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.
For research use only. We do not sell to patients.
- Formula: C19H15NO6S
- Molecular Weight:385.39
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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All AP-1 Isoforms
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Biological Activity
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ΔFOSB/JUND 13.7 |
ΔFOSB 12.3 μM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
hippocampus; for 3 consecutive days) reduces the binding level of ΔFOSB to genomic DNA in the hippocampus of APP transgenic mice by ~94%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:J20 (2-3 month-old; heterozygous transgenic; male and female; Alzheimer's disease model expressing human amyloid precursor protein with Swedish and Indiana mutations)[1]
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Dosage:50 μM; 18.5 ng per hour
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Administration:infused into the
hippocampus; continuous; 3 consecutive days -
Result:Reduced total ΔFOSB-bound genomic DNA peaks from 9642 to 540, representing a ~94% reduction in total binding events.
Decreased average peak width of remaining ΔFOSB-bound sites from ~286 bp to ~254 bp.
Reduced ΔFOSB binding to unique target genes by ~94%, with a 95% reduction in promoter-bound genes and 91% reduction in distal intergenic-bound genes.
Eliminated ΔFOSB occupancy across all genomic regions (promoters, exons, introns, distal intergenic regions), with no induction of ΔFOSB binding to novel ectopic sites.
Chemical Information
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Molecular Weight 385.39
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Formula C19H15NO6S
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SMILES
O=C(/C=C/C1=CC=CO1)NC(C=C2S(O)(=O)=O)=CC=C2OC3=CC=CC=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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