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Merck
CN

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:
154447-36-6
分子量:
307.34
MDL编号:
MFCD00270881
UNSPSC代码:
12352200
NACRES:
NA.77

主要文件

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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.

质量水平

100

方案

≥98% (HPLC)

表单

solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

off-white

溶解性

DMSO: 20 mg/mL
ethanol: soluble

运输

ambient

储存温度

−20°C

SMILES字符串

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

相关类别

一般描述

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。

生化/生理作用

主要靶标
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

制备说明

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。

其他说明

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.


法律信息

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

免责声明

毒性：标准处理（A）

储存分类代码

11 - Combustible Solids

WGK

WGK 2

闪点(°F)

487.4 °F

闪点(°C)

253.0 °C

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The multifunctional protein Y-box binding protein-1 (YB-1) regulates all the so far described cancer hallmarks including cell proliferation and survival. The MAPK/ERK and PI3K/Akt pathways are also the major pathways involved in cell growth, proliferation, and survival, and are the
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Kidney fibrosis is a highly deleterious process and a final manifestation of chronic kidney disease. Alpha-(α)-synuclein (SNCA) is an actin-binding neuronal protein with various functions within the brain; however, its role in other tissues is unknown. Here, we describe the
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Nuclear expression of Y-box-binding protein (YBX1) is closely correlated with clinical poor outcomes and drug resistance in breast cancer. Nuclear translocation of YBX1 is facilitated by YBX1 phosphorylation at serine 102 by AKT, p70S6K, and p90RSK, and the phosphorylated YBX1
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相关内容

An Introduction to Inhibitors and Their Biological Applications - 1st Edition

An Introduction to Inhibitors and Their Biological Applications

Bulk Product Guide
Human Kinome & InhibitorSelect™ Libraries

Human Kinome Poster: The InhibitorSelect™ Protein Kinase Inhibitor Libraries provide broad coverage of the human kinome as shown here. The depicted human kinome dendrogram of 518 kinases are classified into five broad groups, 90 families, and 145 subfamilies. Inhibitor coverage was assigned based upon published data related to potency (IC50, EC50, Kd, etc.) for individual kinases harvested from the literature. Colored dots denote which library contains an inhibitor with demonstrated potent activity against the designated kinase and do not necessarily reflect known specificity of the inhibitor. Coverage of lipid and atypical kinases are depicted as a separate dendrogram. As shown, Calbiochem® Protein Kinase Inhibitor Libraries cover all major kinase families including TK, CMGC, CAMK, AGC, CK1, STE, TKL, as well as Lipid or Atypical kinase families.

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