Enpp-1-IN-30
Enpp-1-IN-30 (compound 44a) is an orally active ENPP1 inhibitor with a human IC50 of 13.1 nM. Enpp-1-IN-30 prevents cGAMP degradation, activates the STING pathway. Enpp-1-IN-30 induces cytokine release to enhance innate immune response. Enpp-1-IN-30 exerts antitumor efficacy in syngeneic mouse models. Enpp-1-IN-30 can be used for the research of colon carcinoma.
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- Formule: C15H16FN5O2S
- Masse moléculaire:349.38
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
Enpp-1-IN-30 (compound 44a) (0.2 nM-1 μM; 2 h) potently inhibits recombinant human ENPP1 with an IC50 of 13.1 nM[1].
Enpp-1-IN-30 (up to 10,000 nM) is highly selective for ENPP1, with no detectable inhibition of recombinant human ENPP2 or ENPP3 at concentrations up to 10,000 nM[1].
Enpp-1-IN-30 (0.01-30 μM; 1 h) dose-dependently enhances cGAMP-mediated STING pathway activation in HCT116-Dual? cells, achieving an 8.8-fold increase in IRF3 luciferase intensity at 10 μM and a 10.1-fold increase at 30 μM[1].
Enpp-1-IN-30 (10 μM; 1-72 h) enhances innate immune activation in THP-1 cells co-treated with cGAMP, significantly increasing IFNB and CXCL10 mRNA expression over time and inducing a gradual, non-excessive increase in TNFA mRNA expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1 cells
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Concentration:10 μM (co-treated with 10 μM cGAMP)
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Incubation Time:24-72 h (IFNB); 1-72 h (CXCL10, TNFA)
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Result:Increased IFNB mRNA expression by 6.7-fold at 72 h (co-treated with 10 μM cGAMP).
Increased CXCL10 mRNA expression by 137-fold at 72 h (co-treated with 10 μM cGAMP).
Induced a gradual increase in TNFA mRNA expression reaching 8-fold at 72 h (co-treated with 10 μM cGAMP), with no instant overexpression of TNFA.
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:C57BL/6 (7-week-old female)[1]
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Dosage:50 mg/kg
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Administration:p.o.; once daily; 14 days
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Result:Reduced tumor volumes significantly relative to vehicle control group.
Produced synergistic tumor volume reduction in combination with anti-mPD-L1 antibody.
Caused no significant body weight loss or other clinical signs of toxicity.
Chemical Information
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Masse moléculaire 349.38
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Formule C15H16FN5O2S
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SMILES
C[S@](=O)(NCC1=CC=C(N2N=NC3=CC(OC)=CC=C32)C(F)=C1)=N
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Enpp-1-IN-30 Related Classifications
HY-181667 Related Classifications
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