NAMPT/PD-1/PD-L1-IN-1
NAMPT/PD-1/PD-L1-IN-1 is a potent the PD-1/PD-L1 interaction and NAMPT dual inhibitor with IC50s of 7.5 nM and 18.8 nM, respectively. NAMPT/PD-1/PD-L1-IN-1 enhances T cell-mediated tumor cell killing, promotes T cell proliferation and CD8+ T cell proportion and depletes intracellular NAD+ biosynthesis. NAMPT/PD-1/PD-L1-IN-1 suppresses tumor progression in a mouse LLC xenograft model by disrupting tumor metabolism and activating the tumor immune microenvironment. NAMPT/PD-1/PD-L1-IN-1 can be used in research on tumor immunotherapy for non-small cell lung cancer.
For research use only. We do not sell to patients.
- CAS No.: 3097045-01-4
- Formula: C36H35ClN10O
- Molecular Weight:659.18
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
NAMPT/PD-1/PD-L1-IN-1 (compound B14) inhibits the PD-1/PD-L1 interaction with an IC50 of 7.5 nM and NAMPT with an IC50 of 18.8 nM[1].
NAMPT/PD-1/PD-L1-IN-1 (72 h) suppresses A2780 cell proliferation with an IC50 of 14.8 nM[1].
NAMPT/PD-1/PD-L1-IN-1 (25, 50, 100 nM; 72 h) enhances T cell-mediated killing of CT26/OE PD-L1 cells in a co-culture model, with relative inhibition rates of 15.17%, 15.65% and 27.23%, respectively[1].
NAMPT/PD-1/PD-L1-IN-1 (25, 50, 100 nM; 72 h) promotes T cell proliferation in CT26/OE PD-L1 or CT26/Vector cells and T cell co-culture models[1].
NAMPT/PD-1/PD-L1-IN-1 (25, 50, 100 nM; 72 h) increases the proportion of CD8+ T cells to 13.37%, 13.95% and 15.20%, respectively, in CT26/OE PD-L1 and T cell co-culture models[1].
NAMPT/PD-1/PD-L1-IN-1 (0-1600 nM; 72 h) augments T cell-mediated cytotoxicity against CT26/OE PD-L1 cells but does not affect CT26/OE PD-L2 cell viability[1].
NAMPT/PD-1/PD-L1-IN-1 (1.95-500 nM; 24 h) induces a dose-dependent reduction in intracellular NAD+ levels in A2780 cells, with NAD+ reduced to 31.5% of control at 1.95 nM[1].
NAMPT/PD-1/PD-L1-IN-1 (50 nM; 24 h) triggers cell growth suppression and NAD+ depletion in A2780 cells, and exogenous NMN reverses the adverse changes in a dose-dependent manner[1].
NAMPT/PD-1/PD-L1-IN-1 (100 nM; 48 h) in T cell-LLC co-culture model suppresses LLC cell proliferation via dual mechanisms of NAMPT inhibition and PD-1/PD-L1 blockade[1].
NAMPT/PD-1/PD-L1-IN-1 (10 nM; 48 h) in T cell-A2780 co-culture model demonstrates synergistic antitumor activity via dual mechanisms[1].
NAMPT/PD-1/PD-L1-IN-1 (0.8, 1.6 μM; 48 h) shows negligible cytotoxicity against L02 human hepatocytes, with only 5-10% growth inhibition[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Coculture models of CT26 cells overexpressing PD-L1 (CT26/OE PD-L1) or CT26 cells overexpressing PD-L2 (CT26/OE PD-L2) cocultured with T cells
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Concentration:0-1600 nM
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Incubation Time:72 h
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Result:Augmented T cell-mediated cytotoxicity against CT26/OE PD-L1 cells in a concentration-dependent manner.
Did not affect the viability of CT26/OE PD-L2 cells over the entire concentration range tested.
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Cell Line:Coculture models of CT26 cells overexpressing PD-L1 (CT26/OE PD-L1) or vector-transfected control CT26 cells (CT26/Vector) cocultured with T cells
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Concentration:25, 50, 100 nM
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Incubation Time:72 h
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Result:Promoted T cell proliferation.
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Cell Line:Coculture models of CT26 cells overexpressing PD-L1 (CT26/OE PD-L1) or vector-transfected control CT26 cells (CT26/Vector) cocultured with T cells
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Concentration:25, 50, 100 nM
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Incubation Time:72 h
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Result:Enhanced T cell-mediated tumor cell killing with relative inhibition rates of 15.17%, 15.65% and 27.23%, respectively.
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Cell Line:A2780 cells
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Concentration:50 nM
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Incubation Time:24 h
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Result:Triggered cell growth suppression and NAD+ depletion.
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Cell Line:LLC and T cells (co-culture model)
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Concentration:100 nM
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Incubation Time:48 h
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Result:Suppressed LLC cell proliferation via dual mechanisms of NAMPT inhibition and PD-1/PD-L1 blockade.
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Cell Line:A2780 and PBMCs (co-culture model)
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Concentration:10 nM
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Incubation Time:48 h
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Result:Demonstrated synergistic antitumor activity via dual mechanisms.
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Cell Line:L02 cells
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Concentration:0.8, 1.6 μM
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Incubation Time:48 h
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Result:Showed negligible cytotoxicity with only 5-10% growth inhibition at 0.8 and 1.6 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LLC OE NAMPT/PD-L1 xenograft model in C57BL/6 mice[1]
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Dosage:5, 10 mg/kg
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Administration:i.p.; once daily for Day 1, 3, 5, 7, 9, 11, 15, 19
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Result:Suppressed tumor growth in a dose-dependent manner.
Exhibited significant body weight loss.
Showed no significant alterations in the weights of major organs.
Reduced NAD+ levels in tumor tissues (10 mg/kg).
Exhibited enhanced infiltration of CD45+ and CD8+ T cells and increased levels of IFN-γ+ and IL-2+ CD8+ T cells among tumor-infiltrating CD8+ T cells (10 mg/kg).
Chemical Information
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CAS No. 3097045-01-4
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Molecular Weight 659.18
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Formula C36H35ClN10O
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SMILES
ClC1=C(C=CC=C1OCCCN2CCCC2)C3=CC=CC4=C3CCN4C5=NC=NC6=C5N=CC(CN/C(NC7=CC=NC=C7)=N\C#N)=C6
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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)
NAMPT/PD-1/PD-L1-IN-1 Related Classifications
HY-184918 Related Classifications
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