Tyk2-IN-23
Tyk2-IN-23 is a potent, orally active, selective TYK2 inhibitor (IC50 = 18 nM), exhibiting more than > 70-fold selectivity over JAK1/2/3 isoforms. Tyk2-IN-23 potently inhibits p-STAT3 in TYK2-dependent signaling activated by IFN-α and IL-10. Tyk2-IN-23 potently inhibits IFN-α-induced STAT1 phosphorylation in H9 cells. Tyk2-IN-23 can be used for the study of alopecia areata and allergic Rhinitis.
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- CAS. Nr.: 2734918-75-1
- Formel: C26H27ClFN5O2
- Molecular Weight:495.98
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Tyk2-IN-23 (Compound 29i) (50 nM-10 μM, 80 min) potently inhibits p-STAT3 in TYK2-dependent signaling activated by IFN-α (IC50 = 230.6 nM) and IL-10 (IC50 = 501.6 nM), but p-STAT3 induction by IL-21, IL-23, or IL-27 results in only marginal inhibition (IC50 > 2700 nM) in human peripheral blood mononuclear cells (hPBMC)[1].
Tyk2-IN-23 (0-10 μM, 1.5 h) potently inhibits IFN-α-induced STAT1 phosphorylation in H9 cells; in contrast, GM-CSF-induced STAT5 phosphorylation (JAK2-dependent), IL-4-induced STAT6 phosphorylation (JAK1/JAK3-mediated), and IL-6-induced STAT3 phosphorylation (JAK1/JAK2/TYK2-cooperative) remain unaffected even at 10000 nM[1].
Tyk2-IN-23 (0.625-40 μM, 24 h) shows no cytotoxicity at concentrations ≤ 10 μM in RBL-2H3 cells[1].
Tyk2-IN-23 (0-5 μM, 30 min) concentration-dependently inhibits the release of β-hexosaminidase from
Compound 48/80 trihydrochloride (HY-130592) (C48/80)-induced RBL-2H3 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RBL-2H3 cells
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Concentration:0.625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM
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Incubation Time:24 h
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Result:Showed no cytotoxicity at concentrations ≤ 10 μM in RBL-2H3 cells.
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Cell Line:H9 cells, THP-1 cells, TF-1 cells
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Concentration:10 nM, 50 nM, 100 nM, 500 nM, 1000 nM, 5000 nM, 10000 nM
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Incubation Time:Preincubated for 1h, then stimulated by IFN-α (1,000 U/mL) for 30 min
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Result:Significantly inhibited IFN-α-induced STAT1 phosphorylation in H9 cells.
No significant inhibitory effect on IL-4-induced STAT6 phosphorylation in THP-1 cells.
No significant inhibitory effect on GM-CSF-induced STAT5 and IL-6-induced STAT3 phosphorylation in TF-1 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C57BL/6J mice (6-8 weeks old) underwent basal sensitization via intraperitoneal injections (every other day for 14 days) of 50 μg OVA and 2 mg aluminum hydroxide dissolved in 200 μL saline (0.9 %), from days 14-20, daily nasal challenges were performed with 2 % OVA solution (10 μL per nostril)[1].
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Dosage:20 mg/kg, 40 mg/kg
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Administration:Intranasal drops, once daily for 8 days
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Result:Dose-dependently reduced AR symptoms (frequency of sneezing and nose scratching).
Reduced OVA-specific IgE (OVA-sIgE) levels.
Alleviated inflammatory cell infiltration and epithelial proliferation in the nasal mucosa.
Reduced mast cell infiltration and degranulation rate.
Reduced eosinophil infiltration.
Inhibited goblet cell proliferation.
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Animal Model:Using female C57BL/6J mice (6-8 weeks old), Alopecia areata (AA) was induced by hair removal and cyclophosphamide injection[1].
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Dosage:15 mg/kg, 30 mg/kg
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Administration:Oral gavage, once daily for 26 days
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Result:Promoted hair regeneration in a dose-dependent manner, with a significant increase in hair length and density in the high-dose group (30 mg/kg).
Decreased in pro-inflammatory factors (TNF-α and IL-23) and an increase in the anti-inflammatory factor IL-10.
Chemical Information
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CAS. Nr. 2734918-75-1
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Molecular Weight 495.98
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Formel C26H27ClFN5O2
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SMILES
O=C1NCCC21CCN(C3=C(C)C=NC(NC4=CC=C(OCC5=CC=CC(F)=C5)C(Cl)=C4)=N3)CC2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Tyk2-IN-23 Related Classifications
HY-178913 Related Classifications
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