2. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt Metabolic Enzyme/Protease
  3. JAK Tyrosinase
  4. JAK3-IN-18

JAK3-IN-18 是一种选择性且口服有效的 JAK3 和 TEC 双靶点抑制剂，IC50 分别为 0.5391 nM 和 12.40 nM。JAK3-IN-18 对 AK1、AK2 和 TYk2 有卓越选择性，选择性比率超过 10,000倍。JAK3-IN-18 在实验性自身免疫性脑脊髓炎小鼠模型中展现出卓越的治疗效果。JAK3-IN-18 可用于多发性硬化症的研究。

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JAK3-IN-18

JAK3-IN-18 Chemical Structure

CAS No. : 2914873-59-7

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JAK3-IN-18 相关抗体

Top Publications Citing Use of Products

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

JAK3-IN-18 is an orally active JAK3 and TEC inhibitor, with IC50s of 0.5391 nM and 12.40 nM, respectively. JAK3-IN-18 demonstrates outstanding selectivity over AK1, AK2, and TYk2, with selectivity ratios exceeding 10,000-fold. JAK3-IN-18 demonstrates excellent therapeutic efficacy in the experimental autoimmune encephalomyelitis (EAE) mouse model. JAK3-IN-18 can be used for the study of multiple sclerosis[1].

IC50 & Target[1]

JAK3

0.5391 nM (IC50)

JAK1

8575 nM (IC50)

JAK2

7431 nM (IC50)

体外研究
(In Vitro)

JAK3-IN-18 (Compound 8a) (1-100000 nM, 80 min) 在 IL-15 刺激的人全血实验中抑制 p-STAT5 的 IC50 值为 177.8 nM[1]。
JAK3-IN-18 (1 μM, 135 min) 在针对 310 种激酶的检测中仅对除 JAK3 和 TEC 外的 11 种激酶表现出超过 60% 的抑制作用[1]。
JAK3-IN-18 (10 μM, 0-60 min) 显示出良好的 GSH 稳定性，并具有良好的类药物特性[1]。

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

JAK3-IN-18 相关抗体:
体内研究
(In Vivo)

JAK3-IN-18 (Compound 8a) (10-100 mg/kg，口服，每日两次，持续 24 天) 在多发性硬化症的实验性自身免疫性脑脊髓炎 (EAE) 小鼠模型中显示出卓越的治疗效果[1]。

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

Animal Model: Experimental autoimmune encephalomyelitis (EAE) mice (6-8 weeks)[1]
Dosage: 10, 100 mg/kg
Administration: p.o. twice daily for 24 days
Result: Decreased the clinical scores.
Showed no body weight loss.
分子量

337.35

Formula

C18H16FN5O
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

JAK3-IN-18 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

JAK3-IN-182914873-59-7JAKTyrosinaseJanus kinasemultiple sclerosisexperimental autoimmune encephalomyelitis (EAE)JAK3Inhibitorinhibitorinhibit

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