NuP-3
NuP-3 is an orally active dual inhibitor of MAPK13 (IC50 < 250 nM), MAPK14 (IC50 = 7 nM), MAPK12 and MAPK11. NuP-3 blocks airway inflammation and mucus production. NuP-3 is used for the research of respiratory system diseases.
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- No. CAS: 2392969-05-8
- Fòrmula: C24H24ClFN4O3
- Peso molecular:470.92
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
NuP-3 (Compound 396) at 0.1 μM selectively inhibits MAPK13, MAPK14, MAPK11, and MAPK12; in a cell-free kinome screening, only 4% of the 400 tested kinases show an inhibition rate > 90%[1].
NuP-3 (21 days) potently inhibits MUC5AC production in primary human tracheobronchial epithelial cells stimulated by IL-13, with an IC50 of 0.005 nM within 21 days and a cell therapeutic index of 200000, indicating high safety[1].
NuP-3 (21 days) inhibits MUC5AC production in primary porcine tracheobronchial epithelial cells stimulated by IL-13, with an IC50 of 0.420 nM within 21 days and a cellular therapeutic index of 2381, indicating low toxicity[1].
NuP-3 (100 nM; 21 days) reduces IL-13-induced MUC5AC production in primary human tracheobronchial epithelial cells with MAPK gene knockout via CRISPR/Cas9[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
NuP-3 (2 mg/kg; p.o.; twice daily; 24 days) blocks virus-induced airway mucus production in Yucatan mini-pigs[1].
NuP-3 (2 mg/kg; i.p.; twice daily) blocks virus-induced airway mucus production, epithelial reprogramming, and type 2 immune response in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Yucatan mini-pigs (male and female, 7-8 weeks of age, 21-25 kg, IL-13-challenged model)[1]
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Dosage:0.2 mg/kg; 2 mg/kg; 20 mg/kg
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Administration:p.o.; twice daily; 6 days
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Result:Significantly decreased BAL fluid levels of MUC5AC and CLCA1, and significantly reduced eosinophil and neutrophil influx into the airspace at 2 mg/kg compared to vehicle control.
Showed decreased anti-mucus and anti-inflammatory effects at 0.2 mg/kg and preserved effects at 20 mg/kg compared to vehicle control.
Observed no adverse effects (behavior, appetite, body weight, vital signs, gastrointestinal/urinary function, complete blood count) at any dose.
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Animal Model:Yucatan mini-pigs (male and female, 7-8 weeks of age, 21-25 kg, Sendai virus-infected model)[1]
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Dosage:2 mg/kg
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Administration:p.o.; twice daily; 24 days
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Result:Significantly attenuated SeV-induced increases in BAL fluid levels of MUC5AC and CLCA1 compared to vehicle control.
Did not alter viral titer or cause detectable adverse effects.
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Animal Model:Mice[1]
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Dosage:2 mg/kg
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Administration:i.p.; twice daily; 23 days (pre-infection); twice daily; 11 days (delayed post-infection)
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Result:Fully blocked SeV-induced increases in lung tissue Muc5ac, Clca1, Aqp3, Krt5, Trp63, Il33, Il13, and Arg1 mRNA levels compared to vehicle control when administered starting 2 days before infection.
Significantly attenuated the aforementioned mRNA levels compared to vehicle control when treatment was delayed until 10 days post-infection.
Did not affect mouse behavior, body weight, or clinical signs of infection.
Chemical Information
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No. CAS 2392969-05-8
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Peso molecular 470.92
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Fòrmula C24H24ClFN4O3
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SMILES
O=C(NC1=CC(C(C)(C)C)=CC=C1Cl)NC2=CC=C(C=C2F)OC3=CC(NC(C)=O)=NC=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NuP-3 Related Classifications
HY-186241 Related Classifications
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