JAK1-IN-20
JAK1-IN-20 (Compound 38) is a gut-restricted, orally active, selective JAK1 inhibitor with an IC50 of <0.5 nM. JAK1-IN-20 inhibits the enzymatic activity of JAK1, reduces the production of proinflammatory cytokines (TNF-α, IL-6), and suppresses the phosphorylation of STAT3. JAK1-IN-20 ameliorates ulcerative colitis. JAK1-IN-20 can be used for the research of inflammatory bowel disease.
For research use only. We do not sell to patients.
- CAS No.: 3106963-85-0
- Formula: C26H25ClFN7O3
- Molecular Weight:537.97
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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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JAK1 <0.5 nM (IC50) |
IL-6 |
STAT3 |
JAK1-IN-20 (dose-response range; 10 min, 60 min, 40 min, 40 min) potently and selectively inhibits JAK1 enzymatic activity with an IC50 < 0.5 nM, showing >312-fold, >20000-fold, and >354-fold selectivity over JAK2, JAK3, and TYK2, respectively[1].
JAK1-IN-20 (dose-response range; 24 h) potently inhibits IL-6-induced JAK/STAT3 signaling in HEK-Blue IL-6 cells with an IC50 of 28.0 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:TF-1 cells, H9 cells
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Concentration:Dose-response range; 100 nM, 500 nM (TF-1 cells, STAT3); 1000 nM (H9 cells, STAT1); 2000 nM (TF-1 cells, STAT5); 1000 nM tofacitinib (control)
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Incubation Time:1 h
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Result:Potently suppressed IL-6-induced STAT3 phosphorylation with an IC50 of 218.6 nM.
Showed a concentration-dependent inhibitory profile and achieved comparable efficacy to 1000 nM tofacitinib at 100 nM.
Reduced IL-6-induced STAT3 phosphorylation at 500 nM.
Reduced IFN-α-induced STAT1 phosphorylation at 1000 nM.
Reduced GM-CSF-induced STAT5 phosphorylation at 2000 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (female, 7-8 weeks old, DSS-induced ulcerative colitis)[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:p.o.; daily
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Result:Significantly reduced DAI scores compared to vehicle controls at 30 mg/kg.
Increased colon length and reduced colon wet weight relative to vehicle controls at 30 mg/kg.
Suppressed colon tissue TNF-α and IL-6 levels compared to vehicle controls at 30 mg/kg.
Reduced colonic tissue damage, including mucosal erosion, crypt architecture loss, and inflammatory cell infiltration, relative to vehicle controls at 30 mg/kg.
Demonstrated a dose-dependent improvement in disease outcomes.
Chemical Information
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CAS No. 3106963-85-0
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Molecular Weight 537.97
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Formula C26H25ClFN7O3
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SMILES
ClC1=CN=C(N=C1NC2CCN(CC2)C(NC3=CC=C(C=C3F)C(C)=O)=O)NC4=CC(CN5)=C(C=C4)C5=O
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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)
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