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440202

Sigma-Aldrich

LY 294002

LY294002, CAS 154447-36-6, is a cell-permeable, potent, reversible, and specific inhibitor of PI 3-kinase ((IC₅₀ = 1.4 µM). Acts on the ATP-binding site.

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Synonym(s):
LY 294002, 2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one, BRD2 Inhibitor IV, BRD3 Inhibitor III, BRD4 Inhibitor IV
Empirical Formula (Hill Notation):
C19H17NO3
CAS Number:
Molecular Weight:
307.34

Quality Level

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 20 mg/mL
ethanol: soluble

shipped in

ambient

storage temp.

−20°C

InChI

1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2

InChI key

CZQHHVNHHHRRDU-UHFFFAOYSA-N

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This Item
440204124011218860
vibrant-m

440202

LY 294002

vibrant-m

440204

LY 294002

vibrant-m

124011

Akt Inhibitor IV

vibrant-m

218860

Casein Kinase II Inhibitor VIII

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥99% (HPLC)

form

solid

form

liquid

form

solid

form

solid

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

storage condition

OK to freeze, protect from light

shipped in

ambient

shipped in

wet ice

shipped in

ambient

shipped in

wet ice

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-PKcs, 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-PKcs, 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).

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

Warning

Toxicity: Standard Handling (A)

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.

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


Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 2

flash_point_f

487.4 °F

flash_point_c

253.0 °C


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