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- PI3K (Phosphoinositide 3-kinase)
- LY 294002
LY 294002
LY294002 是一种广谱 PI3K 抑制剂，抑制 PI3Kα, PI3Kδ 和 PI3Kβ 的 IC50 分别为 0.5, 0.57, 0.97 μM。LY294002 也可抑制 CK2 的活性，IC50 为 98 nM。LY294002 是一种竞争性 DNA-PK 抑制剂，可逆结合 DNA-PK 的激酶结构域，IC50 为 1.4 μM。LY294002 是一种凋亡 (apoptosis) 激活剂。
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包装价格促销价数量
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5mg￥563.00350.00- +
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10mg￥700.00450.00- +
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50mg￥1250.00850.00- +
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100mg￥1500.001200.00- +
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500mg￥5000.004000.00- +
- 货号: ajci15212
- CAS: 154447-36-6
- 别名: LY294002/PI3K抑制剂
- 分子式: C19H17NO3
- 分子量: 307.34
- 纯度: ＞98%
- 溶解度: ≥40.37mg/mL in DMSO, ≥13.55mg/mL in EtOH
- 储存: Store at -20°C
- 库存: 现货
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]
参考文献:
[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.
