PI 3-Kα Inhibitor IV is a cell-permeable morpholino-thienopyrimidine compound that acts as a potent and isoform-selective inhibitor of the PI 3-kinase family (IC50 = 2 nM, 16 nM, 660 nM, and 220 nM for PI 3-kinase p110 α (p110α), PI 3-kinase p110 β (p110β), p110γ, and PI 3-K C2β, respectively) and inhibits non-PI 3-kinase targets only at much higher concentrations (IC50 ≥3.4 μM for Cdk2/E, KDR, PKA, and PKCα). PI 3-Kα Inhibitor IV has been shown to inhibit cell proliferation (IC50 = 580 nM) and serum-stimulated Akt phosphorylation (IC50 <3 μM) in A375 melanoma cells.
1. Hayakawa, M., et al. 2006. Bioorg. Med. Chem. 14: 6847-6858. PMID: 16837202
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