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

JAK1/TYK2-IN-3 是一种有效的，选择性和口服活性的双重 TYK2/JAK1 抑制剂，IC50 值分别为 6 和 37 nM。JAK1/TYK2-IN-3 选择性的作用于 JAK2 (IC50=140 nM) 和 JAK3 (IC50=362 nM)。JAK1/TYK2-IN-3 通过调节 TYK2/JAK1 相关基因的表达以及 Th1 、Th2 和 Th17 细胞的形成来发挥抗炎作用。

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JAK1/TYK2-IN-3

JAK1/TYK2-IN-3 Chemical Structure

CAS No. : 2734918-37-5

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JAK1/TYK2-IN-3 相关抗体

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查看 JAK 亚型特异性产品:

查看所有亚型
JAK1 JAK2 JAK3 Tyk2 JAK

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
H9c2 IC50
13.4 μM
Compound: 48
Cytotoxicity against rat H9C2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Cytotoxicity against rat H9C2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 35113547]
HUVEC IC50
76.7 μM
Compound: 48
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 35113547]
L02 IC50
146.9 μM
Compound: 48
Cytotoxicity against human LO2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Cytotoxicity against human LO2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 35113547]
体外研究
(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].

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

JAK1/TYK2-IN-3 相关抗体:
体内研究
(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

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.
分子量

377.39

Formula

C17H21F2N7O
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

JAK1/TYK2-IN-3 相关分类

  • 摩尔计算器

  • 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:

JAK1/TYK2-IN-32734918-37-5JAKJanus kinaseorally activeanti-inflammatoryulcerative colitisselectiveInflammatory Bowel DiseaseInhibitorinhibitorinhibit

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