2. Immunology/Inflammation
  3. PD-1/PD-L1
  4. PD-L1-IN-11

PD-L1-IN-11 is a PD-L1 inhibitor with human PD-L1 IC50 and KD of 27.82 μM and 49.50 μM, respectively. PD-L1-IN-11 directly binds to PD-L1 via a dimer-locking mechanism, occluding the PD-1 interaction surface to disrupt PD-1/PD-L1 interaction. PD-L1-IN-11 can be used for the research of melanoma, colon carcinoma.

For research use only. We do not sell to patients.

PD-L1-IN-11

PD-L1-IN-11 Chemical Structure

CAS No. : 324054-99-1

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PD-L1-IN-11 Related Antibodies

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Description

PD-L1-IN-11 is a PD-L1 inhibitor with human PD-L1 IC50 and KD of 27.82 μM and 49.50 μM, respectively. PD-L1-IN-11 directly binds to PD-L1 via a dimer-locking mechanism, occluding the PD-1 interaction surface to disrupt PD-1/PD-L1 interaction. PD-L1-IN-11 can be used for the research of melanoma, colon carcinoma[1][2].

In Vitro

PD-L1-IN-11 (3.125-100 μM) binds directly to recombinant human PD-L1 protein with a KD of 49.50 μM[2].
PD-L1-IN-11 (50-100 μM) inhibits the PD-1/PD-L1 protein-protein interaction with an IC50 of 27.82 μM, reaching 65.1% blocking efficiency at 100 μM[2].
PD-L1-IN-11 (25-50 μM; 30 min) blocks the interaction between hPD-L1 protein and hPD-1-expressing Jurkat cells, with 10.2% efficiency at 25 μM and 37.3% efficiency at 50 μM, without inducing cell toxicity[2].
PD-L1-IN-11 (5-25 μM; 48 h coculture) dose-dependently enhances IFN-γ and TNF-α secretion from preactivated human CD4+ T cells cocultured with hPD-L1-expressing NCI-H1975 cells, restoring PD-L1-mediated T cell suppression[2].
PD-L1-IN-11 (10-50 μM; 48 h coculture) dose-dependently enhances TNF-α secretion from preactivated human CD4+ T cells cocultured with hPD-L1-overexpressing HEK293T cells, with effects dependent on PD-1/PD-L1 blockade[2].
PD-L1-IN-11 (200 μM; 24-48 h) has minimal cytotoxicity, with inhibition ratios below 25.6% at 200 μM after 24 or 48 h incubation with B16F10-hPD-L1, HeLa, BIC-1, and primary human CD4+ T cells[2].

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

PD-L1-IN-11 Related Antibodies

ELISA Assay[2]

Cell Line: preactivated human CD4+ T cells, NCI-H1975 cells (constitutively expressing hPD-L1)
Concentration: 5 μM; 10 μM; 25 μM
Incubation Time: 48 h
Result: Caused a dose-dependent increase in IFN-γ and TNF-α secretion from CD4+ T cells cocultured with NCI-H1975 cells.
Significantly elevated IFN-γ levels at 10 μM, 25 μM compared to control.
Significantly elevated TNF-α levels at 10 μM, 25 μM compared to control.

ELISA Assay[2]

Cell Line: preactivated human CD4+ T cells, HEK293T cells stably overexpressing hPD-L1 (HEK293T-hPD-L1)
Concentration: 10 μM; 25 μM; 50 μM
Incubation Time: 48 h
Result: Caused a dose-dependent increase in TNF-α secretion from CD4+ T cells cocultured with HEK293T-hPD-L1 cells.
Increased TNF-α levels by 41.8% at 10 μM compared to control.
Increased TNF-α levels by 86.6% at 50 μM compared to control.
Had no significant effect on cytokine secretion when CD4+ T cells were cultured alone or cocultured with PD-L1-negative HEK293T cells.

Cell Viability Assay[2]

Cell Line: B16F10-hPD-L1, HeLa, BIC-1, primary human CD4+ T cells
Concentration: 200 μM
Incubation Time: 24 h; 48 h
Result: Exhibited significantly low toxicity across all tested cell lines.
Showed inhibition ratios less than 25.6% at 200 μM after 24 h or 48 h incubation.
In Vivo

PD-L1-IN-11 (APBC) (10-15 mg/kg; i.p.; every 2 days; 8 total doses) exerts potent antitumor efficacy in hPD-L1 knock-in B16F10 melanoma-bearing mice[2].
PD-L1-IN-11 (10 mg/kg; i.p.; every 2 days; 7 total doses) exhibits significant antitumor efficacy in MC38 colon carcinoma-bearing mice without inducing weight loss[2].
PD-L1-IN-11 (15-50 mg/kg; i.p.; daily; 7 days) is well tolerated in hPD-L1 knock-in B16F10 melanoma-bearing mice, with no observable liver toxicity and a reduction in tumor-associated liver injury markers[2].

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

Animal Model: C57BL/6 (female, 5-6 weeks old, 18-22 g, subcutaneous inoculation with hPD-L1 knock-in B16F10 melanoma cells)[2]
Dosage: 10 mg/kg; 15 mg/kg
Administration: i.p.; every 2 days; 8 total doses
Result: Achieved 62.1% tumor growth inhibition relative to vehicle control, with reduced final tumor weight compared to vehicle.
Achieved 82.2% tumor growth inhibition relative to vehicle control, with 4 of 10 treated mice nearly tumor-free; final tumor weight was drastically reduced compared to vehicle.
Normalized spleen weight, significantly lower than the splenomegaly observed in vehicle-treated mice.
Increased splenic CD3+, CD3+CD4+, and CD3+CD8+ T lymphocyte percentages (P<0.001) relative to vehicle.
Increased perforin production in CD3+ cells (P<0.01) relative to vehicle.
Increased IFN-γ and TNF-α production in CD3+CD4+ T cells (P<0.01) relative to vehicle.
Increased infiltration of CD4+ and CD8+ T cells in tumor tissue relative to vehicle.
Elevated perforin and Granzyme B expression in CD3+ T cells in tumor tissue relative to vehicle.
Upregulated immune pathways including antigen processing and presentation, TNF signaling, and Th1/Th2 cell differentiation in tumors.
Significantly enriched CD8+ tumor-infiltrating lymphocytes in tumors.
Animal Model: C57BL/6 (female, 5-6 weeks old, 18-22 g, subcutaneous inoculation with MC38 colon carcinoma cells)[2]
Dosage: 10 mg/kg
Administration: i.p.; every 2 days; 7 total doses
Result: Significantly inhibited MC38 colon carcinoma growth relative to vehicle control.
Caused no significant effect on mouse body weight during treatment.
Animal Model: C57BL/6 (female, 5-6 weeks old, 18-22 g, subcutaneous inoculation with hPD-L1 knock-in B16F10 melanoma cells)[2]
Dosage: 15 mg/kg; 50 mg/kg
Administration: i.p.; daily; 7 days
Result: Showed no significant changes in serum alkaline phosphatase (ALP) or albumin (ALB) levels relative to vehicle.
Showed a tendency to decrease serum glutamic oxaloacetic transaminase (GOT) and glutamic pyruvic transaminase (GPT) levels relative to vehicle, with no observable liver toxicity.
Caused no drug-related deaths or toxic effects.
Molecular Weight

316.35

Formula

C20H16N2O2
CAS No.
SMILES

O=C(C1=C(NC(C2=CC=C(C3=CC=CC=C3)C=C2)=O)C=CC=C1)N
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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PD-L1-IN-11 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:

PD-L1-IN-11324054-99-1PD-1/PD-L1PD-1/Programmed death-ligand 1tumor microenvironmentCD8+ T cellprimary T-lymphocytehPD-L1 knock-in B16F10melanomahuman PD-L1Jurkat cellscolon carcinomaPD-1CD4+ T cellAPBCInhibitorinhibitorinhibit

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