TOPK-p38/JNK-IN-1
TOPK-p38/JNK-IN-1 (Compound B12) is an orally active TOPK-p38/JNK signaling pathway inhibitor with the IC50 value of 2.14 µM for NO production. TOPK-p38/JNK-IN-1 shows anti-inflammatory activities. TOPK-p38/JNK-IN-1 also inhibits phosphorylate downstream related proteins and avoids degradation of TOPK.
For research use only. We do not sell to patients.
- CAS No.: 2745108-35-2
- Formula: C17H15F3N2O4
- Molecular Weight:368.31
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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JNK |
NO Production 2.14 μM (IC50) |
TOPK-p38/JNK-IN-1 (Compound B12) (10 µM, 1 h) inhibits the NO production in RAW264.7 cells[1]
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TOPK-p38/JNK-IN-1 (Compound B12) (0-100 µM, 24 h for RAW264.7 cells; 0-50µM, 6h for HaCaT cells) inhibits cell proliferation in a dose-dependent manner[1]
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TOPK-p38/JNK-IN-1 (Compound B12) (0-10 µM, 1h for RAW264.7 cells; 6 h for HaCaT cells) suppresses LPS-induced TOPK/NF-jB/p38/JNK activation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7 cell lines
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Concentration:4 µM, 20 µM and 100µM
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Incubation Time:24 h
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Result:Inhibited cell proliferation in a dose-dependent manner.
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Cell Line:HaCaT cell line.
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Concentration:0.78 µM, 1.56 µM, 3.125µM, 6.25 µM, 12.5 µM, 25 µM and 50 µM.
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Incubation Time:Pre-treated with compound B12 for 6 h, incubated with LPS (100 g/mL) for 24 h
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Result:Inhibited excessive proliferation of LPS-induced HaCaT cells in a dose-dependent manner.
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Cell Line:RAW264.7 and HaCaT cell line.
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Concentration:2.5 µM, 5 µM and 10µM.
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Incubation Time:Pre-treated for 1 h, co-treated with LPS (0.5 µg/mL) for 0.5 h or 24 h and pre-treated for 6 h before SUV irradiation respectively.
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Result:Inhibited the expression of iNOS and COX-2 in a dose-dependent manner, affected the phosphorylation of TOPK and inhibited P38/JNK protein phosphorylation and NF-κB p65 translocated into the nucleus.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Inbred 6–8-week-old female BALB/c mice[1].
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Dosage:20 mg/kg, 40 mg/kg
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Administration:IG, once a day, each group for 7 days. Induce skin inflammation by topically applying 62.5 mg of IMQ cream on the shaved 2 cm × 3 cm back skins.
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Result:Successfully reduced the scales, thickness and erythema in psoriasis-like mice, histopathologically alleviated hyperkeratosis, acanthocyte proliferation and inflammatory cell infiltration. Inhibited the expression of related proteins (p-STAT3, p-TOPK, TOPK, p-p38, p-JNKs, PCNA, p-H2AX) in mouse skin tissues in a dose-dependent manner.
Chemical Information
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CAS No. 2745108-35-2
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Molecular Weight 368.31
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Formula C17H15F3N2O4
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SMILES
O=C(NC1=CC=CC(C(F)(F)F)=C1)NC2=CC(C(C)=O)=C(O)C=C2OC
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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)
TOPK-p38/JNK-IN-1 Related Classifications
HY-144761 Related Classifications
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