3,5-Dimethoxystilbene exhibits a diverse range of bioactivities across various biological assays and targets. It inhibits the production of PGE-2 in LPS-stimulated RAW264.7 cells with an IC50 value of 100.0 nM and has larvicidal activity against Aedes aegypti larvae at a minimum concentration of 3.0 ppm, achieving complete larval mortality within 24 hours. The compound shows antimicrobial activity, though it is not highly effective against certain bacteria strains such as Mycobacterium smegmatis, Escherichia coli, Bacillus cereus, methicillin-resistant Staphylococcus aureus, and Staphylococcus aureus, with MIC values greater than 512.0 ug/mL.
3,5-Dimethoxystilbene also displays potency in several biochemical assays, including inhibition of JMJD2A-Tudor Domain, Nrf2 activation, HP1-beta Chromodomain interactions, polymerase iota, and mammalian selenoprotein thioredoxin reductase 1 (TrxR1). It inhibits Marburg Virus binding or entry into cells and induces DNA re-replication in MCF 10a breast cells and SW480 colon adenocarcinoma cells. Additionally, it modulates PINK1 expression, inhibits the SWI/SNF chromatin remodeling complex, and acts as an agonist of the gsp mutation responsible for Fibrous Dysplasia/McCune-Albright Syndrome.
The compound inhibits Electrophorus electricus C2888 AChE with an IC50 value of 9,000.0 nM and exhibits dual activity at human and rat TRPA1 receptors. It acts as an antagonist at human TRPV1 receptors (IC50 > 10,000.0 nM) and also performs as both an agonist (EC50 of 1,700.0 nM, efficacy of 84.1%) and antagonist (IC50 of 3,400.0 nM) at rat TRPA1 receptors. Furthermore, it shows inhibition of TRPA1 activity at 30 µM, preincubated for 6 minutes, resulting in decreased AITC-induced calcium influx, while also inducing calcium influx under similar conditions.
Characterized by a log P value of 4.15, 3,5-Dimethoxystilbene has high lipophilicity, which could influence its bioavailability, distribution, and interaction with biological systems..
Note: Summary generated by AI. Data source: ChEMBL 