PD-1/PD-L1-IN-54
PD-1/PD-L1-IN-54 (Compound 6) is a moderately affinic PD-1/PD-L1 inhibitor (KD: PD-1, 55.8 μM; PD-L1, 46.4 μM; IC50: 88.6 μM). PD-1/PD-L1-IN-54 inhibits PD-1/PD-L1 interactions and shows anticancer activity by activating CD8+ T cells, upregulating PD-1 expression, and increasing secretion of IFN-γ and IL-2. PD-1/PD-L1-IN-54 inhibits cancer cell proliferation and promotes apoptosis. PD-1/PD-L1-IN-54 also regulates T cell immunity through the PI3K/Akt pathway correlated with PD-1/PD-L1.
For research use only. We do not sell to patients.
- CAS No.: 1393644-68-2
- Formula: C17H17ClO7
- Molecular Weight:368.77
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
IL-2 |
PI3K |
Akt |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
>10 μM
Compound: 2
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Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 31359750] |
| L5178Y | IC50 |
>10 μM
Compound: 2
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Cytotoxicity against mouse L5178Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against mouse L5178Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 31359750] |
In Vitro
PD-1/PD-L1-IN-54 (15-60 μM, 48 h) facilitates the proliferation of CD8+ T cells and inhibits the expansion of tumor cells (LLC and MC38) [1].
PD-1/PD-L1-IN-54 (15-60 μM, 48 h) promotes secretion of immune cytokines (IFN-γ and IL-2) in CD8+ T cells, and promotes apoptosis of tumor cells (LLC and MC38) in the co-culture system[1].
PD-1/PD-L1-IN-54 (15-60 μM, 48 h) increases PD-1 expression on CD8+ T cells cocultured with LLC or MC38 cells[1].
PD-1/PD-L1-IN-54 (15-60 μM, 48 h) activates the PI3K/Akt and NF-κB pathway, the downstream pathways of PD-1/PD-L1 interactions[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Co-culture system consisting of activated CD8+ T cells and tumor cells (LLC or MC38) added in a 5:1 ratio
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Concentration:15, 30, 60 μM
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Incubation Time:48 h
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Result:Promoted phosphorylation of PI3K, Akt and NF-κB in T cells
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Cell Line:Co-culture system consisting of activated CD8+ T cells and tumor cells (LLC or MC38) added in a 5:1 ratio
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Concentration:15, 30, 60 μM
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Incubation Time:48 h
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Result:Inhibited the proliferation of LLC and MC38 tumor cells and stimulated the proliferation of CD8+ T cells
- RNA extraction experimental
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Research Protocol for Cancer Immunology
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Apoptosis Solutions
- MTT Cell Proliferation Assay
Chemical Information
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CAS No. 1393644-68-2
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Molecular Weight 368.77
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Formula C17H17ClO7
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SMILES
COC1=CC(O)=C(C(OC)=O)C(OC2=C(C)C=C(O)C=C2OC)=C1Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PD-1/PD-L1-IN-54 Related Classifications
HY-159892 Related Classifications
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