2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. JAK STAT
  4. 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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Tyk2-IN-23

Tyk2-IN-23 Chemical Structure

CAS No. : 2734918-75-1

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Tyk2-IN-23 Related Antibodies

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Description

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[1].

In Vitro

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.

Tyk2-IN-23 Related Antibodies

Cell Viability Assay[1]

Cell Line: RBL-2H3 cells
Concentration: 0.625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM
Incubation Time: 24 h
Result: Showed no cytotoxicity at concentrations ≤ 10 μM in RBL-2H3 cells.

Western Blot Analysis[1]

Cell Line: H9 cells, THP-1 cells, TF-1 cells
Concentration: 10 nM, 50 nM, 100 nM, 500 nM, 1000 nM, 5000 nM, 10000 nM
Incubation Time: Preincubated for 1h, then stimulated by IFN-α (1,000 U/mL) for 30 min
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.
In Vivo

Tyk2-IN-23 (Compound 29i) (15-40 mg/kg, intranasal drops or oral gavage, once daily, 8-26 days) effectively relieves the symptoms of Alopecia areata (AR) and Allergic Rhinitis (AA) in mice without showing significant toxicity[1].

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

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].
Dosage: 20 mg/kg, 40 mg/kg
Administration: Intranasal drops, once daily for 8 days
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.
Animal Model: Using female C57BL/6J mice (6-8 weeks old), Alopecia areata (AA) was induced by hair removal and cyclophosphamide injection[1].
Dosage: 15 mg/kg, 30 mg/kg
Administration: Oral gavage, once daily for 26 days
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.
Molecular Weight

495.98

Formula

C26H27ClFN5O2
CAS No.
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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References
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Tyk2-IN-23 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:

Tyk2-IN-232734918-75-1JAKSTATJanus kinaseJAK-STAT Signaling PathwayAllergic Rhinitis (AR) ModelAlopecia Areata (AA) ModelInhibitorinhibitorinhibit

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