Acacetin

SKU: orb1224983

Description

Acacetin has anti-plasmodial activity and anti-peroxidant activity. Also acacetin is an ATP-competitive PI3K inhibitor. And has anti-cancer and antitumor activities, such as prostate cancer, melanoma angiogenesis tumor , via Akt/NF-κB,Stat signaling pathway.Has anti-inflammatory and antiarthritic effects in FLSs, can inhibit p38 and JNK phosphorylation and reduces MMP-1, MMP-3 and MMP-13 expression in interleukin-1β-induced FLSs.

Key Properties

• CAS Number: 480-44-4
• MW: 284.3
• Purity: >98% (HPLC)
• Formula: C₁₆H₁₂O₅
• SMILES: O=C1C=C(C2=CC=C(OC)C=C2)OC3=C1C(O)=CC(O)=C3
• Target: COX
• Solubility: DMSO: >10.7mg/mL

Bioactivity

• In Vivo:
  Acacetin (5, 7-Dihydroxy-4'-methoxyflavone; 5, 20 mg/kg/day; orally; for 3 days) significantly suppresses microglial activation in an LPS-induced neuroinflammation mouse model. Acacetin (25 mg/kg/day; orally; for 3 days) reduces neuronal cell death in an Animal model of ischemia. Acacetin (1.8-56.2 mg/kg/day; ip; single dose) decreases visceral and inflammatory nociception and prevented the formalin-induced oedema. Animal model: Male C57BL/6 mice, 7 weeks of age. Dosage: 5, 20 mg/kg. Administration: Orally; once a day for 3 days. Result: Significantly suppressed microglial activation in an LPS-induced (ip; 5 mg/kg) neuroinflammation mouse model.
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• In Vitro:
  Acacetin (5, 7-Dihydroxy-4'-methoxyflavone; 10-200 μM; 24 hours) decreases cell viabilities in a dose-dependent manner. Acacetin has little effect on human normal glial cell line HEB and non-tumorigenic epithelial cell line MCF-10A. Acacetin (50-150 μM; 24 hours) causes G2/M cell cycle arrest and induces apoptosis and autophagy. Acacetin (50-150 μM; 24 hours) leads to decreases in levels of PI3Kγ-p110, p-AKT, p-mTOR, p-p70S6K, and p-ULK in a dose-dependent manner. Cell Viability Assay Cell line: Breast cancer MCF-7 cells, hepatocellular carcinoma SMMC-7721 cells, lung adenocarcinoma A549 cells, esophageal carcinoma Eca109 cells. Concentration: 10, 20, 40, 60, 80, 100, 150, 200 μM. Incubation time: 24 hours. Result: Decreased cancer cell viabilities in a dose-dependent manner. Had IC50 values of 82.75 μM, 103.9 μM, 157.4 μM, 54.7 μM in MDA-MB-231, MCF-7, A549, Eca109 cells, respectively. Cell Cycle Analysis Cell line: MDA-MB-231 cells. Concentration: 50, 100, 150 μM. Incubation time: 24 hours. Result: Resulted in increase in percentage of cells at G2/M phase and decrease in percentage of cells at G1 and S phase in a dose-dependent manner. Apoptosis Analysis Cell line: MDA-MB-231 cells. Concentration: 50, 100, 150 μM. Incubation time: 24 hours. Result: Induced apoptosis. Cell Autophagy Assay Cell line: MDA-MB-231 cells. Concentration: 50, 100, 150 μM. Incubation time: 24 hours. Result: Induced autophagy. Resulted in marked increases in EGFP-LC3 puncta formation and a dose-dependent accumulation of LC3-II. Western blot analysis. Cell line: MDA-MB-231 cells. Concentration: 50, 100, 150 μM. Incubation time: 24 hours. Result: Resulted in decrease in levels of Bcl-2 and Bcl-xL and increase in levels of p53. Led to decreases in levels of PI3Kγ-p110, p-AKT, p-mTOR, p-p70S6K, and p-ULK in a dose-dependent manner.
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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

LY064233 | NSC 76061

Quick Database Links

Gene Symbol

COX