Anthracene-9-carboxylic acid exhibits a broad spectrum of bioactivities, acting as an inhibitor in various assays targeting multiple molecular interactions and enzymes. It demonstrates potent inhibition of the Menin-MLL interaction in MLL-related leukemias, HSD17B4, JMJD2E, Cytochrome P450 2C19, Aldehyde Dehydrogenase 1 (ALDH1A1), HPGD (15-Hydroxyprostaglandin Dehydrogenase), human alpha-Galactosidase, and USP1/UAF1. It also functions as a lipid storage modulator. The compound inhibits lactate uptake in Xenopus laevis oocytes with significant activity.
In Caenorhabditis elegans N2 Bristol, it inhibits a voltage-gated calcium channel by 20.0% at 50 mg/l after 1 hour, and shows ovicidal activity against Meloidogyne incognita eggs, with an EC50 of 48.01 ug/mL. It has nematicidal activity against J2 juveniles and adult C. elegans N2 Bristol, with LC50 values ranging from 5.35 to 42.7 ug/mL. Additionally, it exhibits high inhibitory activity in OATP1B3 and OATP1B1-transfected CHO cells, showing 87.88% and 95.94% inhibition, respectively, in the uptake of sodium fluorescein at 10 uM.
Regarding antiviral properties, Anthracene-9-carboxylic acid inhibits SARS-CoV-2 induced cytotoxicity in Caco-2 cells by 5.36% at 10 uM after 48 hours, inhibits the SARS-CoV-2 3CL-Pro protease by 16.23% at 20 µM, and shows a 0.72% inhibition rate in VERO-6 cells at 10 uM after 48 hours of viral exposure.
Finally, it shows inhibitory activity against human HDAC6 enzyme, with a 22.87% inhibition in an enzymatic assay using a commercial peptide substrate, though it exhibited a lower inhibition of -0.75% in a separate assay with a custom peptide substrate..
Note: Summary generated by AI. Data source: ChEMBL 