PI3K-IN-37

PI3K-IN-37 (Example 84.1) is a PI3K α/β/δ inhibitor with IC50s of 6, 8, 4 nM, respectively. PI3K-IN-37 can also inhibit mTOR (IC50=4 nM)[1].

Signaling Pathways >> PI3K/Akt/mTOR >> mTOR

Research Areas >> Others

Signaling Pathways >> PI3K/Akt/mTOR >> PI3K

PI3Kα:6 nM (IC50)

PI3Kβ:8 nM (IC50)

PI3Kδ:4 nM (IC50)

mTOR:4 nM (IC50)

PI3K-IN-37 (0.005-10 μM; 30 min) treatment inhibits PKB Ser473 phosphorylation in Rat1 cells[1]. PI3K-IN-37 (0.005-1 μM; 60 min) treatment inhibits S6 Ribosomal Protein phosphorylation Ser235/236 in TSC1 nult MEF cells[1]. Cell Viability Assay[1] Cell Line: Rat1 cells Concentration: 0.005-10 μM Incubation Time: 30 min Result: Inhibited Pl3-kinase isoforms alpha, beta or delta phosphorylation with the IC50s of <5 nM, 8 nM, and 18 nM, respectively. Cell Viability Assay[1] Cell Line: TSC1-/- MEF cells Concentration: 0.005-1 μM Incubation Time: 60 min Result: Inhibited S6 Ribosomal Protein phosphorylation (IC50=2 nM).

[1]. FURET Pascal, et al. 1H-IMIDAZO[4,5-c]QUINOLINONE DERIVATIVES. WO2010139731A1.