flap

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].

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.

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.

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

Quiflapon sodium (MK591) is a selective inhibitor of 5-Lipoxygenase-activating protein (FLAP).

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).

Veliflapon is an orally active and selective inhibitor of 5-lipoxygenase activating protein (FLAP). Veliflapon inhibits the synthesis of the leukotrienes B4 and C4.

Fiboflapon sodium (GSK2190915) is an 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.

Eflapegrastim, a humanized IgG4 monoclonal antibody and granulocyte colony-stimulating factor (G-CSF), targets the G-CSF receptor (c-Fms). It promotes the proliferation and differentiation of neutrophil progenitor cells, ensuring a stable count of mature and functional neutrophils, and effectively shortens the duration of neutropenia [1].

FEN1-IN-5 (compound 12A) is a potent inhibitor of Flap endonuclease-1 (FEN1) with an IC50 of 12 nM, contributing to DNA repair mechanisms [1].

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].

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].

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].

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.

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

FEN1-IN-1 (LNT-1) is an inhibitor of flap endonuclease 1 (FEN1). FEN1-IN-1 binds to the active site of FEN1. It partly achieves inhibition by the co-ordination of Mg2+ ions.

FEN1-IN-3 is a human flap endonuclease-1 ( hFEN1 ) inhibitor that stabilizes hFEN1 with an EC 50 of 6.8 μM .

(S)-BI 665915 is an orally active inhibitor of oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) with an IC50 of 1.7 nM for FLAP binding.

FEN1-IN-2 is a selective and potent inhibitor of flap endonuclease 1 (FEN1), inhibits FEN1 and XPG, has potential anticancer activity, and can be used to study DNA damage repair.

FEN1-IN-4 (FEN1 Inhibitor C2) is an inhibitor of human flap endonuclease-1 (hFEN1)

AZD5718 is a potent and selective FLAP inhibitor (IC50 = 2.0 nM) for Treatment of Coronary Artery Disease. AZD5718 demonstrated a dose dependent and greater than 90% suppression of leukotriene production over 24 h. Preclinical toxicology studies in rat and dog did not show any serious adverse events of clinical significance. Currently, AZD5718 is evaluated in a phase 2a study for treatment of coronary artery disease.

AM679 is a potent and selective FLAP inhibitor with IC50s of 2.2 nM/0.6 nM/154 nM for FLAP binding/hLA/hWB respectively. IC50 value: 2.2 nM/0.6 nM/154 nM(FLAP binding/hLA/hWB) [1] AM679 showed an improved CYP inhibition profile (IC50 3A4 = 16.7 lM, 2C9 =

JFD00950 is a human flap endonuclease 1 (FEN1) inhibitor with in vitro inhibition of flap cleavage activity as well as cytotoxic activity against a colon cancer cell line, DLD-1.

ALR-27 serves as an antagonist of the 5-lipoxygenase (5-LOX) activating protein FLAP and exhibits anti-inflammatory properties. It effectively inhibits 5-LOX product formation (>80%) in pro-inflammatory M1-MDM without significantly inhibiting 5-LOX directly. Additionally, ALR-27 decreases prostaglandin and leukotriene (LT) production in neutrophils and enhances the production of specialized prolytic mediators in certain human macrophage phenotypes [1].