3',​4',​5',​5,​7-​Pentamethoxyflavone

SKU: orb1698446

Description

3',4',5',5,7-Pentamethoxyflavone is a brassinosteroid flavonoid isolated from the Rutaceae family. It acts as an Nrf2 pathway inhibitor, demonstrating potential to overcome chemoresistance in cancer cells. Research applications include in vitro studies investigating its mechanisms and anticancer properties.

Research Area

Immunology & Inflammation

Key Properties

• CAS Number: 53350-26-8
• MW: 372.37
• Purity: 98.00% (May vary between batches)
• Formula: C₂₀H₂₀O₇
• SMILES: COc1cc(OC)c2c(c1)oc(cc2=O)-c1cc(OC)c(OC)c(OC)c1
• Target: Nrf2
• Solubility: DMSO:22.5 mg/mL (60.42 mM);10% DMSO+90% Corn Oil:2 mg/mL (5.37 mM)

Bioactivity

• In Vivo:
  The flavones tricin (4',5,7-trihydroxy-3',5'-dimethoxyflavone) and 3',4',5',5,7-Pentamethoxyflavone (PMF) are under development as potential colorectal cancer chemopreventive agents as they reduced adenoma development in the Apc(Min) mouse model of intestinal carcinogenesis. Plasma concentrations and area under the plasma concentration versus time curve for PMF were higher than those for tricin. A mono-O-desmethyl PMF and several isomeric mono-O-desmethyl PMF glucuronides and sulfonates were major PMF metabolites in murine plasma, liver and intestinal tissue. In murine and human liver fractions, in vitro metabolic removal of tricin was faster than that of PMF.
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• In Vitro:
  3',4',5',5,7-Pentamethoxyflavone (PMF), a natural flavonoid extracted from Rutaceae plants, sensitized A549/CDDP to CDDP and substantially induced apoptosis compared with that of CDDP alone treated group, and this reversal effect decreased when Nrf2 was downregulated by siRNA. Mechanistically, PMF reduced Nrf2 expression leading to a reduction of Nrf2 downstream genes, and in contrast, this effect was decreased by blocking Nrf2 with siRNA. Taken together, these results demonstrated that PMF could be used as an effective adjuvant sensitizer to increase the efficacy of chemotherapeutic drugs by downregulating Nrf2 signaling pathway.
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Storage & Handling

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

Alternative Names

Caspase, Bcl-2, 5,7,3',4',5'-Pentamethoxyflavone, 3',4',5',5,7-Pentamethoxyflavone, NO, PARP, Nrf2, IL Recepter, P-gp

Compound Identifiers

PubChem CID

493376