lufenuron exhibits a broad spectrum of bioactivity, demonstrating inhibitory actions in various biological assays. It effectively inhibits Tau fibril formation, ROR gamma transcriptional activity, 15-human lipoxygenase, Menin-MLL interaction (relevant in MLL-related leukemias), Ubiquitin-specific Protease USP2a, USP1/UAF1, the antioxidant response element signaling pathway, human tyrosyl-DNA phosphodiesterase 1 (TDP1), the human pregnane X receptor (PXR) signaling pathway, human apurinic/apyrimidinic endonuclease 1 (APE1), and exhibits potential to block Ebola Virus entry. Additionally, it has demonstrated potency against schistosomiasis, evidenced through its activity in Schwann cell PMP22 intronic element assays.
In insecticidal assays, lufenuron shows significant activity against 5th instar nymphs of Dysdercus koenigii, with an LD50 of 9.0 µg, and reduces the fertility of various fruit fly species including Anastrepha striata, Anastrepha obliqua, and Anastrepha serpentina by lowering egg hatching rates. Its toxicity towards red blood cells (RBCs) is relatively low, with an HC50 greater than 1000.0 µg mL^-1. However, it shows no significant antifungal effects, with MIC or GI values greater than 512.0 µg mL^-1 for various fungal strains.
lufenuron displays potent inhibition of sodium fluorescein uptake in OATP1B3 and OATP1B1-transfected CHO cells, with inhibition rates of 97.09% and 102.79% respectively at 10 µM. Antiviral activity was observed in inhibiting SARS-CoV-2 induced cytotoxicity in Caco-2 cells at a concentration of 10 µM (36.21% inhibition), though it showed low antiviral activity against SARS-CoV-2 (USA-WA1/2020 strain) in HRCE cells and only a slight inhibition of SARS-CoV-2 3CL-Pro protease at 20 µM (-2.546%).
Lastly, lufenuron exhibited minimal inhibition of human HDAC6 in enzyme assays using both commercial and custom peptide substrates, with inhibition percentages of 2.46% and -1.65% respectively. These diverse bioactivities reflect its multifaceted potential across various biological pathways and diseases..
Note: Summary generated by AI. Data source: ChEMBL 