2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Immunology/Inflammation
  3. JAK Interleukin Related STAT
  4. 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.

JAK1-IN-20

JAK1-IN-20 Chemical Structure

CAS No. : 3106963-85-0

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JAK1-IN-20 Related Antibodies

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JAK1 JAK2 JAK3 Tyk2 JAK

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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STAT3 STAT5 STAT6 STAT1

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Description

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[1].

IC50 & Target[1]

JAK1

<0.5 nM (IC50)

IL-6

 

STAT3

 

In Vitro

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.

JAK1-IN-20 Related Antibodies

Western Blot Analysis[1]

Cell Line: TF-1 cells, H9 cells
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)
Incubation Time: 1 h
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.
Parmacokinetics
Species Dose Route Plasma Concentration T1/2 AUC0-24 Vd CL Cmax Bioavailability
Rat[1] 1 mg/kg i.v. / 0.65 h 610 ng·h/mL 1.08 L/kg 27.5 mL/min/kg / /
Rat[1] 5 mg/kg p.o. / 1.3 h 254 ng·h/mL / / 167 ng/mL 8.3 %
Mice[1] 30 mg/kg p.o. <1 (0.5 h) ng/mL / / / / / /
In Vivo

JAK1-IN-20 (10-30 mg/kg; p.o.; daily) significantly ameliorates DSS-induced acute ulcerative colitis in female C57BL/6J mice, reducing disease activity, increasing colon length, suppressing pro-inflammatory cytokine production, and improving colonic histopathology[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J (female, 7-8 weeks old, DSS-induced ulcerative colitis)[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: p.o.; daily
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.
Molecular Weight

537.97

Formula

C26H25ClFN7O3
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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JAK1-IN-20 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JAK1-IN-203106963-85-0JAKInterleukin RelatedSTATJanus kinaseILJAK2Caco-2TF-1 cellsinflammatory bowel diseaseJAK3STAT3TYK2HEK-Blue IL-6 cellsC57BL/6J miceJAK1Inhibitorinhibitorinhibit

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