Acacetin (5, 7-Dihydroxy-4'-methoxyflavone) is an orally active flavonoid derived from Tephroseris kirilowii (Turcz.) Holub. Acacetin docks in the ATP binding pocket of PI3Kγ. Acacetin causes cell cycle arrest and induces apoptosis and autophagy in cancer cells. Acacetin has potent anti-cancer and anti-inflammatory activity and has the potential for pain-related diseases research.

Product information

CAS Number: 480-44-4

Molecular Weight: 284.26

Formula: C16H12O5

Synonym:

5,7-Dihydroxy-4'-methoxyflavone

Chemical Name: 5, 7-dihydroxy-2-(4-methoxyphenyl)-4H-chromen-4-one

Smiles: COC1=CC=C(C=C1)C1=CC(=O)C2=C(C=C(O)C=C2O)O1

InChiKey: DANYIYRPLHHOCZ-UHFFFAOYSA-N

InChi: InChI=1S/C16H12O5/c1-20-11-4-2-9(3-5-11)14-8-13(19)16-12(18)6-10(17)7-15(16)21-14/h2-8,17-18H,1H3

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 37 mg/mL (130.16 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

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.

References:

1. Hong-Wei Zhang, et al. Flavonoids inhibit cell proliferation and induce apoptosis and autophagy through downregulation of PI3Kγ mediated PI3K/AKT/mTOR/p70S6K/ULK signaling pathway in human breast cancer cells. Sci Rep. 2018 Jul 26;8(1):11255.
2. Sang Keun Ha, et al. Acacetin attenuates neuroinflammation via regulation the response to LPS stimuli in vitro and in vivo. Neurochem Res. 2012 Jul;37(7):1560-7.
3. A I Carballo-Villalobos, et al. Evidence of mechanism of action of anti-inflammatory/antinociceptive activities of acacetin. Eur J Pain. 2014 Mar;18(3):396-405.

Products are for research use only. Not for human use.