Biochem/physiol Actions

Target IC₅₀: 1.4 µM against phosphatidylinositol 3-kinase

Reversible: yes

Product competes with ATP.

Cell permeable: yes

Primary TargetPhosphatidylinositol 3-kinase

General description

A cell-permeable, potent, reversible and specific phosphatidylinositol 3-kinase inhibitor (IC₅₀ = 1.4 µM) that acts on the ATP-binding site of the enzyme. Also inhibits nonhomologous DNA end-joining (NHEJ) activity of the 460 kDa phosphatidylinositol 3-like kinase DNA-PKc_s, which is the catalytic subunit of DNA-activated protein kinase. Does not affect the activities of EGF receptor kinase, MAP kinase, PKC, Pl 4-kinase, S6 kinase, and c-Src even at 50 µM. Promotes the nuclear accumulation of active GSK-3b. Reported to suppress the proliferation of murine embryonic stem cells. Blocks the proliferation of cultured rabbit aortic smooth muscle cells without inducing apoptosis. Shown to bind to the same site as I-BET (Cat. No. 40101050 ~ 10 µM). A 10 mM (1 mg/325 µl) solution of LY 294002 (Cat. No. 440204) in DMSO is also available.

A cell-permeable, potent, reversible, and specific phosphatidylinositol 3-kinase (PI 3-kinase) inhibitor that acts on the ATP-binding site of the enzyme (IC₅₀ = 1.4 µM). Also inhibits nonhomologous DNA end-joining (NHED) in the 460 kDa phosphatidylinositol 3-like kinase DNA-PK_cs, which is the catalytic subunit of DNA-activated protein kinase. Does not affect the activity of EGF receptor kinase, MAP kinase, PKC, PI 4-kinase, S6 kinase, and c-src at 50 µM. Promotes the nuclear accumulation of active GSK-3b. Reported to suppress the proliferation of murine embryonic stem cells. Blocks the proliferation of cultured rabbit aortic smooth muscle cells without inducing apoptosis. Reported to inhibit histamine secretion in RBL-2H3 cells (IC₅₀ = 5 µM).

Legal Information

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

Other Notes

Dittman, A., et al. 2013. ACS Chem. Biol.9, 495.Bechard, M., and Dalton. S. 2009. Mol. Cell. Biol.29, 2092.Lianguzova, M.S. et al. 2007. Cell Biol. Int.31, 330.Baumann, P., and West, S.C. 1998. Proc. Natl. Acad. Sci. USA 95, 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 CitationsLee, J., et al. 2009. Cell Stem Cell5, 76.

Packaging

5, 10, 25 mg in Plastic ampoule

Preparation Note

Slight warming may be required to achieve complete solubilization.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)