A FEN1 inhibitor
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FEN1-IN-4

Item No. 37790

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-(cyclopropylmethyl)-3-hydroxy-2,4(1H,3H)-quinazolinedione
CAS Number
1995893-58-7
Synonyms
  • FEN1 Inhibitor 4
  • Flap Endonuclease 1-IN-4
  • Flap Endonuclease 1 Inhibitor 4
Molecular Formula
C12H12N2O3
Formula Weight
232.2
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Methanol: Soluble
SMILES
O=C1C2=C(N(CC3CC3)C(N1O)=O)C=CC=C2
InChi Code
InChI=1S/C12H12N2O3/c15-11-9-3-1-2-4-10(9)13(7-8-5-6-8)12(16)14(11)17/h1-4,8,17H,5-7H2
InChi Key
JAFLWTUYSKADJS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    25 mg

    $590

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    Cayman Chemical
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    Product Description

    FEN1-IN-4 is an inhibitor of flap endonuclease 1 (FEN1; IC50 = 30 nM for FEN1-336Δ).1 It also inhibits exonuclease 1 in a concentration-dependent manner. FEN1-IN-4 (10 µM) inhibits ATP-induced mitochondrial DNA (mtDNA) fragmentation and levels of cytosolic mtDNA in LPS-primed primary mouse bone marrow-derived macrophages (BMDMs).2 It also inhibits ATP-induced phosphorylation of STING in LPS-primed wild-type and Nlrp3-/- primary mouse BMDMs. FEN1-IN-4 (40 mg/kg) decreases peritoneal levels of IL-1β and neutrophil and monocyte infiltration in a mouse model of alum-induced peritonitis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Exell, J.C., Thompson, M.J., Finger, L.D., et al. Cellularly active N-hydroxyurea FEN1 inhibitors block substrate entry to the active site. Nat. Chem. Biol. 12(10), 815-821 (2016).

    2. Xian, H., Watari, K., Sanchez-Lopez, E., et al. Oxidized DNA fragments exit mitochondria via mPTP- and VDAC-dependent channels to activate NLRP3 inflammasome and interferon signaling. Immunity 55(8), 1370-1385 (2022).