2. Signaling Pathways
  3. Immunology/Inflammation
  4. FLAP

FLAP

5-lipoxygenase-activating protein; 5-LO activating protein

FLAP

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FLAP (Arachidonate 5-lipoxygenase-activating protein) is an integral membrane protein, which 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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-14166
    MK-886
    		Inhibitor 99.87%
    MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis.
    MK-886
  • HY-123834
    FEN1-IN-1
    		Inhibitor 99.85%
    FEN1-IN-1 (compound 1) is a small molecule flap endonuclease 1 (FEN1) inhibitor with antitumor activity. FEN1-IN-1 binds to the active site of FEN1 and partly achieves inhibition by the co-ordination of Mg2+ ions. FEN1-IN-1 initiaties a DNA damage response and activates the ATM checkpoint signalling pathway, the phosphorylation of histone H2AX and the ubiquitination of FANCD2 in mammalian cells. FEN1-IN-1 is promising for research of cancers.
    FEN1-IN-1
  • HY-10037
    Quiflapon
    		Inhibitor 99.44%
    Quiflapon (MK-591) is a selective and specific 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.6 nM in a FLAP binding assay. Quiflapon is also a potent and orally active Leukotriene biosynthesis (LT) inhibitor, shows IC50 values of 3.1 and 6.1 nM in intact human and elicited rat PMNLs, respectively. Quiflapon induces cell apoptosis.
    Quiflapon
  • HY-136485
    FEN1-IN-4
    		Inhibitor 99.86%
    FEN1-IN-4 (Compound 2) is a human flap endonuclease-1 (hFEN1) inhibitor.
    FEN1-IN-4
  • HY-15874
    Fiboflapon
    		Inhibitor 99.50%
    Fiboflapon (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
    Fiboflapon
  • HY-125089
    AM-643
    		Inhibitor
    AM-643 is a FLAP inhibitor with human IC50 of 2 nM, oral activity, and dermal activity.AM-643 selectively inhibits FLAP, reduces leukotriene biosynthesis and reduces inflammatory ear swelling.AM-643 can be used for the research of skin disorders involving leukotriene production.
    AM-643
  • HY-185455
    FEN1-IN-9
    		Inhibitor
    FEN1-IN-9 is a selective flap endonuclease 1 (FEN1) inhibitor with an IC50 of 37.9 μM. FEN1-IN-9 can be used for the research of DNA damage repair.
    FEN1-IN-9
  • HY-120580
    L 689037
    		Ligand
    L 689037 is a leukotriene biosynthesis (LT) inhibitor and a 5-lipoxygenase-activating protein (FLAP) binder. [125I]-L 691,831 serves as a standard probe to precisely locate the key structural domains that determine the binding of inhibitors to FLAP. L 689037 can be used in the research of asthma and inflammatory bowel disease.
    L 689037
  • HY-50714
    Quiflapon sodium
    		Inhibitor 98.72%
    Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. Quiflapon sodium is an orally active Leukotriene biosynthesis inhibitor. Induces apoptosis.
    Quiflapon sodium
  • HY-122695
    FEN1-IN-2
    		Inhibitor 99.94%
    FEN1-IN-2 (compound 20) is a flap endonuclease 1 (FEN1) inhibitor, with IC50 values of 3 nM and 226 nM for FEN1 and XPG, respectively.
    FEN1-IN-2
  • HY-122908
    Atuliflapon
    		Inhibitor 98.97%
    Atuliflapon (AZD5718) is an orally active inhibitor of FLAP (5?Lipoxygenase activating protein), with an IC50 of 2 nM. Atuliflapon is used in the study for coronary artery disease.
    Atuliflapon
  • HY-128171
    Diflapolin
    		Inhibitor 99.33%
    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. Diflapolin inhibits 5-LOX product formation in intact human monocytes and neutrophils with IC50s?of? 30 and 170?nM, respectively, and suppressed the activity of isolated sEH (IC50=20?nM).
    Diflapolin
  • HY-177512
    MSC778
    		Inhibitor
    MSC778 is an effective and orally active flap endonuclease 1 (FEN1) inhibitor with an IC50 of 3 nM and a KD of 2.9 nM. MSC778 exhibits 145-fold, 516-fold, and 65-fold selectivity over EXO1, GEN1, and XPG, respectively. MSC778 selectively kills BRCA2-deficient cells and potentiates the activity of Niraparib (HY-10619) to induce tumor stasis in a BRCA2 KO DLD-1 mouse xenograft. MSC778 can be used in the research of colorectal cancer.
    MSC778
  • HY-14460
    AM679
    		Inhibitor 99.72%
    AM679 is a potent, selective 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 2 nM in a human FLAP membrane binding assay. AM679 markedly reduces the respiratory syncytial virus-driven ocular pathology as well as the synthesis of cysteinyl leukotrienes (CysLTs) in the eye.
    AM679
  • HY-15874A
    Fiboflapon sodium
    		Inhibitor 98.51%
    Fiboflapon sodium (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
    Fiboflapon sodium
  • HY-153792
    FEN1-IN-7
    		Inhibitor 99.85%
    FEN1-IN-7 (compound 16) is a selective inhibitor of Flap endonuclease-1 (FEN1, IC50=18 nM), involving in mammalian cells to repair DNA damage. FEN1-IN-7 also targets to related endonuclease, xeroderma pigmentosum G (XPG) with an IC50 value of 3.04 μM. FEN1-IN-7 increases the cellular sensitivity of cancer cells to potent DNA alkylating agents or methylating agents.
    FEN1-IN-7
  • HY-14165
    Veliflapon
    		Inhibitor 99.31%
    Veliflapon (BAY X 1005; DG-031) is an orally active and selective 5-lipoxygenase activating protein (FLAP) inhibitor. Veliflapon inhibits the synthesis of the leukotrienes B4 and C4.
    Veliflapon
  • HY-153790
    FEN1-IN-5
    		Inhibitor 99.79%
    FEN1-IN-5 (compound 12A) is a potent inhibitor of Flap endonuclease-1 (FEN1, IC50=12 nM), involving in DNA repair.
    FEN1-IN-5
  • HY-14165A
    (S)-Veliflapon
    		Inhibitor 99.25%
    (S)-Veliflapon ((S)-BAY X 1005) is an orally active inhibitor of leukotriene biosynthesis and 5-lipoxygenase activating protein (FLAP). (S)-Veliflapon inhibits the formation of leukotriene B4 (LTB4) in rat, mouse and human leukocytes with IC50 values of 0.026 µM, 0.039 µM and 0.22 µM respectively. (S)-Veliflapon showes enantioselectivity in human whole blood.
    (S)-Veliflapon
  • HY-153791
    FEN1-IN-6
    		Inhibitor
    FEN1-IN-6 (compound 9) is a potent inhibitor of Flap endonuclease-1 (FEN1, IC50=10 nM), involving in mammalian cells to repair DNA damage. FEN1-IN-6 also targets to related endonuclease, xeroderma pigmentosum G (XPG) with an IC50 value of 23 nM.
    FEN1-IN-6
Cat. No. Product Name / Synonyms Application Reactivity