JNK3 inhibitor-8
JNK3 inhibitor-8 is a potent, delective, orally active and cross the blood-brain barrier JNK3 inhibitor with IC50 values of 21, 2203, >10000 nM for JNK3, JNK2, JNK1, respectively. JNK3 inhibitor-8 shows significant neuroprotective effects. JNK3 inhibitor-8 has the potential for the research of Alzheimer’s disease (AD).
For research use only. We do not sell to patients.
- CAS No.: 3034676-53-1
- Formula: C32H30FN7O3
- Molecular Weight:579.62
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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JNK3 21 nM (IC50) |
JNK2 2203 nM (IC50) |
JNK1 >10000 nM (IC50) |
JNK3 inhibitor-8 (compound 3h; 10, 20 µM; 24, 48 h) increases primary rat cortex neuron cell viability when treatment with 10 μM amyloid-β1-42[1].
JNK3 inhibitor-8 (10, 20 µM) decreases the expression of p-c-jun (S63), p-c-jun (S73), PARP and p-Tau 10 μM amyloid-β1-42 stitumed[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:primary rat cortex neuron cells
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Concentration:10, 20 µM
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Incubation Time:24, 48 h
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Result:Increased cell viability when treatment with 10 μM amyloid-β1-42.
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Cell Line:primary rat cortex neuron cells
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Concentration:10, 20 µM
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Incubation Time:
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Result:Decreased the expression of p-c-jun (S63) and p-c-jun (S73) in 0.5 μM anisomycin or 10 μM amyloid-β1-42 stitumed, and decreased the expression of PARP and p-Tau expression when treatment with 10 μM amyloid-β1-42.
Pharmacokinetic Parameters of JNK3 inhibitor-8 in Sprague-Dawley rats[1].
| compound | 2h |
| admin. | PO |
| dose (mg/kg) | 3 |
| AUClast (h ng/ml) | 727.09 |
| C0 or Cmax (ng/mL) | 423.17 |
| Tmax (h) | 0.39 |
| T1/2 (h) | 0.97 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6 month-old APP/PS1 AD mice[1]
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Dosage:30, 60 mg/kg
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Administration:P.o.; daily for 4 weeks
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Result:Decrease in escape time and distance traveled, showed a significantly higher level of altered behavioral ability compared to APP/PS1 and vehicle control in the Y-maze test, improved memory and cognitive function.
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Animal Model:10 month-old 3xTg AD mice[1]
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Dosage:30, 60 mg/kg
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Administration:P.o.; daily for 4 weeks
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Result:Decreased the escape time and the distance, increased TSPQ and TSTZ levels, significantly decreased the expression of pTau levels and improved memory and cognitive function.
Chemical Information
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CAS No. 3034676-53-1
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Molecular Weight 579.62
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Formula C32H30FN7O3
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SMILES
O=C(N1C[C@@H](NC2=NC=CC(N3C4=C(N=C3C5=CC6=C(C=C5)C=CC=C6)C(F)=CC(OC(NC)=O)=C4)=N2)CCC1)C7CC7
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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)