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Immunology/Inflammation

Aryl Hydrocarbon Receptor

Immunology/Inflammation related

NOD-like Receptor (NLR)

Prostaglandin Receptor

Reactive Oxygen Species

Thrombopoietin Receptor

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.

Filter HomeSignaling PathwaysImmunology/InflammationFLAP

AM103

T103141147872-22-7

AM103 is an effective and selective inhibitor of FLAP (IC50 = 4.2 nM).

$146

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MK-886

T6893118414-82-7

MK-886 (L 663536) is an inhibitor of leukotriene biosynthesis, acting by inhibiting the 5-lipoxygenase-activating protein (FLAP), and serves as a moderately potent PPARα antagonist.

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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).

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Atuliflapon

T90232041075-86-7

Atuliflapon (AZD5718) is a novel 5-Lipoxygenase Activating Protein(FLAP) inhibitor for Treatment of Coronary Artery Disease.

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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.

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Diflapolin

T8844724453-98-9

Diflapolin is a highly active dual 5-lipoxygenase-activating protein (FLAP) and soluble epoxide hydrolase (sEH) inhibitor, exhibiting marked anti-inflammatory efficacy and high target selectivity.

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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 also targets the related endonuclease xeroderma pigmentosum G (XPG) with an IC50 of 23 nM [1].

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8-10 weeks

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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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8-10 weeks

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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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sEH/FLAP-IN-1

T81181

sEH FLAP-IN-1 (Compound 46A) serves as a dual inhibitor targeting both sEH and FLAP, effectively suppressing 5-LOX product formation with an EC50 of 11 nM in SACM-stimulated PBMCs, inhibiting sEH activity (EC50: 18 nM), and reducing thromboxane production. This compound is utilized in the study of inflammatory diseases [1].