PD-1/PD-L1-IN-62
PD-1/PD-L1-IN-62 is a PD-L1 inhibitor and mTOR modulator. PD-1/PD-L1-IN-62 inhibits PD-L1 with an IC50 of 6.9 nM and abrogates immune suppression mediated by the PD-1/PD-L1 pathway. By inhibiting mTOR phosphorylation and downregulating the downstream target SREBP1, PD-1/PD-L1-IN-62 significantly reduces cholesterol and triglyceride levels to decrease lipid accumulation. PD-1/PD-L1-IN-62 promotes the infiltration of CD3+CD8+ T cells into tumor tissues, thereby effectively inhibiting tumor growth. PD-1/PD-L1-IN-62 can be used for the research of hepatocellular carcinoma.
For research use only. We do not sell to patients.
- Formula: C33H44N4O4
- Molecular Weight:560.73
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
PD-1/PD-L1-IN-62 (ZQ8) (0.25-1 μM; 48 h) exhibits minimal cytotoxicity against monocultured HepG2 cells[1].
PD-1/PD-L1-IN-62 (0.25-1 μM; 48 h) reverses PD-1/PD-L1-mediated immunosuppression in a HepG2/Jurkat T cell coculture model[1].
PD-1/PD-L1-IN-62 (0.05-0.4 μM; 48 h) dose-dependently reduces lipid accumulation in PA/OA-induced steatotic HepG2 cells, decreasing cholesterol by 41% and triglycerides by 19% at 0.4 μM[1].
PD-1/PD-L1-IN-62 (0.05-0.4 μM; 48 h) dose-dependently inhibits mTOR phosphorylation and downregulates SREBP1 expression in PA/OA-induced steatotic HepG2 cells[1].
PD-1/PD-L1-IN-62's lipid-lowering effects in Palmitic acid (HY-N0830)/Oleic acid (HY-N1446)-induced steatotic HepG2 cells are associated with modulation of the PD-L1-mTOR-SREBP1 signaling axis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2/Jurkat T cell coculture
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Concentration:0.25-1 μM (coculture); 10 ng/mL IFN-γ (HepG2 pretreatment); PHA-P (HY-N7038A) (Jurkat pretreatment)
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Incubation Time:48 h (coculture); 24 h (HepG2 pretreatment); 48 h (Jurkat pretreatment)
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Result:Reduced HepG2 cell viability in a concentration-dependent manner in the coculture model.
At 1 μM, reduced HepG2 viability to 65.4%, showing significantly enhanced potency compared to NP19 (73.3% viability) and BMS-202 (78.9% viability).
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Cell Line:PA/OA-induced steatotic HepG2 cells
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Concentration:0.05-0.4 μM (with PA/OA); 0.25 mM PA/0.5 mM OA
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Incubation Time:48 h
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Result:Dose-dependently suppressed phosphorylation of mTOR, with a 40% reduction at 0.4 μM, while total mTOR levels remained unchanged.
Concomitantly, downregulated SREBP1 expression in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice with Hepatocellular carcinoma[1]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:intraperitoneal; once daily; 7 days
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Result:Achieved 75.1% tumor volume reduction and 64.7% tumor weight reduction, with no significant body weight fluctuations or overt toxicities observed.
Achieved 86.2% tumor volume reduction and 73.4% tumor weight reduction, with no significant body weight fluctuations or overt toxicities observed.
Increased the proportion of CD3+CD8+ cytotoxic T cells in tumor tissues to 5.5%.
Reduced serum triglyceride levels to 65.5% of the control group levels.
Reduced serum total cholesterol levels to 78.4% of the control group levels.
Induced a mild, non-statistically significant reduction in lipid accumulation within tumor tissues via Oil Red O staining.
Chemical Information
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Molecular Weight 560.73
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Formula C33H44N4O4
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SMILES
OC(CC1)CN1CCCCCOC2=CC(C3=CC=CC(C4=NC(OC)=C(CNCCNC(C)=O)C=C4)=C3C)=CC=C2
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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)
PD-1/PD-L1-IN-62 Related Classifications
HY-182048 Related Classifications
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