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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C73H86Cl3N13O12
- 分子量:1443.90
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
PD-L1 323 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1299 | IC50 |
10 μM
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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.
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41729103 |
| H1975 | IC50 |
10 μM
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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.
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41729103 |
| HaCaT | IC50 |
10 μM
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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.
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41729103 |
| PBMC | IC50 |
10 μM
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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.
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41729103 |
体外実験
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.
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Cell Line:human NSCLC cell lines (H1299, H1975), normal immortalized human keratinocyte (HaCaT) cells, human peripheral blood mononuclear cells (PBMCs)
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Concentration:1, 2, 5, 10, 25, 50 and 100 μM
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Incubation Time:48 h
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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.
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Cell Line:cocultures of human NSCLC cell lines (H1299, H1975) with stimulated human PBMCs
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Concentration:2 μM
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Incubation Time:48 h
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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.
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Cell Line:cocultures of human H1975 NSCLC cells with stimulated human PBMCs
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Concentration:2 μM
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Incubation Time:48 h
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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.
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Cell Line:human NSCLC cell lines (H1299, H1975) with IFN-γ-induced PD-L1 upregulation (H1299) or basal PD-L1 expression (H1975)
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Concentration:2 μM
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Incubation Time:18 h, 24 h
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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.
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Cell Line:human NSCLC cell lines (H1299, H1975) with IFN-γ-induced PD-L1 upregulation (H1299) or basal PD-L1 expression (H1975)
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Concentration:2 μM this compound; 20 μM Cycloheximide (HY-12320), 30 μM Chloroquine (HY-17589A)
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Incubation Time:24 h (this compound); 2 h, 4 h, 6 h (Cycloheximide (HY-12320), Chloroquine (HY-17589A))
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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.
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Cell Line:cocultures of human NSCLC cell lines (H1299, H1975) with stimulated human PBMCs, in combination with TIGIT inhibitor DTBP-3
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Concentration:2 μM this compound, 2.5 μM DTBP-3 (HY-P11903)
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Incubation Time:48 h
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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.
化学情報
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分子量 1443.90
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分子式 C73H86Cl3N13O12
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配列
Cyclo({Phe(4-Cl)}-Lys-{Phe(4-Cl)}-{d-Pro}-Pro-Trp-Tyr-{Phe(4-Cl)}-Leu-Asn)
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シーケンスの短縮
Cyclo({Phe(4-Cl)}-K-{Phe(4-Cl)}-{d-Pro}-PWY-{Phe(4-Cl)}-LN)
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
FM213 関連分類
HY-P11891 関連分類
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