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Art. -Nr.: HY-184200

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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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₁₅H₁₁ClN₆O₃S
Molecular Weight:390.80

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Enpp-1-IN-32 Chemical Structure

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Phosphodiesterase (PDE) Isoform-spezifische Produkte anzeigen :

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.

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	T_max	T_1/2	C_max	CL	V_ss	AUC_0-24	AUC_0-∞	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.

Chemical Information

Molecular Weight 390.80
Formel C₁₅H₁₁ClN₆O₃S
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Nong C, et al. Discovery of Pyrrolo[1',2':1,6]pyrimido[5,4-c]pyridazin-6(5H)-one Derivatives as Ectonucleotide Pyrophosphatase/Phosphodiesterase 1 Inhibitors. J Med Chem. 2026 Jun 11;69(11):13272-13293. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
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Enpp-1-IN-32

Alle Phosphodiesterase (PDE) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

Enpp-1-IN-32 Related Classifications

HY-184200 Related Classifications