440202

LY 294002

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

• 동의어(들): LY 294002, 2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one, BRD2 Inhibitor IV, BRD3 Inhibitor III, BRD4 Inhibitor IV
• 실험식(Hill 표기법): C₁₉H₁₇NO₃
• CAS Number: 154447-36-6
• Molecular Weight: 307.34
• MDL number: MFCD00270881
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• 제품명: 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.
• Quality Level: 100
• 분석: ≥98% (HPLC)
• 양식: solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: off-white
• solubility: DMSO: 20 mg/mL; ethanol: soluble
• 배송 상태: ambient
• 저장 온도: −20°C
• SMILES string: N4(CCOCC4)c1[o]c2c([c](c1)=O)cccc2c3ccccc3
• 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

설명

일반 설명

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).

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
Phosphatidylinositol 3-kinase

Product competes with ATP.

Reversible: yes

Target IC₅₀: 1.4 µM against phosphatidylinositol 3-kinase

경고

Toxicity: Standard Handling (A)

제조 메모

Slight warming may be required to achieve complete solubilization.

재구성

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

기타 정보

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.

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point (°F): 487.4 °F
• Flash Point (°C): 253.0 °C