440202
LY 294002
≥98% (HPLC), solid, PI3K inhibitor, Calbiochem®
别名:
LY 294002
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关于此项目
经验公式（希尔记法）:
C19H17NO3
化学文摘社编号:
分子量:
307.34
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
产品名称
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
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
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
General description
一种可渗透细胞的，强效的，可逆的和特异性磷脂酰肌醇3-激酶（PI 3-激酶）抑制剂，可作用于酶的ATP结合位点（IC50 = 1.4 µ M）。还抑制460 kDa磷脂酰肌醇3样激酶DNA-PKcs中的非同源DNA末端连接（NHED），DNA-PKcs是DNA激活的蛋白激酶的催化亚基。在50 µM时不影响EGF受体激酶，MAP激酶，PKC，PI 4-激酶，S6激酶和c-src的活性。促进活性GSK-3b的核积累。据报告可抑制鼠胚胎干细胞的增殖。阻断培养的兔主动脉平滑肌细胞增殖，而不诱导凋亡。据报告可抑制RBL-2H3细胞中的组胺分泌（IC50 = 5 µM）。
一种细胞可渗透的、强效的、可逆的和特异性磷脂酰肌醇3-激酶抑制剂（IC50 = 1.4 µM），作用于酶的ATP结合位点。还抑制460 kDa磷脂酰肌醇3样激酶DNA-PKcs的非同源DNA末端连接（NHEJ）活性，DNA-PKcs是DNA激活的蛋白激酶的催化亚基。即使在50 µM时也不影响EGF受体激酶，MAP激酶，PKC，PI 4-激酶，S6激酶和c-Src的活性。促进活性GSK-3b的核积累。据报告可抑制鼠胚胎干细胞的增殖。阻断培养的兔主动脉平滑肌细胞增殖，而不诱导凋亡。显示与I-BET（目录号40101050 ~ 10 µM）结合在同一位点。也可购买10 mM（1 mg/325 µl）LY 294002（目录号440204） DMSO溶液。
Biochem/physiol Actions
主要靶标
磷脂酰肌醇3-激酶
磷脂酰肌醇3-激酶
产物与ATP竞争。
可逆性：是
细胞可渗透性：具有
靶标IC50：磷脂酰肌醇3-激酶为1.4 µM
Preparation Note
复溶后，等分并冷冻保存（-20°C）。贮备液在-20°C下可稳定保存至多6个月。
实现完全溶解可能需要轻微加热。
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.
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
Disclaimer
毒性：标准处理（A）
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存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
487.4 °F
flash_point_c
253.0 °C
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全球贸易项目编号
| 货号 | GTIN |
|---|---|
| 440202-5MG | 07790788050290 |
| 440202-10MG | 04055977186666 |
| 440202-25MG | 04055977186673 |