2. Metabolic Enzyme/Protease Immunology/Inflammation
  3. Phosphodiesterase (PDE) STING IFNAR
  4. 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.

For research use only. We do not sell to patients.

Enpp-1-IN-32

Enpp-1-IN-32 Chemical Structure

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Enpp-1-IN-32 Related Antibodies

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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Description

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[1].

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.

Enpp-1-IN-32 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: MDA-MB-231, 4T1, HEK-293T, THP-1 cells
Concentration: 12.5; 25; 50 μM
Incubation Time: 48 h
Result: Did not reduce the viability of MDA-MB-231, 4T1, HEK-293T, or THP-1 cells at concentrations up to 50 μM.

Western Blot Analysis[1]

Cell Line: THP-1 cells
Concentration: 25 μM
Incubation Time: 1 h, followed by 6 h cGAMP (2 μM)
Result: Increased p-STING levels.
Increased phosphorylation of TBK1 and IRF3.

ELISA Assay[1]

Cell Line: THP-1 cells
Concentration: 25 μM
Incubation Time: 6; 24 h
Result: Increased IFN-β secretion in THP-1 cells.

Real Time qPCR[1]

Cell Line: THP-1 cells
Concentration: 25 μM
Incubation Time: 6 h
Result: Increased CXCL10, IFIT3, ISG15 mRNA levels.
Parmacokinetics
Species Dose Route Tmax T1/2 Cmax CL Vss AUC0-24 AUC0-∞ F
Rat[1] 1 mg/kg i.v. 0.13 h 1.85 h 262 ng/mL 2.10 L/h/kg 5.64 L/kg 430 ng/mL·h 476 ng/mL·h /
Rat[1] 20 mg/kg p.o. 1.32 h 3.25 h 449 ng/mL 6.85 L/h/kg 31.97 L/kg 2903 ng/mL·h 2924 ng/mL·h 33.7 %
In Vivo

Enpp-1-IN-32 (Compound A25) (100 mg/kg; p.o.; daily; 14 days) exhibits significant antitumor efficacy in a 4T1 syngeneic TNBC mouse model[1].

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

Animal Model: BALB/c mice (female, 6 to 8 weeks old) subcutaneously inoculated with 4T1 cells[1]
Dosage: 100 mg/kg
Administration: p.o.; daily; 14 days
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.
Molecular Weight

390.80

Formula

C15H11ClN6O3S
SMILES

NS(C(C=C1)=CN=C1CN2C3=CC(Cl)=NN=C3C4=CC=CN4C2=O)(=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Enpp-1-IN-32 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:

Enpp-1-IN-32Phosphodiesterase (PDE)STINGIFNARStimulator of Interferon GenesTMEM173MITAERISMPYSInterferon-α/β receptorInterferon-alpha/beta receptorSTING pathwayTBK14T1 cellsENPP1IRF3triple-negative breast carcinomaENPP2ENPP3MDA-MB-231 cellsInhibitorinhibitorinhibit

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