Western blot analysis of extracts from Jurkat cells, untreated or treated with ZSTK474 (24 hr) at the indicated concentrations, using Phospho-Akt (Ser473) (D9E) XP® Rabbit mAb #4060 (upper) or Akt (pan) (C67E7) Rabbit mAb #4691 (lower).Learn more about how we get our images
Chemical Structure of ZSTK474.Learn more about how we get our images
ZSTK474 is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 5 mg in 1.20 ml DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used at 0.01 - 10 μM for 2-24 hours.
Store lyophilized or in solution at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
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 IC50 values of 16, 44, 4.6 and 49 nM, respectively. ZSTK474 demonstrates increased potency of PI3K inhibition over LY294002 (Average IC50 = 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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