| Description |
ZSTK474 is a pan PI3K inhibitor that acts through ATP-competition by binding at the ATP-binding pocket of PI3Kγ (1,2). ZSTK474 inhibits PI3K isoforms α, β, δ, and γ with IC 50 values of 16, 44, 4.6 and 49 nM, respectively. ZSTK474 demonstrates increased potency of PI3K inhibition over LY294002 (Average IC 50 = 1.4 μM) as well as decreased observable toxicity. It has also been shown that ZSTK474 is a weak mTOR inhibitor, demonstrating increased specificity over other PI3K inhibitors, including LY294002 (3). Research studies show that ZSTK474 inhibits cell proliferation by arresting cells in G1 phase (2). By blocking vascular endothelial growth factor (VEGF) and matrix metalloproteinase (MMP) secretion, ZSTK474 is able to inhibit cell migration, invasion, and adhesion (4).
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