1. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  2. JAK
  3. JAK1/TYK2-IN-3

JAK1/TYK2-IN-3 is a potent, selective and orally active dual TYK2/JAK1 inhibitor with IC50 values of 6 and 37 nM, respectively. JAK1/TYK2-IN-3 also shows selectively relative to JAK2 (IC50=140 nM) and JAK3 (IC50=362 nM). JAK1/TYK2-IN-3 shows anti-inflammatory effect by regulating the expression of related TYK2/JAK1-regulated genes, as well as the formation of Th1, Th2, and Th17 cells.

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JAK1/TYK2-IN-3 Chemical Structure

JAK1/TYK2-IN-3 Chemical Structure

CAS No. : 2734918-37-5

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Description

JAK1/TYK2-IN-3 is a potent, selective and orally active dual TYK2/JAK1 inhibitor with IC50 values of 6 and 37 nM, respectively. JAK1/TYK2-IN-3 also shows selectively relative to JAK2 (IC50=140 nM) and JAK3 (IC50=362 nM). JAK1/TYK2-IN-3 shows anti-inflammatory effect by regulating the expression of related TYK2/JAK1-regulated genes, as well as the formation of Th1, Th2, and Th17 cells[1].

IC50 & Target

Tyk2

6 nM (IC50)

JAK1

37 nM (IC50)

JAK2

140 nM (IC50)

JAK3

362 nM (IC50)

In Vitro

JAK1/TYK2-IN-3 (compound 48) (10, 20, 30 mg/kg) shows anti-inflammatory effect by regulating the formation of Th1, Th2, Th17 cells[1].
JAK1/TYK2-IN-3 (10, 20, 30 mg/kg) inhibits the NF-κB signaling pathway by inhibits the JAK-STAT pathway, thereby reducing the inflammatory response in ulcerative colitis (UC) mice[1].
JAK1/TYK2-IN-3 (10, 20, 30 mg/kg) dose-dependently inhibits the mRNA expression of TNF-α, IL-1β, IL-12, IL-17A, IL-22, IFN-α, and IFN-β[1].

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

In Vivo

JAK1/TYK2-IN-3 (10, 20, 30 mg/kg; p.o.; twice a day for 12 days) shows a good therapeutic effect on ulcerative colitis (UC)[1].
JAK1/TYK2-IN-3 (5 mg/kg, p.o.) shows 23.7% oral bioavailability in rats[1].
Pharmacokinetic Parameters of JAK1/TYK2-IN-3 in male Sprague-Dawley rats[1].

compd dose(mg/kg) Administration Cmax(ng/mL) Cl (Lh-1kg-1) T1/2(h) AUC0-t(ng·h/mL) F (%)
48 5 mg/kg p.o. 400.4±55.3 11.3±5.2 2.4±2.1 440.9±157.0 23.7

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

Animal Model: 6-8 weeks, 270-325g male Sprague-Dawley rats[1]
Dosage: 5 mg/kg
Administration: p.o.
Result: Showed 23.7% oral bioavailability in rats.
Animal Model: Six-eight week old male C57BL/6 mice, 20-22 g (2.5% dextran sulfate sodium (DSS)-induced acute UC mouse model)[1]
Dosage: 10, 20, 30 mg/kg
Administration: p.o., twice a day, 12 days
Result: Improved the infiltration of inflammatory factors and reduced the damage caused by DSS.
Molecular Weight

377.39

Formula

C17H21F2N7O

CAS No.
SMILES

O=C1NCCC12CCN(C3=NC(NC4=CN(C(F)F)N=C4)=NC=C3C)CC2

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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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    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.

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JAK1/TYK2-IN-3
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