PTPN2-IN-2
PTPN2-IN-2 is a potent and orally active PTPN2 inhibitor (IC50 = 7.05 nM) that enhances the IFN-γ signaling pathway. PTPN2-IN-2 inhibits PTP1B with an IC50 of 9.88 nM. PTPN2-IN-2 inhibits tumor growth, promotes the activation and infiltration of tumor immune cells in a B16-OVA mouse model. PTPN2-IN-2 can be used for the research of melanoma.
For research use only. We do not sell to patients.
- CAS No.: 3093350-44-5
- Formula: C19H22FN5O5S
- Molecular Weight:451.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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PTPN2 7.05 nM (IC50) |
PTP1B 9.88 nM (IC50) |
PTPN2-IN-2 (compound K-38) (0-100 µM; 24 h) enhances the IFN-γ/JAK/STAT1 signaling pathway in Jurkat and B16 cells, as evidenced by increased STAT1 phosphorylation upon IFN-γ stimulation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat and B16 cells
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Concentration:0; 1; 10; 50; 100 µM
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Incubation Time:24 h
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Result:Induced an increase in STAT1 phosphorylation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C57BL/6J mice subcutaneously implanted with B16-OVA cells[1]
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Dosage:50; 100; 150 mg/kg
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Administration:p.o.; once daily for 24 days
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Result:Significantly inhibited the volume, proliferation rate and tumor weight of melanoma in mice.
Significantly enhanced the inhibitory activity of PD-1 on tumor growth.
Had no significant effect on the body weight.
Markly increased CD8+ T and CD45+ leukocyte infiltration in B16-OVA tumors.
Increased IFN-γ levels in tumor tissues.
Upreugalted PD-L1 and p-STAT1 levels.
Chemical Information
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CAS No. 3093350-44-5
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Molecular Weight 451.47
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Formula C19H22FN5O5S
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SMILES
FC1=C(C(O)=CC(C2=CNC(C(NC3CCCCCC3)=O)=N2)=C1)N4CC(NS4(=O)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)