2. Metabolic Enzyme/Protease Immunology/Inflammation JAK/STAT Signaling Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK
  3. Phosphatase IFNAR JAK STAT
  4. 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.

PTPN2-IN-2

PTPN2-IN-2 Chemical Structure

CAS No. : 3093350-44-5

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PTPN2-IN-2 Related Antibodies

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Description

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[1].

IC50 & Target[1]

PTPN2

7.05 nM (IC50)

PTP1B

9.88 nM (IC50)

In Vitro

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.

PTPN2-IN-2 Related Antibodies

Western Blot Analysis[1]

Cell Line: Jurkat and B16 cells
Concentration: 0; 1; 10; 50; 100 µM
Incubation Time: 24 h
Result: Induced an increase in STAT1 phosphorylation.
Parmacokinetics
Species Dose Route Cmax MRT0-∞ T1/2 AUC0-∞ Tmax F
Rat[1] 1 mg/kg i.v. 5416.68 ng/mL 0.17 h 0.69 h 252.23 ng·h/mL / /
Rat[1] 10 mg/kg i.g. 26.60 ng/mL 8.73 h 4.36 h 263.79 ng·h/mL 5.33 h 10.46 %
In Vivo

PTPN2-IN-2 (50-150 mg/kg; p.o.; once daily for 24 days) inhibits tumor growth via modulates IFN-γ signaling transduction in a B16-OVA mouse model[1].

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

Animal Model: Female C57BL/6J mice subcutaneously implanted with B16-OVA cells[1]
Dosage: 50; 100; 150 mg/kg
Administration: p.o.; once daily for 24 days
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.
Molecular Weight

451.47

Formula

C19H22FN5O5S
CAS No.
SMILES

FC1=C(C(O)=CC(C2=CNC(C(NC3CCCCCC3)=O)=N2)=C1)N4CC(NS4(=O)=O)=O
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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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PTPN2-IN-2 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:

PTPN2-IN-23093350-44-5PhosphataseIFNARJAKSTATInterferon-α/β receptorInterferon-alpha/beta receptor Janus kinasePTPN2,PTPN2 inhibitor,therapeutic target,compound,PTPN2-targeted therapeutics,inhibitor,K-38,melanomaInhibitorinhibitorinhibit

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