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FLAP

FLAP (Arachidonate 5-lipoxygenase-activating protein) is an integral membrane protein, it facilitates the transfer of the substrate arachidonic acid (AA) to 5-lipoxygenase (5-LO) to produce leukotrienes (LTs), and is shown to be indispensable for cellular LT biosynthesis. FLAP transfers arachidonic acid to 5-LOX protein, thereby enabling this enzyme to efficiently produce oxidized lipid products (mainly eicosanoids) that are important in cell growth, differentiation and death particularly apoptosis.

  • MK-886
    T6893118414-82-7
    MK-886 (L 663536) is an inhibitor of leukotriene biosynthesis, inhibiting 5-lipoxygenase-activating protein (FLAP). It is also a moderately potent PPARα antagonist.
    • $30
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    TargetMol | Citations Cited
  • sEH/FLAP-IN-1
    T81181
    sEH/FLAP-IN-1 (Compound 46A) serves as a dual inhibitor targeting both sEH and FLAP. It effectively suppresses 5-LOX product formation with an EC50 of 11 nM in SACM-stimulated PBMCs and also inhibits sEH activity (EC50: 18 nM) as well as thromboxane production. This compound is utilized in the study of inflammatory diseases [1].
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    TargetMol | Inhibitor Sale
  • Atuliflapon
    T90232041075-86-7
    Atuliflapon (AZD5718) is a novel 5-Lipoxygenase Activating Protein(FLAP) inhibitor for Treatment of Coronary Artery Disease.
    • $73
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  • Diflapolin
    T8844724453-98-9
    Diflapolin is a highly active dual 5-lipoxygenase-activating protein (FLAP)/soluble epoxide hydrolase (sEH) inhibitor with marked anti-inflammatory efficacy and high target selectivity.
    • $38
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  • Fiboflapon
    T11487936350-00-4
    Fiboflapon (GSK2190915) is an orally available and effective 5-lipoxygenase-activating protein (FLAP) inhibitor that binds FLAP with a titer of 2.9 nM and inhibition of LTB4 in human blood with an IC50 of 76 nM.
    • $51
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  • AM103
    T103141147872-22-7
    AM103 is an effective and selective inhibitor of FLAP (IC50 = 4.2 nM).
    • $146
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  • FEN1-IN-6
    T79134824983-84-8
    FEN1-IN-6 (compound 9) is a potent Flap endonuclease-1 (FEN1, IC50 = 10 nM) inhibitor, crucial for DNA damage repair in mammalian cells, and additionally targets the related endonuclease xeroderma pigmentosum G (XPG) with an IC50 of 23 nM [1].
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  • FEN1-IN-7
    T79135824983-90-6
    FEN1-IN-7 (compound 16), a selective Flap endonuclease-1 (FEN1) inhibitor with an IC50 of 18 nM, plays a role in DNA damage repair in mammalian cells. Additionally, it targets the related endonuclease, xeroderma pigmentosum G (XPG), with an IC50 of 3.04 μM. FEN1-IN-7 enhances the sensitivity of cancer cells to potent DNA alkylating or methylating agents [1].
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  • LTB4-IN-2
    T79389
    LTB4-IN-2 (Compound 6x) is a selective inhibitor of Leukotriene B4 (LTB4), acting by specifically targeting the 5-Lipoxygenase-activating protein (FLAP) with an inhibitory concentration (IC 50) of 1.15 μM, thus serving as a potential agent for anti-inflammatory research [1].
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  • Quiflapon
    T16087136668-42-3
    Quiflapon (MK-591) causes cell apoptosis. Quiflapon is a selective and specific 5-lipoxygenase-activating protein (FLAP) inhibitor (IC50: 1.6 nM in a FLAP binding assay) and is also an effective and orally active Leukotriene biosynthesis (LT) inhibitor (IC50: 3.1 and 6.1 nM in intact human and elicited rat PMNLs, respectively).
    • $40
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  • FEN1-IN-5
    T78192824983-93-9
    FEN1-IN-5 (compound 12A) is a potent Flap endonuclease-1 (FEN1) inhibitor with an IC50 value of 12 nM, playing a role in DNA repair mechanisms [1].
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  • Quiflapon sodium
    TQ0098147030-01-1
    Quiflapon sodium (MK591) is a selective inhibitor of 5-Lipoxygenase-activating protein (FLAP).
    • $85
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