2. Metabolic Enzyme/Protease Immunology/Inflammation
  3. Phosphodiesterase (PDE) STING
  4. Enpp-1-IN-27

Enpp-1-IN-27 is a selective ENPP1 inhibitor with an IC50 of 14.68 nM, exhibiting approximately 410-fold selectivity against ENPP2 and 10-fold selectivity against ENPP3. Enpp-1-IN-27 stabilizes cGAMP levels and activates the STING pathway, promoting cytokine release and enhancing innate immune responses. Enpp-1-IN-27 induces ISRE activation and amplified cGAMP-mediated immune responses and shows the desired antitumor efficacy in the 4T1 and CT26 syngeneic mouse models. Enpp-1-IN-27 can used for the studies of breast cancer and colon cancer.

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

Enpp-1-IN-27

Enpp-1-IN-27 Chemical Structure

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Enpp-1-IN-27 Related Antibodies

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Description

Enpp-1-IN-27 is a selective ENPP1 inhibitor with an IC50 of 14.68 nM, exhibiting approximately 410-fold selectivity against ENPP2 and 10-fold selectivity against ENPP3. Enpp-1-IN-27 stabilizes cGAMP levels and activates the STING pathway, promoting cytokine release and enhancing innate immune responses. Enpp-1-IN-27 induces ISRE activation and amplified cGAMP-mediated immune responses and shows the desired antitumor efficacy in the 4T1 and CT26 syngeneic mouse models. Enpp-1-IN-27 can used for the studies of breast cancer and colon cancer[1].

In Vitro

Enpp-1-IN-27 (Compound 31) (0-50 μM, 25 h) enhances cGAMP-mediated STING activity more effectively than cGAMP alone in both THP-1 cells (EC50 = 16.5 μM) and HCT116 cells[1].
Enpp-1-IN-27 (25-50 μM, 4-25 h) stimulates type I interferon responses by activation of STING signaling pathway in THP-1 and HCT116 cells[1].
Enpp-1-IN-27 (10 μM) demonstrates negligible inhibition of five major CYP enzyme isoforms (CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4) and exhibits excellent metabolic stability, with microsomal stability exceeding 95% in human, mouse, and rat liver microsomes[1].
Enpp-1-IN-27 exhibits favorable kinetic solubility (191 μM) and demonstrates no significant inhibition of the human Ether-à-go-go-related gene (hERG) channel (IC50 > 100 μM)[1].

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

Enpp-1-IN-27 Related Antibodies

ELISA Assay[1]

Cell Line: THP-1 cells and HFF cells
Concentration: 25 and 50 μM
Incubation Time: Pretreat for 1 h and treated with 5 μM of cGAMP for 24 h
Result: Significantly increased extracellular cytokine secretion compared to cGAMP treatment alone and demonstrated stronger innate immune activation than MV-658 in both THP-1 cells and HFF cells.

Western Blot Analysis[1]

Cell Line: THP-1 cells
Concentration: 25 and 50 μM
Incubation Time: Pretreat for 1 h and treated with 5 μM of cGAMP for 6 h
Result: Enhanced the phosphorylation of STING, TBK1, and IRF3, indicating robust activation of the STING signaling cascade.

RT-PCR[1]

Cell Line: THP-1 cells
Concentration: 25 and 50 μM
Incubation Time: Pretreat for 1 h and treated with 5 μM of cGAMP for 3 h
Result: Increased the expression levels of representative interferon-stimulated genes (ISGs), including IFNB, ISG15 and IFIT3.
Parmacokinetics[1]
Species Dose Route Indicator value
Mice 1 mg/kg i.v. T1/2 0.50 h
Mice 10 mg/kg p.o. T1/2 1.20 h
Mice 1 mg/kg i.v. Tmax 0.08 h
Mice 10 mg/kg p.o. Tmax 1.17 h
Mice 1 mg/kg i.v. Cmax 424.56 ng/mL
Mice 10 mg/kg p.o. Cmax 164.53 ng/mL
Mice 1 mg/kg i.v. AUClast 220.36 ng·h/mL
Mice 10 mg/kg p.o. AUClast 527.27 ng·h/mL
Mice 1 mg/kg i.v. AUCINF_obs 225.36 ng·h/mL
Mice 10 mg/kg p.o. AUCINF_obs 534.10 ng·h/mL
Mice 1 mg/kg i.v. MRTlast 0.45 h
Mice 10 mg/kg p.o. MRTlast 2.11 h
Mice 1 mg/kg i.v. MRTINF_obs 0.52 h
Mice 10 mg/kg p.o. MRTINF_obs 2.21 h
Mice 1 mg/kg i.v. Vss 2287.18 mL/kg
Mice 10 mg/kg p.o. F 23.93 %
Mice 1 mg/kg i.v. CL 75.61 mL/min/kg
In Vivo

Enpp-1-IN-27(Compound 31) (50 mg/kg, i.p., once daily for 15-20 days) shows the desired antitumor efficacy in the 4T1 and CT26 syngeneic mouse models without observable toxicity or side effects[1].
Enpp-1-IN-27 (50 mg/kg, i.p., single dose) has high safety and key biomarkers for liver toxicity. including aspartate transaminase (AST) and alanine trans-aminase (ALT), as well as kidney toxicity markers, such as blood Urea nitrogen (BUN) and serum creatinine both remained within the normal range[1].

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

Animal Model: 4T1 induced xenograft model established in female BALB/c mice (8 weeks old) [1]
Dosage: 50 mg/kg with or without anti-CTLA-4 antibodies (αCTLA-4)
Administration: Intraperitoneal injection (i.p.), once daily for 15 days
Result: Significantly inhibited tumor growth (47%) and the combination-treated group worked better (92%).
No significant toxicity was observed during the administration period, as indicated by stable body weight and the absence ofhair loss.
Animal Model: CT26 induced xenograft model established in female BALB/c mice (8 weeks old) [1]
Dosage: 50 mg/kg with or without anti-PD-L1
Administration: Intraperitoneal injection (i.p.), once daily for 20 days
Result: Showed significantly stronger anticancer effects in the combination therapy with PD-L1 blockade than ICIs monotherapy.
No significant toxicity was observed during the administration period, as indicated by stable body weight and the absence ofhair loss.
Promoted T cell-mediated immune activation and facilitates the conversion of cold tumor into hot tumor.
Significantly increased CD80 expression (M1 marker) and decreased CD206 levels (M2 marker).
Enhanced infiltration ofDiD-labeled PBMCs into tumor spheroids, as visualized by fluorescence imaging.
Molecular Weight

374.85

Formula

C13H19ClN6O3S
SMILES

O=C1NC(N=CN=C2N3CCC(CNS(N)(=O)=O)(CC3)CCl)=C2C1
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-27 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-27Phosphodiesterase (PDE)STINGStimulator of Interferon GenesTMEM173MITAERISMPYS4T1 cellsCT26 cellsTHP-1 cellsHCT116 cellsxenograft mice modelsInhibitorinhibitorinhibit

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