Enpp-1-IN-34
Enpp-1-IN-34 is a selective ENPP1 inhibitor. Enpp-1-IN-34 inhibits human ENPP1 with an IC50 value of 1.20 nM at pH 7.5. Enpp-1-IN-34 weakly inhibits ENPP2/autotaxin and ENPP3, with IC50 values of 202 nM and 37.5 nM, respectively. Enpp-1-IN-34 induces cGAMP (HY-12512)-mediated STING pathway activation and the expression of interferon-stimulated genes and chemokines. Enpp-1-IN-34 can be used for research on colorectal cancer.
For research use only. We do not sell to patients.
- Formula: C19H15BF2N2O5
- Molecular Weight:400.14
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
ENPP1 1.20 nM (IC50) |
Autotaxin 202 nM (IC50) |
ENPP3 37.5 nM (IC50) |
STING |
In Vitro
Enpp-1-IN-34 inhibits ENPP1 preferentially over ENPP3 and ENPP2, with IC50 values of 37.5 nM and 202 nM for the latter two, respectively[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:0.5; 1 μM
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Incubation Time:12 h
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Result:Enhanced cGAMP-induced mRNA expression of IFNB1, IL6, and CXCL10.
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Cell Line:THP-1 cells
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Concentration:2.5; 5; 10 μM
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Incubation Time:2 h
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Result:Increased the protein levels of p-TBK1 and p-IRF3.
Parmacokinetics
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | AUC0-∞ | Clearance (CL) | MRT0-∞ | Vz | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 2 mg/kg | i.v. | 1.24 h | 0.08 h | 1719 ng/mL | 686 ng·h/mL | 687 ng·h/mL | 49.73 mL/min/kg | 0.43 h | 5374 mL/kg | / |
| Mice[1] | 20 mg/kg | i.p. | 1.66 h | 0.08 h | 6456 ng/mL | 3513 ng·h/mL | 3522 ng·h/mL | 95.02 mL/min/kg | 0.525 h | 13563 mL/kg | / |
| Mice[1] | 20 mg/kg | p.o. | 1.13 h | 0.14 h | 1646 ng/mL | 1191 ng·h/mL | 1196 ng·h/mL | 284 mL/min/kg | 0.99 h | 27667 mL/kg | 17.4 % |
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 (female, 6-8 weeks old)[1]
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Dosage:20 mg/kg; 30 mg/kg; 20 mg/kg in combination with Oxaliplatin 5 mg/kg
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Administration:i.p.; once daily for 12 consecutive days; Oxaliplatin i.p. once on day 1 in combination
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Result:Single-agent dosing at 20 mg/kg achieved 57.4% TGI.
Single-agent dosing at 30 mg/kg achieved 58.5% TGI.
At 20 mg/kg combined with Oxaliplatin 5 mg/kg achieved 80.7% TGI.
The combination group had the lowest final tumor weight among experimental groups.
Tumor tissue IFN-β and IL-6 levels were elevated compared with vehicle.
In combination with Oxaliplatin, CD8+ T-cell and macrophage infiltration increased and regulatory T cells were reduced.
Chemical Information
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Molecular Weight 400.14
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Formula C19H15BF2N2O5
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SMILES
O=C(N1CC2=CC=C(B(O)O)C(OC)=C2)OCC3=C1C4=CC(F)=C(F)C=C4N=C3
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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)
Enpp-1-IN-34 Related Classifications
HY-190868 Related Classifications
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