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.
Biological Activity
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IL-2 |
PI3K |
Akt |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
>10 μM
Compound: 2
|
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
|
[PMID: 31359750] |
| L5178Y | IC50 |
>10 μM
Compound: 2
|
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
|
[PMID: 31359750] |
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
-
Concentration:15, 30, 60 μM
-
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
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)