1. Immunology/Inflammation Cell Cycle/DNA Damage
  2. AP-1 DNA Alkylator/Crosslinker
  3. 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.

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YL0441

YL0441 Chemical Structure

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Description

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].

IC50 & Target[1]

ΔFOSB/JUND

13.7<br/> μM (IC50)

ΔFOSB

12.3 μM (IC50)

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 50 μM; 18.5 ng per hour
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.
Molecular Weight

385.39

Formula

C19H15NO6S

SMILES

O=C(/C=C/C1=CC=CO1)NC(C=C2S(O)(=O)=O)=CC=C2OC3=CC=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
YL0441
Cat. No.:
HY-182050
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