LY 294002，1MG，440204-1MGCN，Sigma

General description

Cell permeable: Yes

Primary Target: phosphatidylinositol 3-kinase
Product competes with ATP.
Reversible: Yes
Target IC50: 1.4 µM against phosphatidylinositol3-kinase
LY294002 is a chemical compound known for its potentinhibitory effects on a variety of proteins, particularly as a strong inhibitorof phosphoinositide 3-kinases (PI3Ks). While it is frequently utilized in research related to the PI3K/AKT signaling pathway, LY294002 is generallyregarded as a non-selective tool for investigating PI3K functions. This flavonoid derivative acts as a competitive andreversible inhibitor of the ATP binding site of PI3K, exhibiting an IC50 approximately 500-fold higher than that of wortmannin, at 1.4 μM. LY294002 doesnot inhibit several ATP-dependent enzymes, including PI4K, EGF receptor tyrosinekinase, c-src, MAP kinase, S6 kinase, diacylglycerol kinase, protein kinase A, protein kinase C, and ATPase. It acts as an antagonist of the aryl hydrocarbonreceptor (AHR), a ligand-activated transcription factor. By binding to AHR, LY294002 inhibits transcriptional activation, thereby preventing gene expression.

Application

LY294002 has been used as a phosphatidylinositol3-kinase (PI3K) inhibitor:

• to induce viral reactivation in a model ofherpes simplex virus type 1 (HSV-1) latency
• to investigate its effects on transforminggrowth factor (TGF)-β1-induced differentiation of cat corneal fibroblasts
• to investigate its role in the insulin-like growthfactor I (IGF-1) signaling pathway and on the phosphorylation of glycogensynthase kinase-3β (GSK-3β)

Biochem/physiol Actions

Cell permeable: yes
Primary Target
phosphatidylinositol 3-kinase
Product competes with ATP.
Reversible: yes
Target IC₅₀: 1.4 µM against phosphatidylinositol 3-kinase

Packaging

Packaged under inert gas

Physical form

A 10 mM (1 mg/325 µl) solution of LY 294002 (Cat. No. 440202) in DMSO.

Preparation Note

Following initial thaw, aliquot and freeze (-20°C).

Other Notes

Dittman, A., et al. 2013. ACS Chem. Biol.9, 495.
Baumann, P., and West, S.C. 1998. Proc. Natl. Acad. Sci. USA95, 14066.
Cardone, M.H., et al. 1998. Science282, 1318.
Vlahos, C.J., et al. 1995. J. Immunol.154, 2413.
Yano, H., et al. 1995. Biochem. J.312, 145.
Vlahos, C.J., et al. 1994. J. Biol. Chem.269, 5241.



Selected Citations
Lee, J., et al. 2009. Cell Stem Cell5, 76.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Irritant (B)