YL0441

YL0441 is an inhibitor of ΔFOSB/JUND heterodimers and ΔFOSB homomultimers, with IC₅₀ values of 13.7 μM and 12.3 μM, respectively. YL0441 blocks the binding of ΔFOSB to DNA. YL0441 reduces ΔFOSB bound to genomic DNA in the hippocampal tissues of APP mice. YL0441 is applicable to the research of Alzheimer's disease ^[1].

In Vivo, YL0441 (50 μM; infused into the hippocampus; for 3 consecutive days) reduces the binding level of ΔFOSB to genomic DNA in the hippocampus of APP transgenic mice by ~94%^[1].

In Vitro, YL0441 (0-200 μM; 15 min) disrupts the binding of purified full-length mouse ΔFOSB/JUND heterodimers and ΔFOSB/ΔFOSB homomers to a TAMRA-labeled AP-1 consensus oligonucleotide with IC₅₀ values of 13.7 μM and 12.3 μM, respectively^[1]. YL0441 (12.5-50 μM; 72 h) shows no detectable toxicity to Neuro 2A cells at concentrations up to 50 μM after 72 h of incubation^[1]. YL0441 (1 μM; up to 60 min) exhibits high metabolic stability in mouse liver microsomes, with a half-life greater than 186.38 min^[1].

References:
[1]. McNeme S, et al. Efficient In Vivo Pharmacological Inhibition of ΔFOSB, an AP-1 Transcription Factor, in the Brain. ACS Chem Neurosci. 2026;17(7):1316-1331.