PTPN22-IN-3
PTPN22-IN-3 is a potent, selective, and orally active inhibitor of PTPN22 with an IC50 of 0.49 μM and a Ki of 0.28 μM. PTPN22-IN-3 exhibits over 14-fold selectivity against a broad panel of PTPs and shows no significant inhibition against SRC/CSK kinases or IDO1/Arginase metalloenzymes. PTPN22-IN-3 enhances TCR signaling, increases IL-2 expression and secretion, and promotes mouse splenic T cell proliferation. In immune-competent C57BL/6J mice, PTPN22-IN-3 suppresses MC38 syngeneic tumor growth and synergizes with Pembrolizumab (anti-PD-1) (HY-P9902A) therapy. PTPN22-IN-3 can be used for the study of colorectal cancer and other solid tumors responsive to T cell-mediated anti-tumor immunity.
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- Formule: C28H25N3O6
- Masse moléculaire:499.51
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Chemical Information
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Activité biologique
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IL-2 |
PTPN22-IN-3 (0-25 μM; 3-60 min) shows over 14-fold selectivity for PTPN22 over SHP-2 (IC50 = 7.11 μM), over 47-fold selectivity over PTP1B (IC50 = 23.43 μM), and over 51-fold selectivity over TCPTP (IC50 > 25 μM), shows no inhibition against PTP-MEG2, STEP, PTP-PEST, PTPα, PTPε, PTPγ, PPK, Laforin, CDC14A, or CD45 at concentrations up to 25 μM[1].
PTPN22-IN-3 (1-10 μM; 30 min) exhibits no detectable inhibition against kinases SRC or CSK at concentrations up to 10 μM, and shows no inhibitory activity against metalloenzymes IDO1 or Arginase at 5 μM[1].
PTPN22-IN-3 (10 μM; 1 h) enhances anti-CD3-induced phosphorylation of LCK (Y394) and ERK1/2 (T202/Y204) in Jurkat T cells[1].
PTPN22-IN-3 (1-10 μM; 1 h) increases LCK and ERK1/2 phosphorylation levels in Jurkat T cells in a dose-dependent manner[1].
PTPN22-IN-3 (10 μM; 1 h) enhances anti-CD28-mediated IL-2 expression and IL-2 secretion in Jurkat T cells[1].
PTPN22-IN-3 (10 μM; 24 h) promotes mouse splenic T cell proliferation[1].
PTPN22-IN-3 (up to 30 μM; 24 h) shows no observable cytotoxicity in HEK293 cells[1].
PTPN22-IN-3 (up to 10 μM; 24 h) does not impair the growth of MC38 tumor cells or murine splenic T cells in CCK8 cytotoxicity assays[1].
PTPN22-IN-3 (0-100 μM; 60 min) shows an IC50 of 0.53 μM against PTPN22 in the presence of Triton X-100 in the assay buffer[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat T cells
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Concentration:10 μM
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Incubation Time:1 h
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Result:Enhanced anti-CD3-induced phosphorylation of LCK (Y394) and ERK1/2 (T202/Y204).
Enhanced anti-CD28-mediated IL-2 expression.
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Cell Line:Jurkat T cells
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Concentration:1, 5, 10 μM
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Incubation Time:1 h
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Result:Increased LCK and ERK1/2 phosphorylation in a dose-dependent manner.
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Cell Line:Mouse splenic T cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Promoted mouse splenic T cell proliferation.
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Cell Line:HEK293 cells
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Concentration:Up to 30 μM
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Incubation Time:24 h
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Result:Showed no observable cytotoxicity at up to 30 μM.
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Cell Line:MC38 cells, mouse splenic T cells
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Concentration:1, 5, 10 μM
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Incubation Time:24 h
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Result:Did not impair the growth of MC38 tumor cells or murine splenic T cells.
PTPN22-IN-3 (10 mg/kg; i.p.; once daily for 2 weeks) significantly inhibits MC38 tumor growth by approximately 53% in immune-competent C57BL/6J mice[1].
PTPN22-IN-3 (10 mg/kg; i.p.; once daily for ten consecutive days) shows no efficacy against MC38 tumor growth in immune-deficient NRG mice[1].
PTPN22-IN-3 (10 mg/kg; i.p.; twice daily for five consecutive days per week for 2 weeks) synergizes with Anti-Mouse PD-1 Antibody (RMP1-14, anti-PD-1) (HY-P99144) in MC38 tumor-bearing C57BL/6J mice[1].
PTPN22-IN-3 (10 mg/kg; i.p.; once daily for 2 weeks) in MC38 tumor-bearing C57BL/6J mice increases CD45+ immune cell infiltration, CD3+ T cell infiltration, CD4+ and CD8+ T cell populations, activates CD8+ T cells and NK cells (increased CD69 expression), and induces higher PD-1 expression on CD8+ T cells in the tumor microenvironment, consistent with a phenotypic shift associated with T cell activation[1].
PTPN22-IN-3 (up to 100 mg/kg; i.p.; once daily for 5 days) shows no signs of toxicity in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Immune-competent C57BL/6J mice (12 weeks old, both sexes)[1]
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Dosage:10 mg/kg
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Administration:i.p.; twice daily for five consecutive days per week for 2 weeks
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Result:Reduced MC38 tumor volume by approximately 83%.
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Animal Model:Immune-competent C57BL/6J mice (12 weeks old, both sexes)[1]
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Dosage:10 mg/kg
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Administration:i.p.; once daily for 2 weeks
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Result:Inhibited MC38 tumor growth by approximately 53%.
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Animal Model:Immune-deficient NRG mice (12 weeks old, females)[1]
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Dosage:10 mg/kg
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Administration:i.p.; once daily for ten consecutive days
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Result:Showed no efficacy against MC38 tumor growth.
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Animal Model:MC38 tumor-bearing C57BL/6J mice (12 weeks old, both sexes)[1]
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Dosage:10 mg/kg
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Administration:i.p.; twice daily for five consecutive days per week for 2 weeks
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Result:Synergized with anti-PD-1 antibody.
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Animal Model:MC38 tumor-bearing C57BL/6J mice (12 weeks old, both sexes)[1]
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Dosage:10 mg/kg
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Administration:i.p.; once daily for 2 weeks
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Result:Increased CD45+ immune cell infiltration, CD3+ T cell infiltration, CD4+ and CD8+ T cell populations, activates CD8+ T cells and NK cells (increased CD69 expression), and induces higher PD-1 expression on CD8+ T cells in the tumor microenvironment, consistent with a phenotypic shift associated with T cell activation.
Chemical Information
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Masse moléculaire 499.51
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Formule C28H25N3O6
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SMILES
O=C1C(C(O)=O)=CNC2=CC=C(C=C21)NC([C@@H](NC(C3=C(C=C(C=C3)C4=CC=C(C=C4)CC)O)=O)C)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PTPN22-IN-3 Related Classifications
HY-184931 Related Classifications
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