JNK3 inhibitor-3
JNK3 inhibitor-3 (compound 15g) is a selective, BBB permeable and orally active c-Jun N-terminal kinase 3 (JNK3) inhibitor. JNK3 inhibitor-3 has inhibitory activities to JNK1, JNK2 and JNK3 with IC50 values of 147.8, 44.0 and 4.1 nM, respectively. JNK3 inhibitor-3 significantly improves the memory in mouse dementia model. JNK3 inhibitor-3 can be used for the research of Alzheimer’s disease.
For research use only. We do not sell to patients.
- CAS No.: 2873465-25-7
- Formula: C26H25N7O2
- Molecular Weight:467.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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JNK3 4.1 nM (IC50) |
JNK2 44 nM (IC50) |
JNK1 147.8 nM (IC50) |
In Vitro
JNK3 inhibitor-3 (0-10 μM) shows inhibitory activities to JNK1, JNK2 and JNK3 with IC50 values of 147.8, 44.0 and 4.1 nM, respectively[1]. JNK3 inhibitor-3 (20 μM; 24 and 48 h) demonstrates neuroprotective effects in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Rat cortical neurons
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Concentration:20 μM
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Incubation Time:24 and 48 hours
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Result:Protected rat cortical neurons against 10 μM Aβ1-42 induced neurotoxicity.
In Vivo
| Rats IV 1 mg/kg |
Rats PO 3 mg/kg |
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| AUC (hr•ng/mL) | 1085.24 | 2806.77 |
| Cmax (ng/mL) | 1238.85 | |
| Tmax (hr) | 0.67 | |
| T1/2 (hr) | 0.36 | 1.14 |
| BA (%) | 86.21 | |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Homozygous 3xTg and APPswe/PS1dE9 double-transgenic mice model of Alzheimer’s disease[1]
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Dosage:30 and 60 mg/kg
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Administration:Oral administration; once daily for 2 or 2.2 month
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Result:Induced no abnormal symptoms or weight changes, significantly enhanced the spontaneous alteration in APP/PS1 and doses of 30 and 60 mg/kg than that of vehicle group in Y-maze test and showed a significant difference compared to the 3xTg vehicle control in the passive avoidance test.
Chemical Information
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CAS No. 2873465-25-7
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Molecular Weight 467.52
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Formula C26H25N7O2
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SMILES
N#CCC1=CN=C(N1C2=NC(N[C@H]3CCCN(C3)C(C4CC4)=O)=NC=C2)C5=CC6=C(OC=C6)C=C5
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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.
Protocols
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JNK3 inhibitor-3 Related Classifications
HY-151928 Related Classifications
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