2. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt
  3. JAK STAT
  4. JAK2-IN-15

JAK2-IN-15 是一种口服有效的强效选择性 JAK2 抑制剂 (IC50 = 1.17 nM)。JAK2-IN-15 可抑制 AK2-STAT 信号通路。在重组人促红素 (rhEPO) 诱导的小鼠模型中，JAK2-IN-15 可显著改善血细胞比容和脾肿大等关键病理指标。JAK2-IN-15 可用于真性红细胞增多症 (PV) 的研究。

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JAK2-IN-15

JAK2-IN-15 Chemical Structure

CAS No. : 3094174-82-7

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JAK2-IN-15 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

查看 STAT 亚型特异性产品:

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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

JAK2-IN-15 is an orally active, potent, selective JAK2 inhibitor (IC50 = 1.17 nM). JAK2-IN-15 can inhibit the AK2-STAT signaling pathway. JAK2-IN-15 significantly improves key pathological indicators such as hematocrit and splenomegaly in an Epoetin beta (HY-114134) (rhEPO)-induced mouse model. JAK2-IN-15 can be used for the study of Polycythemia Vera (PV)[1].

IC50 & Target

JAK2

1.17 nM (IC50)

体外研究
(In Vitro)

JAK2-IN-15 (Compound 2) 表现出强效的 JAK2 抑制活性 (IC50 = 1.17 nM)[1]。
JAK2-IN-15 (72 小时) 能有效抑制携带 JAK2V617F 突变的 HEL (IC50 = 1.88 μM) 和 SET-2 (IC50 = 9.56 μM) 细胞的增殖[1]。
JAK2-IN-15 (0.3-10 μM，72 小时) 通过剂量依赖性地抑制 JAK2-STAT 信号通路，对携带 JAK2V617F 突变的 HEL 和 SET-2 细胞表现出显著的抗增殖活性[1]。
JAK2-IN-15 (100 μM) 仅抑制 17 种野生型激酶，表现出很强的选择性[1]。

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

JAK2-IN-15 相关抗体:

Western Blot Analysis[1]

Cell Line: HEL 92.1.7 cells, SET-2
Concentration: 0.3 μM, 1 μM, 3 μM, 10 μM
Incubation Time: 4 h
Result: Effectively inhibited phosphorylation of JAK2 (Y1007/8 site), STAT3, STAT5, AKT and ERK.
体内研究
(In Vivo)

JAK2-IN-15 (Compound 2) (25-75 mg/kg，口服，每日一次，持续 4 天) 在 rhEPO 诱导的红细胞增多症小鼠模型中表现出显著的治疗效果，剂量依赖性地抑制脾肿大、血细胞比容和网织红细胞增多，且具有良好的安全性[1]。

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

Animal Model: A model of polycythemia and splenomegaly was created using female BALB/c mice (8-10 weeks old, weighing 17-20 g) by subcutaneous injection of 10 units of recombinant human erythropoietin (rhEPO) daily for 4 consecutive days[1].
Dosage: 25 mg/kg, 50 mg/kg, 75 mg/kg
Administration: P.o., once daily for 4 days
Result: Spleen weight decreased.
Dose-dependent inhibition of hematocrit.
Reduction of rhEPO-induced reticulocyte proliferation.
Inhibition of Ter119/CD71 erythroblast expansion in the spleen and bone marrow.
No significant effect on white blood cell count or body weight.
分子量

517.62

Formula

C29H35N5O4
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

JAK2-IN-15 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:

JAK2-IN-153094174-82-7JAKSTATJanus kinaseMacrocyclic compoundsDeep learning modelsDrug designCycleGPTInhibitorinhibitorinhibit

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