JPC0661
JPC0661 is a direct and allosteric ΔFOSB inhibitor. JPC0661 inhibits the binding of ΔFOSB/JUND and ΔFOsB to DNA with IC50 values in the micromolar range (9-52 uM), directly inhibits ΔFOSB-mediated transcription with IC50 of 0.82 μM in vitro. JPC0661 significantly reduces ΔFOSB occupancy at genomic AP1 sites in vivo. JPC0661 binds to a novel groove outside the DNA-binding cleft of ΔFOSB and disrupt the formation of the ΔFOSB/JUND-DNA complex. JPC0661 can be used for Alzheimer's disease research.
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- CAS No.: 30479-81-3
- Formule: C15H13N3O5S
- Masse moléculaire:347.35
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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FosB |
JPC0661 (0-100 μM) regulate ΔFOSB-driven gene expression with IC50 of 0.82 μM and accumulates ΔFOSB protein in HEK293 cells[1].
JPC0661 (0-100 μM, 24 or 72 h) has good tolerance in neuronal progenitor cells, AP1-luc HEK293 cells and d Neuro2A cells (NPC) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Neuronal progenitor cells (NPC)
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Concentration:0.16, 0.31, 0.63, 1.25, 2.5, 5.00, 10.00 and 20 μM,
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Incubation Time:24,72 h
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Result:Observed no discernable decrease after 24 h and only minimal losses after 72 h.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Heterozygous transgenic male and female mice (2-3 months)[1]
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Dosage:50 μM in 0.2% DMSO/0.9% saline with 0.96 μL/h
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Administration:intra-hippocampal infusion for 3 days
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Result:Exhibited an approximately 60% reduction in total binding sites.
Decreased average peak width.
Directly disrupted ΔFOSB–DNA interactions.
Caused a modest decline in promoter proximal peaks (≤1 kb) and a relative enrichment in distal intergenic peaks.
Chemical Information
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CAS No. 30479-81-3
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Masse moléculaire 347.35
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Formule C15H13N3O5S
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SMILES
O=C1N(C2=CC(S(=O)(O)=O)=C(OC3=CC=CC=C3)C=C2)N=C(N)C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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