Enpp-1-IN-32
Enpp-1-IN-32 is an orally active, selective ENPP-1 inhibitor with an IC50 of 9.5 nM. Enpp-1-IN-32 shows selectivity over ENPP2/ENPP3. Enpp-1-IN-32 blocks cGAMP hydrolysis, and activates the STING pathway. Enpp-1-IN-32 exhibits antitumor effects in syngeneic mouse models. Enpp-1-IN-32 can be used for the research of triple-negative breast carcinoma.
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- Formule: C15H11ClN6O3S
- Masse moléculaire:390.80
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Stockage:
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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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
Enpp-1-IN-32 (compound A25) shows negligible activity against recombinant human ENPP2 and weak activity against recombinant human ENPP3 (IC50 > 1000 nM)[1].
Enpp-1-IN-32 (3 h) potently inhibits cellular ENPP1 activity in MDA-MB-231 cells with an IC50 of 262.3 nM[1].
Enpp-1-IN-32 (12.5-50 μM; 48 h) shows no cytotoxicity toward MDA-MB-231, 4T1, HEK-293T, or THP-1 cells[1].
Enpp-1-IN-32 (25 μM; 1-24 h) effectively enhances cGAMP-mediated STING pathway activation in THP-1 cells, increasing downstream gene expression, IFN-β secretion, and phosphorylation of STING, TBK1, and IRF3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MDA-MB-231, 4T1, HEK-293T, THP-1 cells
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Concentration:12.5; 25; 50 μM
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Incubation Time:48 h
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Result:Did not reduce the viability of MDA-MB-231, 4T1, HEK-293T, or THP-1 cells at concentrations up to 50 μM.
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Cell Line:THP-1 cells
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Concentration:25 μM
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Incubation Time:1 h, followed by 6 h cGAMP (2 μM)
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Result:Increased p-STING levels.
Increased phosphorylation of TBK1 and IRF3.
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Cell Line:THP-1 cells
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Concentration:25 μM
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Incubation Time:6; 24 h
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Result:Increased IFN-β secretion in THP-1 cells.
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Cell Line:THP-1 cells
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Concentration:25 μM
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Incubation Time:6 h
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Result:Increased CXCL10, IFIT3, ISG15 mRNA levels.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice (female, 6 to 8 weeks old) subcutaneously inoculated with 4T1 cells[1]
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Dosage:100 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 31.5%, significantly reducing both tumor volume and weight.
Increased the proportion of CD3+CD8+ cytotoxic T lymphocytes in spleen tissue to 12.5% and in tumor tissue to 2.27%.
Significantly elevated plasma IP-10 (CXCL10) levels.
Caused no significant body weight changes or histopathological abnormalities in major organs (heart, liver, spleen, lung, kidney) in any treated groups.
Chemical Information
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Masse moléculaire 390.80
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Formule C15H11ClN6O3S
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SMILES
NS(C(C=C1)=CN=C1CN2C3=CC(Cl)=NN=C3C4=CC=CN4C2=O)(=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Enpp-1-IN-32 Related Classifications
HY-184200 Related Classifications
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