LY294002 hydrochloride 是一种有效的广谱PI3K抑制剂,对P110α,P110δ和P110β的IC50分别为 0.5, 0.57 和 0.97 μM。 IC50值分别为P110α、P110δ和P110β的0.5、0.57和0.97 μM。LY294002 hydrochloride 也能抑制CK2,其IC50为 98 nM。LY294002 hydrochloride 可用于胰腺癌研究。
生物活性 | LY294002 hydrochloride is a potent and broad-spectrumPI3Kinhibitor, withIC50values of 0.5, 0.57, and 0.97 μM forP110α,P110δandP110β, respectively. LY294002 hydrochloride also inhibitsCK2with anIC50of 98 nM. LY294002 hydrochloride can be used for pancreaticcancerresearch[1][2][3]. |
IC50& Target | CK2 0.098 μM (IC50) | CK2α2 3.869 μM (IC50) |
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体外研究 (In Vitro) | LY294002 hydrochloride (0-75 μM; 24 hours and 48 hours) remarkably decreases human nasopharyngeal carcinoma CNE-2Z cells in a dose-dependent fashion[4]. LY294002 hydrochloride (0-75 μM; 24 hours and 48 hours ) induces CNE-2Z cells apoptosis rate in dose-dependent[4]. LY294002 hydrochloride (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[4]. LY294002 hydrochloride (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[6].
Cell Proliferation Assay Cell Line: | CNE-2Z cells[4] | Concentration: | 0 μM, 10 μM, 25 μM, 50 μM, and 75 μM | Incubation Time: | 24 hours and 48 hours | Result: | Decreased CNE-2Z cells in a dose-dependent fashion. |
Apoptosis Analysis Cell Line: | CNE-2Z cells[4] | Concentration: | 0 μM, 10 μM, 25 μM, 50 μM, and 75 μM | Incubation Time: | 24 hours and 48 hours | Result: | Induced apoptosis rate in a dose-dependent manner. |
Western Blot Analysis Cell Line: | CNE-2Z cells[4] | Concentration: | 0 μM, 10 μM, 25 μM, 50 μM, and 75 μM | Incubation Time: | 24 hours and 48 hours | Result: | Decreased phosphorylated Akt (S473) expression levels were significantly, up-regulated caspase-9 activity in CNE-2Z cells in treated group. |
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体内研究 (In Vivo) | LY294002 hydrochloride (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[4]. LY294002 hydrochloride (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[5].
Animal Model: | Athymic nude mice (6-8 weeks) with CNE-2Z xenograft[4] | Dosage: | 10 mg/kg, 25 mg/kg, 50 mg/kg, and 75 mg/kg | Administration: | IP; twice weekly, for 4 weeks | Result: | Mean Nasopharyngeal carcinoma (NPC) tumor burden was remarkably decreased in a dose-dependent manner. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |