LY-294002 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LY294002 是 PI3Kα/δ/β 的合成分子抑制剂（IC50：0.5/0.57/0.97 μM，无细胞测定）；在溶液中比渥曼青更稳定，也是自噬体形成的阻断剂。

LY294002 is a synthetic molecule inhibitor of PI3Kα/δ/β (IC50: 0.5/0.57/0.97 μM, in cell-free assays); more stable than Wortmannin in solution, and also is a blocker of autophagosome formation.

LY294002 hydrochloride (0-75 μM; 24 hours and 48 hours) remarkably decreases human nasopharyngeal carcinoma CNE-2Z cells in a dose-dependent fashion.LY294002 hydrochloride (0-75 μM; 24 hours and 48 hours ) induces CNE-2Z cells apoptosis rate in dose-dependent.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.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. Cell Proliferation Assay Cell Line:CNE-2Z cells 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 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 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.

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. 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. Animal Model:Athymic nude mice (6-8 weeks) with CNE-2Z xenograft 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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Others

Other Targets

p110α| p110β| p110δ

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934389-88-5

343.81

C19H17NO3·HCl

>98% (HPLC)

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C1COCCN1C2=CC(=O)C3=C(O2)C(=CC=C3)C4=CC=CC=C4.Cl

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(-20℃)

With Ice Pack

≥ 2 years