An ENPP1 inhibitor
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ENPP1 Inhibitor 4e

Item No. 37687

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
7-fluoro-2-(((5-methoxy-1H-imidazo[4,5-b]pyridin-2-yl)thio)methyl)quinazolin-4(3H)-one
Synonyms
  • cGAMP-compound 4e
Molecular Formula
C16H12FN5O2S
Formula Weight
357.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 1 mg/mlEthanol: Slightly solublePBS (pH 7.2): 0.25 mg/ml
λmax
226, 309 nm
SMILES
FC(C=C1)=CC2=C1C(NC(CSC3=NC4=NC(OC)=CC=C4N3)=N2)=O
InChi Code
InChI=1S/C16H12FN5O2S/c1-24-13-5-4-10-14(21-13)22-16(19-10)25-7-12-18-11-6-8(17)2-3-9(11)15(23)20-12/h2-6H,7H2,1H3,(H,18,20,23)(H,19,21,22)
InChi Key
PTZJKRPYZKMREN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $44

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    25 mg

    $120

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    50 mg

    $217

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    Cayman Chemical
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    Product Description

    ENPP1 inhibitor 4e is an inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase family member 1 (ENPP1; IC50 = 0.188 µM), an enzyme that degrades the stimulator of interferon genes (STING) activator 2'3'-cGAMP (Item No. 19887).1 It inhibits ENPP1 in MDA-MB-231 cells, which highly express ENPP1 (IC50 = 0.732 µM). ENPP1 inhibitor 4e is selectively cytotoxic to 4T1 murine metastatic breast cancer cells (IC50 = 2.99 µM) over non-cancerous L-02 and 293T cells at 50 µM. It increases serum levels of IFN-β in mice when administered at a dose of 0.5 mg/kg in combination with cGAMP when compared to mice administered only cGAMP or mice not receiving either compound, indicating that ENPP1 inhibitor 4e reduces the degradation of cGAMP.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, X., Lu, X., Yan, D., et al. Development of novel ecto-nucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) inhibitors for tumor immunotherapy. Int. J. Mol. Sci. 23(13), 7104 (2022).