LY294002

SKU: orb1226118

Description

A classic, broad-spectrum PI3K inhibitor with IC50 of 0.5/0.57/0.97 uM for PI3Kα/δ/β, respectively; completely and specifically abolishes PI3K activity (IC50=1.4 uM), but does not inhibit PI4K or other lipid kinases; demonstrates growth-inhibitory and apoptosis-inducing effect in colon cancer cell lines, with decreased phosphorylated Akt Ser(473); suppresses tumor growth in mouse xenografts; also is a potent inhibitor of CK2 with IC50 of 98 nM.(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.\n(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.

Key Properties

• CAS Number: 154447-36-6
• MW: 307.3432
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₇NO₃
• SMILES: O=C1C=C(N2CCOCC2)OC3=C(C4=CC=CC=C4)C=CC=C13
• Target: PI3K
• Solubility: DMSO: 14.9 mg/mL

Bioactivity

• 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. 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: Intraperitoneal injection; twice weekly, for 4 weeks. Result: Mean Nasopharyngeal carcinoma (NPC) tumor burden was remarkably decreased in a dose-dependent manner.
• 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. 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 dose-dependent. Western blot analysis. Cell line: CNE-2Z cells. Concentration: 10 μM, 25 μM, 50 μM, and 75 μM. Incubation time: Result: Decreased phosphorylated Akt (S473) expression levels were significantly, up-regulated caspase-9 activity in CNE-2Z cells in treated group.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NSC 697286 | SF 1101 | LY 294002 | LY-294002

Quick Database Links

Gene Symbol

PI3K