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Referencia número: HY-P11891

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FM213

FM213 is a PD-L1 inhibitor with a human IC₅₀ of 323 nM. FM213 blocks PD-1/PD-L1 protein-protein interactions, and promotes endocytosis and lysosome-dependent degradation of PD-L1 on the surface of cancer cells. FM213 binds to PD-L1 on cancer cells and exosomes, and enhances the recognition and killing of cancer cells by human PBMC. Combination of FM213 with the TIGIT inhibitor DTBP-3 (HY-P11903) enhances anti-tumor immunity. FM213 can be used in research related to non-small cell lung cancer.

Para uso exclusivo en investigación. No vendemos a pacientes.

Fòrmula: C₇₃H₈₆Cl₃N₁₃O₁₂
Peso molecular:1443.90

Almacenamiento:

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

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FM213 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
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Actividad biológica

Descripciòn

IC₅₀ & Target

^[1]

PD-L1

323 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
NCI-H1299	IC50	10 μM	Inhibition of cell viability against human H1299 NSCLC cells assessed by CCK-8 assay after 48-hour incubation. Inhibition of cell viability against human H1299 NSCLC cells assessed by CCK-8 assay after 48-hour incubation.	41729103
H1975	IC50	10 μM	Inhibition of cell viability against human H1975 NSCLC cells assessed by CCK-8 assay after 48-hour incubation. Inhibition of cell viability against human H1975 NSCLC cells assessed by CCK-8 assay after 48-hour incubation.	41729103
HaCaT	IC50	10 μM	Inhibition of cell viability against human HaCaT normal immortalized keratinocyte cells assessed by CCK-8 assay after 48-hour incubation. Inhibition of cell viability against human HaCaT normal immortalized keratinocyte cells assessed by CCK-8 assay after 48-hour incubation.	41729103
PBMC	IC50	10 μM	Inhibition of cell viability against human peripheral blood mononuclear cells assessed by CCK-8 assay after 48-hour incubation. Inhibition of cell viability against human peripheral blood mononuclear cells assessed by CCK-8 assay after 48-hour incubation.	41729103

In Vitro

FM213 (1 h) potently inhibits the interaction between human recombinant PD-1 and PD-L1 proteins in HTRF assays, with an IC₅₀ of 323 nM^[1].
FM213 (10 μM) specifically binds to human recombinant PD-L1 and PD-L1 protein, and does not interact with mouse recombinant PD-L1 and PD-1 protein^[1].
FM213 (6.25-50 μM) binds to specific surface residues on human recombinant PD-L1 protein, including those at the PD-1 interaction site^[1].
FM213 (1-100 μM; 48 h) inhibits the viability of H1299 non-small cell lung cancer cells, H1975 non-small cell lung cancer cells, HaCaT normal keratinocytes, and peripheral blood mononuclear cells (PBMCs)^[1].
FM213 (2 μM; 48 h) significantly increases the level of IL-2 and decreases the levels of IL-6 and TNF-α in the co-culture system of H1975 non-small cell lung cancer cells and activated peripheral blood mononuclear cells^[1].
FM213 (10 μM; 2 h) thermostabilizes PD-L1 in IFN-γ-stimulated H1299 cells and basal-state H1975 non-small cell lung cancer cells^[1].
FM213 (5 μM; 2 h) protects PD-L1 from proteolytic degradation in IFN-γ-stimulated H1299 cells and basal-state H1975 non-small cell lung cancer cells^[1].
FM213 (2 μM; 24 h) significantly reduces PD-L1 levels on the surface of IFN-γ-stimulated H1299 cells as well as basal-state H1975 non-small cell lung cancer (NSCLC) cells^[1].
FM213 (2 μM; 18-24 h) induces PD-L1 endocytosis and increases its colocalization with lysosomes in IFN-γ-stimulated H1299 cells and basal-state H1975 non-small cell lung cancer (NSCLC) cells^[1].
FM213 (2 μM; 24 h) shortens the half-life of PD-L1 in IFN-γ-stimulated H1299 cells and basal-state H1975 non-small cell lung cancer (NSCLC) cells via a lysosome-dependent pathway^[1].
FM213 (500 μM) specifically binds to PD-L1 on the surface of ex vivo exosomes derived from A549 non-small cell lung cancer cells^[1].
FM213 (2 μM; 48 h) significantly enhances apoptosis in H1299 and H1975 non-small cell lung cancer (NSCLC) cells and increases IFN-γ secretion levels in stimulated peripheral blood mononuclear cells (PBMCs)^[1].
The combination of FM213 (2 μM; 48 h) and 2.5 μM DTBP-3 (HY-P11903) synergistically significantly enhances apoptosis in H1299 and H1975 non-small cell lung cancer (NSCLC) cells and increases IFN-γ secretion levels in stimulated peripheral blood mononuclear cells (PBMCs)^[1].

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

Cell Viability Assay^[1]

Cell Line:

human NSCLC cell lines (H1299, H1975), normal immortalized human keratinocyte (HaCaT) cells, human peripheral blood mononuclear cells (PBMCs)
Concentration:

1, 2, 5, 10, 25, 50 and 100 μM
Incubation Time:

48 h
Result:

Reduced cell viability in a concentration-dependent manner across all tested cell lines.
The IC₅₀ value for cell viability inhibition was 10 μM in all tested cell lines.
At 2 μM, cell viability remained near 100% in all cell lines, confirming this as a non-cytotoxic concentration.

Apoptosis Analysis^[1]

Cell Line:

cocultures of human NSCLC cell lines (H1299, H1975) with stimulated human PBMCs
Concentration:

2 μM
Incubation Time:

48 h
Result:

Significantly increased the rate of Annexin V-positive apoptotic cells in both H1299 (to ~20%) and H1975 (to ~12%) cell lines compared to untreated cocultures.
Significantly increased IFN-γ secretion by stimulated PBMCs to ~3500 pg/mL in H1299 cocultures and ~3800 pg/mL in H1975 cocultures, which was higher than levels induced by control compounds.

ELISA Assay^[1]

Cell Line:

cocultures of human H1975 NSCLC cells with stimulated human PBMCs
Concentration:

2 μM
Incubation Time:

48 h
Result:

Significantly increased IL-2 levels to a mean of 404.9 pg/mL.
Significantly reduced IL-6 levels to a mean of 3150 pg/mL.
Significantly reduced TNF-α levels to a mean of 30.22 pg/mL compared to untreated cocultures.

Immunofluorescence^[1]

Cell Line:

human NSCLC cell lines (H1299, H1975) with IFN-γ-induced PD-L1 upregulation (H1299) or basal PD-L1 expression (H1975)
Concentration:

2 μM
Incubation Time:

18 h, 24 h
Result:

Dramatically reduced cell-surface PD-L1 expression and increased colocalization of PD-L1 with lysosomes after 18 and 24 hours of treatment, indicating PD-L1 internalization and lysosomal targeting.

Western Blot Analysis^[1]

Cell Line:

human NSCLC cell lines (H1299, H1975) with IFN-γ-induced PD-L1 upregulation (H1299) or basal PD-L1 expression (H1975)
Concentration:

2 μM this compound; 20 μM Cycloheximide (HY-12320), 30 μM Chloroquine (HY-17589A)
Incubation Time:

24 h (this compound); 2 h, 4 h, 6 h (Cycloheximide (HY-12320), Chloroquine (HY-17589A))
Result:

In the presence of cycloheximide, significantly reduced the PD-L1 half-life to less than 6 hours in both cell lines compared to cycloheximide-only controls.
This effect was abrogated by cotreatment with chloroquine, confirming lysosome-dependent degradation.

Apoptosis Analysis^[1]

Cell Line:

cocultures of human NSCLC cell lines (H1299, H1975) with stimulated human PBMCs, in combination with TIGIT inhibitor DTBP-3
Concentration:

2 μM this compound, 2.5 μM DTBP-3 (HY-P11903)
Incubation Time:

48 h
Result:

Cotreatment significantly increased the rate of Annexin V-positive apoptotic cells in both H1299 (to ~50%) and H1975 (to ~60%) cell lines compared to single-agent treatments and untreated cocultures.
Significantly increased IFN-γ secretion by stimulated PBMCs to ~5000 pg/mL in H1299 cocultures and ~5500 pg/mL in H1975 cocultures, which was higher than levels induced by single-agent treatments.

Chemical Information

Peso molecular 1443.90
Fòrmula C₇₃H₈₆Cl₃N₁₃O₁₂
Sequence

Cyclo({Phe(4-Cl)}-Lys-{Phe(4-Cl)}-{d-Pro}-Pro-Trp-Tyr-{Phe(4-Cl)}-Leu-Asn)
Sequence Shortening

Cyclo({Phe(4-Cl)}-K-{Phe(4-Cl)}-{d-Pro}-PWY-{Phe(4-Cl)}-LN)
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Merlino F, et al. Coupling PD-L1 Inhibition and Lysosomal Degradation: Innovative Anti-PD-L1 Peptides for NSCLC Immunotherapy. Journal of medicinal chemistry. 2026 Mar 12;69(5):5477-5500.

Calculators

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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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