Cell Signaling Technology

Product Pathways - PI3K / Akt Signaling

ZSTK474 #13213

474   LY294002   matrix metalloproteinase   MMP   Pi3   PI3K   VEGF   ZSTK  

Applications Dilution Species-Reactivity Sensitivity MW (kDa) Isotype

Species cross-reactivity is determined by western blot.

Applications Key:

Description

Molecular Weight:

417.41 g/mol

Molecular Characterization

C19H21F2N7O2

Purity

>99%

Bioactivity

Solubility: Soluble in DMSO at 20 mg/ml and soluble in ethanol at 2.5 mg/ml with warming. Very poorly soluble in water.

Structure

Structure

Chemical Structure of ZSTK474.

Western Blotting

Western Blotting

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).

Directions for Use

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.

Background

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).

Application References

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Companion Products


For Research Use Only. Not For Use In Diagnostic Procedures.

Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.

XP is a registered trademark of Cell Signaling Technology, Inc.

Cell Signaling Technology® is a trademark of Cell Signaling Technology, Inc.

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