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.

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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].

Cellular Effect
Cell Line Type Value Description References
K562 GI
21.6 %
Compound: 14a
Growth inhibition of human K562 cells at 10 uM after 24 hrs by MTT assay relative to control
Growth inhibition of human K562 cells at 10 uM after 24 hrs by MTT assay relative to control
[PMID: 28365319]
In Vitro

PD-L1-IN-11 (APBC) (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

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Storage

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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?

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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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