2. Immunology/Inflammation
  3. PD-1/PD-L1
  4. NPH16

NPH16 is an orally active PD-1/PD-L1 inhibitor with an IC50 of 2.24 nM. NPH16 can promote HepG2 cell apoptosis. NPH16 shows excellent in vivo antitumor efficacy and favorable pharmacokinetic properties. NPH16 can be used for the study of liver cancer.

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NPH16 Chemical Structure

NPH16 Chemical Structure

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NPH16 Related Antibodies

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Description

NPH16 is an orally active PD-1/PD-L1 inhibitor with an IC50 of 2.24 nM. NPH16 can promote HepG2 cell apoptosis. NPH16 shows excellent in vivo antitumor efficacy and favorable pharmacokinetic properties. NPH16 can be used for the study of liver cancer[1].

In Vitro

NPH16 (0-2 μM, 48 h) exhibits dose-dependent cytotoxicity against HepG2 cells in the coculture system[1].
NPH16 (0.02-20 μM, 0-700 s) interacts with human PD-L1 (KD = 54.6 nM) and mouse PD-L1 (KD = 51.6 nM) in a concentration-dependent manner[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NPH16 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: HepG2, HepG2/Jurkat T cell coculture
Concentration: 0, 0.25, 0.5, 1, 2 μM
Incubation Time: 48 h
Result: Demonstrated low toxicity at 2 μM, with cell viability exceeding 98%.
Exhibited dose-dependent cytotoxicity in the coculture system.
Reduced cell viability to 58.7% in the HepG2/Jurkat coculture model.
In Vivo

NPH16 (50-100 mg/kg, p.o., for 7 days) demonstrates significant dose-dependent antitumor activity throughout the treatment period in C57BL/6 mice bearing HEPA1-6 hepatoma tumors[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice bearing HEPA1-6 hepatoma tumors[1]
Dosage: 50 mg/kg, 100 mg/kg
Administration: p.o., for 7 days
Result: Caused no significant weight loss or adverse reactions in the mice.
Demonstrated significant dose-dependent antitumor activity throughout the treatment period.
Reduced tumor weight and volume by 92.1 and 91.2%, respectively at a dose of 100 mg/kg.
Significantly decreased the tumor weight and volume, amounting to 77.5 and 74.8%, respectively at a dose of 50 mg/kg.
Maintained the cellular boundaries within the organ tissues distinct and no obvious cell necrosis observed.
Significantly reduced PD-L1 expression by approximately 40%.
Markedly elevated IFN-γ levels in tumor tissues (5.4-fold increase vs control) .
Increased the percentage of CD3+CD8+ cells (activated cytotoxic T cells) to 3.9% at a dose of 100 mg/kg.
Significantly reduced splenic Treg populations (0.7% vs 2.6% in vehicle controls), while producing a modest decrease in intratumoral Tregs at a dose of 100 mg/kg.
Substantially downregulated TIM3 protein expression relative to control groups(100 mg/kg) .
Molecular Weight

686.24

Formula

C39H44ClN3O6
SMILES

N#CC1=CC=CC(COC2=CC(OCC3=C(C(C4=CC(OCCOCCN5CC(CC5)O)=CC=C4)=CC=C3)C)=C(C=C2CNCCO)Cl)=C1
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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NPH16 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NPH16NPH 16NPH-16PD-1/PD-L1PD-1/Programmed death-ligand 1Small-moleculeHepG2CancerCD8+Mouse tumor modelInhibitorinhibitorinhibit

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