440202

LY 294002

≥98% (HPLC), solid, PI3K inhibitor, Calbiochem^®

• Sinonimo/i: LY 294002, 2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one, BRD2 Inhibitor IV, BRD3 Inhibitor III, BRD4 Inhibitor IV
• Formula empirica (notazione di Hill): C₁₉H₁₇NO₃
• Numero CAS: 154447-36-6
• Peso molecolare: 307.34
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• product name: 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.
• Livello qualitativo: 100
• Saggio: ≥98% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: off-white
• Solubilità: DMSO: 20 mg/mL; ethanol: soluble
• Condizioni di spedizione: ambient
• Temperatura di conservazione: −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; CZQHHVNHHHRRDU-UHFFFAOYSA-N

Descrizione

Descrizione generale

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).

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
Phosphatidylinositol 3-kinase

Product competes with ATP.

Reversible: yes

Target IC₅₀: 1.4 µM against phosphatidylinositol 3-kinase

Attenzione

Toxicity: Standard Handling (A)

Nota sulla preparazione

Slight warming may be required to achieve complete solubilization.

Ricostituzione

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

Altre note

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.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 2
• Punto d’infiammabilità (°F): 487.4 °F
• Punto d’infiammabilità (°C): 253.0 °C