiation.3 Inhibits the growth of gefitinib-resistant non-small cell lung cancer cell lines.4 Induces autophagy in drug-resistant glioma.5 Protects against a-synuclein-induced toxicity in human neurons by induction of macroautophagy.6
Biochemicals & reagents
371935-74-9
1) Knight et al. (2006), A Phamacological map of the PI3-K family defines a role for p110alpha in insulin signaling; Cell, 125 733 2) Raynaud et al. (2007), Pharmacologic characterization of a potent inhibitor of a class I phosphatidylinositide 3-kinases; Cancer Res., 67 5840 3) Hong et al. (2011), Arsenic disulfide synergizes with the phosphoinositide 3-kinase inhibitor PI-103 to eradicate acute myeloid leukemia stem cells by inducing differentiation; Carcinogenesis, 32 1550 4) Zou et al. (2009), A ovel dual PI3Kalpha/mTOR inhibitor PI-103 with high antitumor activity in non-small cell lung cancer cells; Int. J. Mol. Med. 24 97 5) Fan et al. (2010), Akt and autophagy cooperate to promote survival of drug-resistant glioma; Sci. Signal., 3 ra81 6) Hollerhage et al. (2019), Multiple molecular pathways stimulating macroautophagy protect from alpha-synuclein-induced toxicity in human neurons; Neuropharmacology, 149 13
-20°C
TARGET: Kinase; DNA -- PATHWAY: Autophagy; PI3K; mTOR; DNA repair -- RESEARCH AREA: Neuroscience; Cell death; Cancer stem cells -- DISEASE AREA: Neurodegeneration; Cancer