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

Tyk2-IN-23 是一种强效的，具有口服活性的选择性 TYK2 抑制剂 (IC50 = 18 nM) ，对 JAK1/2/3 亚型的选择性超过 70 倍。Tyk2-IN-23 能有效抑制 IFN-α 和 IL-10 激活的 TYK2 依赖性信号通路中的 p-STAT3。Tyk2-IN-23 还能有效抑制 H9 细胞中 IFN-α 诱导的 STAT1 磷酸化。Tyk2-IN-23 可用于斑秃和过敏性鼻炎的研究。

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Tyk2-IN-23

Tyk2-IN-23 Chemical Structure

CAS No. : 2734918-75-1

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Tyk2-IN-23 相关抗体

Top Publications Citing Use of Products

查看 JAK 亚型特异性产品:

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JAK1 JAK2 JAK3 Tyk2 JAK

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STAT3 STAT5 STAT6 STAT1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

Tyk2-IN-23 (Compound 29i) (50 nM-10 μM，80 分钟) 能有效抑制 IFN-α (IC50 = 230.6 nM) 和 IL-10 (IC50 = 501.6 nM) 激活的 TYK2 依赖性信号通路中的 p-STAT3，但 IL-21、IL-23 或 IL-27 诱导的 p-STAT3 在人外周血单核细胞 (hPBMC) 中仅表现出轻微的抑制作用 (IC50 > 2700 nM)[1]。
Tyk2-IN-23 (0-10 μM，1.5 小时) 能有效抑制 H9 细胞中 IFN-α 诱导的 STAT1 磷酸化；相反，即使在 10000 nM 的浓度下，GM-CSF 诱导的 STAT5 磷酸化 (JAK2 依赖性)、IL-4 诱导的 STAT6 磷酸化 (JAK1/JAK3 介导) 和 IL-6 诱导的 STAT3 磷酸化 (JAK1/JAK2/TYK2 协同) 也未受影响[1]。
Tyk2-IN-23 (0.625-40 μM，24 小时) 在浓度 ≤ 10 μM 时对 RBL-2H3 细胞无细胞毒性[1]。
Tyk2-IN-23 (0-5 μM，30 分钟) 浓度依赖性地抑制 Compound 48/80 trihydrochloride (HY-130592) (C48/80) 诱导的 RBL-2H3 细胞释放 β-己糖胺酶[1]。

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

Tyk2-IN-23 相关抗体:

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.
体内研究
(In Vivo)

Tyk2-IN-23 (Compound 29i) (15-40 mg/kg，鼻内滴剂或口服灌胃，每日一次，8-26 天) 能有效缓解小鼠斑秃 (AR) 和过敏性鼻炎 (AA) 的症状，且无明显毒性[1]。

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.
分子量

495.98

Formula

C26H27ClFN5O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Tyk2-IN-23 相关分类

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  • 稀释计算器

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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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