切换导航

LY 294002

现货
Catalog No.
A8250
PI3K抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
10mg
¥ 900.00
现货
50mg
¥ 2,100.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

LY294002 is a potent inhibitor of class I phosphoinositide 3-kinases (PI3Ks) [1, 2]. It is cell permeable and reversible, and selective against p110α, p110β, p110γ and p110δ, which acts on ATP binding site of the catalytic subunit.

PI3K family is divided into 3 classes: class I, II and III. LY294002 can inhibit 3 out of 4 isoforms of catalytic subunit of class I group. The IC50s for p110α, β andδ are 500 nM, 973 nM and 570 nM [3]. Even though it is less potent than wortmannin, other PI3K inhibitor, but it is more stable in solution. In addition, LY294002 is a reversible inhibitor whereas wortmannin acts irreversibly. [2]

PI3Ks signal through Akt, activates mTOR and inhibits Bad, leading to cell growth and proliferation. LY294002 potently inactivates PI3K class I catalytic subunit, resulting in induction of apoptosis and suppression of tumor cell growth in vitro and in vivo. [2, 4]

LY294002 is also a potent autophagy inhibitor by blocking autophagosome formation. [5]

Quantitative chemoproteomic profiling shows that LY294002 inhibits the BET bromodomain proteins BRD2, BRD3, and BRD4 with IC50 value of 1-2 µM. [6]

References:
[1]Maira et al. (2009). PI3K inhibitors for cancer treatment: where do we stand?. doi:10.1042/BST0370265.
[2]Vlahos CJ., et al. (1994). A Specific Inhibitor of Phosphatidylinositol 3-Kinase, 2-(4-Morpholinyl)-8-phenyl-4H-l-benzopyran-4-one (LY294002). Journal of Biological Chemistry 269 (7): 5241–5248.
[3]Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J, 2007, 404(3), 449-58.
[4]Hu L, et al. In vivo and in vitro ovarian carcinoma growth inhibition by a phosphatidylinositol 3-kinase inhibitor (LY294002). Clin Cancer Res, 2000, 6(3), 880-6.
[5]Blommaart EF., et al., (1997). The phosphatidylinositol 3-kinase inhibitors wortmannin and LY294002 inhibit autophagy in isolated rat hepatocytes. Eur. J. Biochem. 243: 240–246.
[6]Dittmann, A., et al. (2013). The Commonly Used PI3-Kinase Probe LY294002 is an Inhibitor of BET Bromodomains. ACS Chemical Biology: 131210150813004.

文献引用

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt307.34
Cas No.154447-36-6
FormulaC19H17NO3
Solubility≥15.37mg/mL in DMSO, ≥13.55mg/mL in EtOH, <2.22 mg/mL in H2O
Chemical Name2-morpholin-4-yl-8-phenylchromen-4-one
SDFDownload SDF
Canonical SMILESC1COCCN1C2=CC(=O)C3=C(O2)C(=CC=C3)C4=CC=CC=C4
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

OVCAR-3细胞

溶解方法

在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

10 μM,24 h

应用

与对照组相比,在24小时处理后,1、5和10 μM LY294002处理孔中细胞数量分别减少了27、56和75%。LY294002(1–10 μM)显著抑制细胞增殖。细胞用10 μM LY294002处理24小时后具有细胞毒性效应,细胞数量减少、细胞簇出现萎缩,细胞内聚力降低;细胞出现深染和固缩核,细胞质减少。在5 μM浓度时,LY294002诱导核固缩,减少胞浆量。

动物实验[1]:

动物模型

植入OVCAR-3细胞的无胸腺免疫缺陷小鼠

剂量

100 mg/kg/day,3周;腹腔注射

应用

在治疗组和对照组中,尸检时发现肿瘤位于腹膜、肠和子宫的表面。然而,在对照组中,还发现肿瘤位于隔膜和肝门区。在肿瘤细胞中,LY294002诱导核固缩,减少胞浆量,一些核从细胞质中分离。与LY294002处理组(6.35 ± 0.42 cm)相比,对照组中小鼠腹围显著增加(7.2 ± 2 cm)。在接种后第一周,两组体重均增加。在对照组中,体重持续增加,而LY294002处理后体重没有显著变化。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Hu L, Zaloudek C, Mills G B, et al. In vivo and in vitro ovarian carcinoma growth inhibition by a phosphatidylinositol 3-kinase inhibitor (LY294002). Clinical Cancer Research, 2000, 6(3): 880-886.

生物活性

描述 LY294002是PI3Kα/δ/β的抑制剂,IC50值分别为0.5 μM/0.57 μM/0.97 μM。
靶点 p110α p110δ p110β      
IC50 0.5 μM 0.57 μM 0.97 μM      

质量控制

化学结构

LY 294002

相关生物数据

LY 294002

相关生物数据

LY 294002

相关生物数据

LY 294002

相关生物数据

LY 294002

相关生物数据

LY 294002

相关生物数据

LY 294002

相关生物数据

LY 294002