1. Immunology/Inflammation Protein Tyrosine Kinase/RTK JAK/STAT Signaling Epigenetics Stem Cell/Wnt
  2. PD-1/PD-L1 JAK
  3. PJ27

PJ27 is a dual PD-1/PD-L1/JAK1 inhibitor, with an IC50 of 414 nM against PD-1/PD-L1, an IC50 of 786 nM against JAK1, a Ka of 294 nM for human PD-1/PD-L1, and a Ka of 473 nM for murine PD-1/PD-L1. PJ27 promotes the infiltration of CD3+CD8+ and CD3+CD4+ cells into the tumor microenvironment and exerts a significant immune activation effect. PJ27 inhibits tumor growth in a dose-dependent manner in the LLC lung cancer mouse model. PJ27 is applicable to relevant research on lung cancer.

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PJ27

PJ27 Chemical Structure

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Description

PJ27 is a dual PD-1/PD-L1/JAK1 inhibitor, with an IC50 of 414 nM against PD-1/PD-L1, an IC50 of 786 nM against JAK1, a Ka of 294 nM for human PD-1/PD-L1, and a Ka of 473 nM for murine PD-1/PD-L1. PJ27 promotes the infiltration of CD3+CD8+ and CD3+CD4+ cells into the tumor microenvironment and exerts a significant immune activation effect. PJ27 inhibits tumor growth in a dose-dependent manner in the LLC lung cancer mouse model. PJ27 is applicable to relevant research on lung cancer[1].

IC50 & Target

JAK3

786 nM (IC50)

In Vitro

PJ27 (0.125-2 μM; 48 h) enhances Jurkat T cell-mediated killing of PD-L1-expressing A549 cells, with significant A549 viability reduction at 2 μM in co-culture[1].
PJ27 binds to human and murine PD-L1 with comparable affinity, with Kd values of 294 nM and 473 nM respectively[1].

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

Cell Viability Assay[1]

Cell Line: A549, Jurkat T cells
Concentration: 0, 0.125, 0.25, 0.5, 1, 2 μM
Incubation Time: 48 h
Result: Showed almost no inhibitory activity against A549 or Jurkat T cells cultured alone.
Significantly decreased A549 cell viability at 2 μM in co-culture model.
Enhanced Jurkat T cell-mediated killing of A549 cells in co-culture model.
In Vivo

PJ27 (25-50 mg/kg; i.p.; daily; 11 days) potently and dose-dependently inhibits LLC lung tumor growth in male C57BL/6J mice, achieving a 56% tumor growth inhibition rate at 50 mg/kg, while enhancing antitumor T cell infiltration and demonstrating no obvious toxicity[1].

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

Animal Model: C57BL/6J (male, 5 to 6 weeks old, subcutaneous inoculation of 1 × 106 LLC cells)[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: i.p.; daily; 11 days
Result: Achieved a tumor growth inhibition rate (TGI) of 21% and reduced phosphorylated STAT3 (p-STAT3) levels in tumor tissues compared to control at 25 mg/kg.
Achieved a TGI of 56%, reduced p-STAT3 and PD-L1 levels in tumor tissues, increased the percentage of CD3+CD8+ cytotoxic T cells in tumor tissues to 38.8% (vs.
16.3% in control), and increased the percentage of CD3+CD4+ helper T cells in tumor tissues to 50.5% (vs.
28.9% in control) at 50 mg/kg.
Showed no significant body weight loss or organ toxicity in either dose group.
Molecular Weight

640.78

Formula

C38H40N8O2

SMILES

CC1=C(C2=NC(OC)=C(CNC3CCN(C(CCCN4C=C(C5=NC=NC6=C5C=CN6)C=N4)=O)CC3)C=C2)C=CC=C1C7=CC=CC=C7

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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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.

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PJ27
Cat. No.:
HY-181663
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