2. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt Anti-infection
  3. JAK Influenza Virus
  4. JAK2-IN-20

JAK2-IN-20 是一种口服有效、靶向 JAK2 激酶 (IC50=49.17 nM) 与甲型流感病毒 PB2 蛋白 (IC50=3.337 μM, Kd=2.82 μM) 的双重抑制剂。JAK2-IN-20 通过降低 STAT1 和 STAT3 的磷酸化水平有效阻断 JAK/STAT 信号通路，进而抑制病毒复制并下调病毒 NP 及 PB2 蛋白的表达。此外，JAK2-IN-20 在炎症及流感感染模型中能显著抑制 IL-6、TNF-α 和 IFN-β 等关键炎症因子的 mRNA 表达。JAK2-IN-20 是甲型流感病毒感染及相关病理研究的重要工具分子。

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JAK2-IN-20

JAK2-IN-20 Chemical Structure

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JAK2-IN-20 相关抗体

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JAK1 JAK2 JAK3 Tyk2 JAK

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JAK2-IN-20 is an orally active dual inhibitor targeting JAK2 kinase (IC50=49.17 nM) and influenza A virus PB2 protein (IC50=3.337 μM, Kd=2.82 μM). JAK2-IN-20 effectively blocks the JAK/STAT signaling pathway by reducing the phosphorylation levels of STAT1 and STAT3, thereby inhibiting viral replication and downregulating the expression of viral NP and PB2 proteins. In addition, JAK2-IN-20 significantly inhibits the mRNA expression of key inflammatory cytokines such as IL-6, TNF-α and IFN-β in inflammation and influenza infection models. JAK2-IN-20 serves as an important tool molecule for the study of influenza A virus infection and related pathologies[1].
IC50 & Target

JAK2

49.17 nM (IC50)

体外研究
(In Vitro)

JAK2-IN-20 (compound 4B) 可强效保护 MDCK 细胞免受 H1N1 流感病毒诱导的损伤 (EC50=14.71 nM)，抑制甲型流感 PB2 蛋白的帽结合活性 (IC50=3.337 nM)[1]。
JAK2-IN-20 在多种细胞系中表现出低细胞毒性，在 MDCK 细胞中的 CC50 >100 μM (48 h)[1]。
JAK2-IN-20 (1 μM; 60 min; 37°C) 在小鼠肝微粒体中具有优异的代谢稳定性，半衰期为 47.8 min，固有清除率 (CLint) 为 29.0 μL/min/mg[1]。
JAK2-IN-20 (250-2000 nM) 可直接与甲型流感病毒 PB2 帽结合域结合，其 Kd 值为 2.82 μM[1]。
JAK2-IN-20 (5-10 μM; 30 min; 6 h) 可剂量依赖性地抑制 RAW 264.7 巨噬细胞中 LPS (1 μg/mL) 诱导的促炎细胞因子 (IL-6、IL-1β) 及 IFN-β 的表达，在 10 μM 时具有强效活性[1]。
JAK2-IN-20 (5-10 μM; 30 min; 6 h) 可在 10 μM 浓度下强效抑制 RAW 264.7 巨噬细胞中由 poly (I:C) 诱导的促炎细胞因子 (IL-6、TNF-α) 及 I 型干扰素 (IFN-α、IFN-β) 的表达[1]。
JAK2-IN-20 (250-500 nM; 24 h) 可抑制 H1N1 病毒 PB2 mRNA 的表达，并在 500 nM 浓度下降低 A549 细胞中病毒诱导的促炎细胞因子 (IL-6、TNF-α) 水平[1]。
JAK2-IN-20 通过降低 STAT1 和 STAT3 的磷酸化水平，在 H1N1 感染的 A549 细胞和 IFN-β 刺激的 THP-1 细胞中均抑制 JAK/STAT 信号通路[1]。

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

JAK2-IN-20 相关抗体:

Real Time qPCR[1]

Cell Line: LPS-induced RAW 264.7 macrophages
Concentration: 5 μM, 10 μM
Incubation Time: 30 min pre-LPS stimulation; 6 h post-stimulation
Result: Reduced LPS-induced IL-6 mRNA levels by 1.5-fold, IL-1β mRNA levels by 6.3-fold, and IFN-β mRNA levels by 83% at 10 μM.
Reduced IFN-β mRNA levels by 55% at 5 μM, with attenuated effects on IL-6 and IL-1β.

Real Time qPCR[1]

Cell Line: Poly(I:C)-induced RAW 264.7 macrophages
Concentration: 5 μM, 10 μM
Incubation Time: 30 min pre-poly(I:C) stimulation; 6 h post-stimulation
Result: Reduced poly(I:C)-induced IL-6 mRNA levels by 4.8-fold, TNF-α mRNA levels by 3.0-fold, IFN-β mRNA levels by 44-fold, and IFN-α mRNA levels by 1.8-fold at 10 μM.

Real Time qPCR[1]

Cell Line: H1N1-induced A549 cells
Concentration: 250 nM, 500 nM
Incubation Time: 24 h (added 1-2 h post-H1N1 infection)
Result: Reduced H1N1-induced PB2 mRNA expression by 67%, IL-6 mRNA levels by 5.2-fold, and TNF-α mRNA levels by 2.5-fold at 500 nM, with moderate inhibition of IFN-α and IFN-β.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Cmax AUC0-t MRT0-t Vz CL F
Mice[1] 3 mg/kg i.v. 0.505 h 1903 ng/mL 751 ng·h/mL 0.293 h 2929 mL/kg 4011 mL/h/kg /
Mice[1] 30 mg/kg p.o. 1.44 h 3513 ng/mL 7422 ng·h/mL 1.56 h / / 99.4 %
体内研究
(In Vivo)

JAK2-IN-20 (3-30 mg/kg; i.v., p.o.; 单次) 在 CD-1 小鼠中表现出良好的药代动力学特性，包括单次口服 30 mg/kg 剂量后近乎完全的口服生物利用度 (99.4%)，以及单次静脉注射 3 mg/kg 剂量后可检测到的全身暴露量[1]。

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

Animal Model: CD-1[1]
Dosage: 3 mg/kg (i.v.); 30 mg/kg (p.o.)
Administration: i.v.; single dose; p.o.; single dose
Result: Achieved a Cmax of 1903 ng/mL, AUC0-t of 751 h ng/mL, T1/2 of 0.505 h, MRT0-t of 0.293 h, Vz of 2929 mL/kg, and Cl of 4011 mL/h/kg following intravenous administration.
Achieved a Cmax of 3513 ng/mL, AUC0-t of 7422 h ng/mL, T1/2 of 1.44 h, MRT0-t of 1.56 h, and oral bioavailability of 99.4% following oral administration.
分子量

333.34

Formula

C16H17F2N5O
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-20 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:

JAK2-IN-20JAKInfluenza VirusJanus kinaseH1N1 influenza virusMDCK cellsInfluenza A virus PB2 proteinSTAT1JAK/STAT signalingSTAT3JAK2 kinaseA549 cellsmiceRAW 264.7 macrophagesInhibitorinhibitorinhibit

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