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JPC0661 is a direct and allosteric inhibitor of ΔFOSB. It inhibits the binding of ΔFOSB/JUND and ΔFOSB to DNA with a micromolar IC50 value (9-52 μM), and directly suppresses ΔFOSB-mediated transcription in vitro with an IC50 of 0.82 μM. In vivo, JPC0661 notably reduces the occupancy of ΔFOSB at genomic AP1 sites. JPC0661 disrupts the formation of the ΔFOSB/JUND-DNA complex by binding to a novel groove outside the ΔFOSBDNA binding cleft. JPC0661 is applicable in Alzheimer's disease research.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | JPC0661 is a direct and allosteric inhibitor of ΔFOSB. It inhibits the binding of ΔFOSB/JUND and ΔFOSB to DNA with a micromolar IC50 value (9-52 μM), and directly suppresses ΔFOSB-mediated transcription in vitro with an IC50 of 0.82 μM. In vivo, JPC0661 notably reduces the occupancy of ΔFOSB at genomic AP1 sites. JPC0661 disrupts the formation of the ΔFOSB/JUND-DNA complex by binding to a novel groove outside the ΔFOSBDNA binding cleft. JPC0661 is applicable in Alzheimer's disease research. |
| In vitro | JPC0661 (0-100 μM) modulates ΔFOSB-driven gene expression with an IC50 of 0.82 μM and induces ΔFOSB protein accumulation in HEK293 cells. At concentrations of 0-100 μM for 24 or 72 hours, JPC0661 demonstrates good tolerability in neural progenitor cells, AP1-luc HEK293 cells, and Neuro2A cells. |
| In vivo | JPC0661 (50 μM, administered at a rate of 16.7 ng/h over 3 days) significantly and broadly decreases the binding of ΔFOSB at most normal genomic binding sites in male and female heterozygous transgenic mice expressing human amyloid precursor protein (APP) with Swedish (K670N, M671L) and Indiana (V717F) mutations. |
| Molecular Weight | 347.35 |
| Formula | C15H13N3O5S |
| Cas No. | 30479-81-3 |
| Smiles | O=C1N(N=C(N)C1)C2=CC=C(OC=3C=CC=CC3)C(=C2)S(=O)(=O)O |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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