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LY294002

CAS No. : 154447-36-6

MCE 国际站：LY294002

产品活性：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。

研究领域：PI3K/Akt/mTOR  |  Stem Cell/Wnt  |  Cell Cycle/DNA Damage  |  Apoptosis  |  Autophagy

作用靶点：PI3K  |  Casein Kinase  |  DNA-PK  |  Apoptosis  |  Autophagy

In Vitro: LY294002 (0-75 μM; 24 hours and 48 hours) remarkably decreases human nasopharyngeal carcinoma CNE-2Z cells in a dose-dependent fashion.
LY294002 (0-75 μM; 24 hours and 48 hours ) induces CNE-2Z cells apoptosis rate in dose-dependent.
LY294002 (10-75 μM) significantly decreases p-Akt (S473) expression levels and up-regulates caspase-9 activity in CNE-2Z cells. Total Akt protein level is not difference with different concentration.
LY294002 (5, 10, 100 µM; for 2 hours) treatment partially suppresses Lysophosphatidic acid (LPA)-induced (20 µM; for 4 hours) nuclear translocation of YAP, accompanied by a reduction in p-AKT levels.

In Vivo: LY294002 (10, 25, 50, 75 mg/kg; i.p.; twice weekly; for 4 weeks) significantly reduces mean NPC tumor burden in a dose-dependent manner. LY294002 (10, 25 mg/kg) is less effective in decreasing tumor burden.
LY294002 (1.2 mg/kg per day; i.p.; for 14 days) prevents Leptin (60 ug/kg)-induced adverse effects on spermatozoa in Sprague-Dawley rats.

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