1. Immunology/Inflammation PI3K/Akt/mTOR
  2. PD-1/PD-L1 IFNAR Interleukin Related PI3K Akt
  3. 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.

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PD-1/PD-L1-IN-54

PD-1/PD-L1-IN-54 Chemical Structure

CAS No. : 1393644-68-2

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Description

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[1].

IC50 & Target[1]

IL-2

 

PI3K

 

Akt

 

Cellular Effect
Cell Line 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]
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.

Western Blot Analysis[1]

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
Result: Promoted phosphorylation of PI3K, Akt and NF-κB in T cells

Cell Viability Assay[1]

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
Result: Inhibited the proliferation of LLC and MC38 tumor cells and stimulated the proliferation of CD8+ T cells
Molecular Weight

368.77

Formula

C17H17ClO7

CAS No.
SMILES

COC1=CC(O)=C(C(OC)=O)C(OC2=C(C)C=C(O)C=C2OC)=C1Cl

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References
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Product Name:
PD-1/PD-L1-IN-54
Cat. No.:
HY-159892
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