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Art. -Nr.: HY-184931

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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 K_i 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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Formel: C₂₈H₂₅N₃O₆
Molecular Weight:499.51

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

PTPN22-IN-3 Chemical Structure

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

IL-2

Alle Interleukin Related Isoform-spezifische Produkte anzeigen :

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

Jurkat T cells
Concentration:

10 μM
Incubation Time:

1 h
Result:

Enhanced anti-CD3-induced phosphorylation of LCK (Y394) and ERK1/2 (T202/Y204).
Enhanced anti-CD28-mediated IL-2 expression.

Western Blot Analysis^[1]

Cell Line:

Jurkat T cells
Concentration:

1, 5, 10 μM
Incubation Time:

1 h
Result:

Increased LCK and ERK1/2 phosphorylation in a dose-dependent manner.

Cell Proliferation Assay^[1]

Cell Line:

Mouse splenic T cells
Concentration:

10 μM
Incubation Time:

24 h
Result:

Promoted mouse splenic T cell proliferation.

Cell Cytotoxicity Assay^[1]

Cell Line:

HEK293 cells
Concentration:

Up to 30 μM
Incubation Time:

24 h
Result:

Showed no observable cytotoxicity at up to 30 μM.

Cell Cytotoxicity Assay^[1]

Cell Line:

MC38 cells, mouse splenic T cells
Concentration:

1, 5, 10 μM
Incubation Time:

24 h
Result:

Did not impair the growth of MC38 tumor cells or murine splenic T cells.

Parmacokinetics

Species	Dose	Route	AUC	C_max	T_1/2	T_max	F
Mice^[1]	10 mg/kg	i.p.	15.37 μM·h	2.31 μM	4.73 h	/	/
Mice^[1]	10 mg/kg	p.o.	/	0.29 μM	/	1 h	50.4 %

In Vivo

PTPN22-IN-3 (compound L-32) (10 mg/kg; i.p.; twice daily for five consecutive days per week for 2 weeks) reduces MC38 tumor volume by approximately 83% in immune-competent C57BL/6J mice^[1].
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.

Animal Model:

Immune-competent C57BL/6J mice (12 weeks old, both sexes)^[1]
Dosage:

10 mg/kg
Administration:

i.p.; twice daily for five consecutive days per week for 2 weeks
Result:

Reduced MC38 tumor volume by approximately 83%.

Animal Model:

Immune-competent C57BL/6J mice (12 weeks old, both sexes)^[1]
Dosage:

10 mg/kg
Administration:

i.p.; once daily for 2 weeks
Result:

Inhibited MC38 tumor growth by approximately 53%.

Animal Model:

Immune-deficient NRG mice (12 weeks old, females)^[1]
Dosage:

10 mg/kg
Administration:

i.p.; once daily for ten consecutive days
Result:

Showed no efficacy against MC38 tumor growth.

Animal Model:

MC38 tumor-bearing C57BL/6J mice (12 weeks old, both sexes)^[1]
Dosage:

10 mg/kg
Administration:

i.p.; twice daily for five consecutive days per week for 2 weeks
Result:

Synergized with anti-PD-1 antibody.

Animal Model:

MC38 tumor-bearing C57BL/6J mice (12 weeks old, both sexes)^[1]
Dosage:

10 mg/kg
Administration:

i.p.; once daily for 2 weeks
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

Molecular Weight 499.51
Formel C₂₈H₂₅N₃O₆
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Lin J, et al. A Potent and Selective Quinolone-Based PTPN22 Inhibitor with Improved Immunotherapeutic Activity. J Med Chem. 2026 Jul 23;69(14):16401-16427. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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Art. -Nr.:
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PTPN22-IN-3

Alle Interleukin Related Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

PTPN22-IN-3 Related Classifications

HY-184931 Related Classifications