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 Chemical Structure

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

 

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