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.
For research use only. We do not sell to patients.
- CAS No.: 30479-81-3
- Formula: C15H13N3O5S
- Molecular Weight:347.35
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
All AP-1 Isoforms
More
Biological Activity
Description
IC50 & Target
[1]|
FosB |
In Vitro
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. Further protocols information, click here.
-
Cell Line:Neuronal progenitor cells (NPC)
-
Concentration:0.16, 0.31, 0.63, 1.25, 2.5, 5.00, 10.00 and 20 μM,
-
Incubation Time:24,72 h
-
Result:Observed no discernable decrease after 24 h and only minimal losses after 72 h.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Heterozygous transgenic male and female mice (2-3 months)[1]
-
Dosage:50 μM in 0.2% DMSO/0.9% saline with 0.96 μL/h
-
Administration:intra-hippocampal infusion for 3 days
-
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
-
CAS No. 30479-81-3
-
Molecular Weight 347.35
-
Formula C15H13N3O5S
-
SMILES
O=C1N(C2=CC(S(=O)(O)=O)=C(OC3=CC=CC=C3)C=C2)N=C(N)C1
-
Synonyms
JFD 00458
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JPC0661 Related Classifications
HY-W471288 Related Classifications
Powered by Bioz