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

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.

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JAK2-IN-20

JAK2-IN-20 Chemical Structure

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JAK2-IN-20 Related Antibodies

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Description

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)

In Vitro

JAK2-IN-20 (compound 4B) potently protects MDCK cells against damage induced by H1N1 influenza virus (EC50=14.71 nM) and inhibits the cap-binding activity of influenza A PB2 protein (IC50=3.337 nM)[1].
JAK2-IN-20 exhibits low cytotoxicity in multiple cell lines, with a CC50 of >100 μM (48 h) in MDCK cells[1].
JAK2-IN-20 (1 μM; 60 min; 37°C) exhibits excellent metabolic stability in mouse liver microsomes, with a half-life of 47.8 min and an intrinsic clearance (CLint) of 29.0 μL/min/mg[1].
JAK2-IN-20 (250-2000 nM) binds directly to the cap-binding domain of influenza A virus PB2, with a Kd value of 2.82 μM[1].
JAK2-IN-20 (5-10 μM; 30 min; 6 h) dose-dependently inhibits LPS (1 μg/mL)-induced expression of pro-inflammatory cytokines (IL-6, IL-1β) and IFN-β in RAW 264.7 macrophages, and exhibits potent activity at 10 μM[1].
JAK2-IN-20 (5-10 μM; 30 min; 6 h) potently inhibits the expression of poly (I:C)-induced proinflammatory cytokines (IL-6, TNF-α) and type I interferons (IFN-α, IFN-β) in RAW 264.7 macrophages at a concentration of 10 μM[1].
JAK2-IN-20 (250-500 nM; 24 h) inhibits the expression of H1N1 virus PB2 mRNA and reduces the levels of virus-induced proinflammatory cytokines (IL-6, TNF-α) in A549 cells at a concentration of 500 nM[1].
JAK2-IN-20 inhibits the JAK/STAT signaling pathway in both H1N1-infected A549 cells and IFN-β-stimulated THP-1 cells by reducing the phosphorylation levels of STAT1 and STAT3[1].

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

JAK2-IN-20 Related Antibodies

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.
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 %
In Vivo

JAK2-IN-20 (compound 4B) (3-30 mg/kg; i.v., p.o.; single dose) exhibits favorable pharmacokinetic properties in CD-1 mice, including nearly complete oral bioavailability (99.4%) following a single 30 mg/kg oral dose and measurable systemic exposure following a single 3 mg/kg intravenous dose[1].

MedChemExpress (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.
Molecular Weight

333.34

Formula

C16H17F2N5O
SMILES

FC1=CC(C(C2=NC(N[C@@H](C)C(C)(C)O)=C(F)C=N2)=CN3)=C3N=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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JAK2-IN-20 Related Classifications

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

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