FLAP

AZD6642 is an inhibitor of 5-Lipoxygenase Activating Protein (FLAP) for the treatment of inflammatory diseases.

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.

MK-0591 is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor with an IC50 value of 1.6 nM in a FLAP binding assay.

MK591 is selective and specific inhibitor of 5-Lipoxygenase-activating protein (FLAP).

GSK2190915 is a potent FLAP(5-Lipoxygenase-activating protein) inhibitor with binding IC50 of 2.9 nM.

AM 103 is a potent and selective FLAP inhibitor, with an IC50 value of 4.2 nM.

MK-886 sodium salt is a potent inhibitor of the 5-lipoxygenase-activating protein (FLAP), exhibiting an IC50 of 30 nM. It effectively inhibits leukotriene biosynthesis with IC50 values of 3 nM in intact leukocytes and 1.1 μM in human whole blood. Additionally, MK-886 acts as a non-competitive antagonist of PPARα and can induce apoptosis, making it a valuable tool for research in inflammatory diseases and apoptosis pathways.

FEN1-IN-1 is a selective inhibitor of flap endonuclease 1 (FEN1), demonstrating significant antitumor activity. It functions by binding to the active site of FEN1, with inhibition partially facilitated by the coordination of Mg2+ ions. This compound triggers a DNA damage response, subsequently activating the ATM checkpoint signaling pathway, leading to the phosphorylation of histone H2AX and the ubiquitination of FANCD2 in mammalian cells. FEN1-IN-1 is a valuable tool for cancer research, particularly in studies focused on DNA repair mechanisms and tumor progression.

FEN1-IN-SC13 is a selective inhibitor of DNA fragmentation endonuclease 1 (FEN1), pivotal in DNA replication and repair processes. This compound demonstrates significant antitumor activity by disrupting the normal functioning of FEN1, leading to impaired DNA metabolism in vitro and within cellular environments. It serves as a valuable tool for researchers investigating the mechanisms of DNA damage response and the development of cancer therapeutics.

MU1409 is a selective inhibitor of the MRE11 nuclease, exhibiting an IC50 of 12.1 μM. Additionally, MU1409 inhibits FEN1 and EXO1, with IC50 values of 24.2 μM and 176.4 μM, respectively. This compound plays a crucial role in modulating DNA repair mechanisms, particularly in BRCA2-deficient cells, by preventing the degradation of stalled replication forks. MU1409 shows promise for research focused on BRCA2 mutation-related cancers and the mechanisms of genomic instability.

FEN1-IN-4 is a selective inhibitor of human flap endonuclease-1 (hFEN1), targeting the enzyme's crucial role in DNA replication and repair. This compound demonstrates significant biological activity by obstructing hFEN1's enzymatic function, which is essential for maintaining genomic stability. FEN1-IN-4 is valuable for research applications in cancer biology and the study of DNA repair mechanisms, providing insights into potential therapeutic strategies for related diseases.

BRP-7 is a highly selective FLAP inhibitor with an IC50 of 0.31 μM. By targeting the 5-lipoxygenase activating protein (FLAP), BRP-7 effectively interrupts the co-localization of FLAP and 5-lipoxygenase, inhibiting the transfer of arachidonic acid and consequently reducing leukotriene production (IC₅₀ = 0.15 μM). It does not inhibit cyclooxygenase (COX-1/COX-2) or microsomal prostaglandin E₂ synthase-1 (mPGES-1), and maintains cell viability. BRP-7 has demonstrated significant anti-inflammatory properties in rodent models of pleurisy and peritonitis, making it a valuable tool for investigating inflammatory diseases.

FEN1-IN-2 is a selective inhibitor of flap endonuclease 1 (FEN1), demonstrating an IC50 of 3 nM. It exhibits significantly lower activity against XPG, with an IC50 of 226 nM. This compound is valuable for investigating FEN1's role in DNA repair processes and its potential implications in cancer research. Researchers can utilize FEN1-IN-2 to study mechanisms of cellular response to DNA damage and identify therapeutic strategies targeting FEN1-related pathways.

Atuliflapon (AZD5718) is a potent, orally active inhibitor of FLAP (5-Lipoxygenase Activating Protein), exhibiting an IC50 of 2 nM. This compound is primarily utilized in research related to inflammatory processes, particularly in the context of coronary artery disease. Its selective inhibition of FLAP contributes to the regulation of leukotriene biosynthesis, making it a valuable tool for investigating therapeutic strategies for cardiovascular conditions.

Diflapolin is a potent dual inhibitor of 5-lipoxygenase-activating protein (FLAP) and soluble epoxide hydrolase (sEH), demonstrating significant anti-inflammatory effects and high target selectivity. It effectively inhibits the formation of 5-LOX products in human monocytes and neutrophils with IC50 values of 30 nM and 170 nM, respectively, while also inhibiting isolated sEH with an IC50 of 20 nM. This compound is valuable for research into inflammatory pathways and related therapeutic interventions.

MSC778 is a potent and orally bioavailable inhibitor of flap endonuclease 1 (FEN1), exhibiting an IC50 of 3 nM and a KD of 2.9 nM. It demonstrates significant selectivity with 145-fold, 516-fold, and 65-fold greater inhibition over EXO1, GEN1, and XPG, respectively. MSC778 preferentially induces apoptosis in BRCA2-deficient cells and enhances the efficacy of Niraparib in tumor stasis within BRCA2 knockout DLD-1 mouse xenografts. This compound is valuable for research focused on colorectal cancer.

FEN1-IN-7 is a selective inhibitor of Flap endonuclease-1 (FEN1), with an IC50 of 18 nM, crucial for DNA repair in mammalian cells. In addition, it exhibits activity against xeroderma pigmentosum G (XPG) with an IC50 of 3.04 μM. FEN1-IN-7 enhances the sensitivity of cancer cells to DNA alkylating and methylating agents, making it a valuable tool for research in cancer therapy and DNA damage response mechanisms.

FEN1-IN-5 is a potent inhibitor of Flap endonuclease-1 (FEN1) with an IC50 of 12 nM. FEN1 plays a crucial role in DNA repair processes, particularly in the maturation of Okazaki fragments during DNA replication. This compound serves as a valuable tool in research applications aimed at dissecting the mechanisms of DNA repair and exploring potential therapeutic targets for conditions associated with FEN1 dysfunction.

FEN1-IN-6 is a potent inhibitor of Flap endonuclease-1 (FEN1), with an IC50 of 10 nM. This compound plays a significant role in cellular mechanisms for DNA damage repair, enhancing research into DNA repair processes. Additionally, FEN1-IN-6 exhibits activity against the related endonuclease xeroderma pigmentosum G (XPG) with an IC50 of 23 nM, making it a valuable tool for studying nucleic acid metabolism and repair pathways.

FEN1-IN-3 is a selective inhibitor of human flap endonuclease-1 (hFEN1), a crucial enzyme involved in DNA replication and repair. With an EC50 value of 6.8 µM, FEN1-IN-3 effectively stabilizes hFEN1, making it a valuable tool for studying DNA metabolic processes. This compound is suitable for research applications focused on cancer biology, gene expression regulation, and the exploration of therapeutic strategies targeting DNA repair mechanisms.

(S)-BI 665915 is a potent FLAP (5-lipoxygenase-activating protein) inhibitor with an IC50 of 1.7 nM, effectively targeting FLAP binding. This compound demonstrates functional inhibition of FLAP in human whole blood with an IC50 of 45 nM and exhibits favorable drug metabolism and pharmacokinetics (DMPK) across species. (S)-BI 665915 provides dose-dependent inhibition of leukotriene B4 (LTB4) production, making it a valuable tool for research into inflammatory responses and related biological pathways.

BI 665915 is a potent oral inhibitor of the 5-lipoxygenase-activating protein (FLAP). By inhibiting FLAP, this compound effectively blocks the biosynthesis of leukotriene B4 (LTB4), making it a valuable tool for exploring inflammatory pathways. BI 665915 has potential applications in research related to various inflammatory diseases, including those affecting the respiratory and cardiovascular systems.

L-669083 is a potent FLAP (5-lipoxygenase-activating protein) inhibitor that specifically targets leukotriene biosynthesis. It is structurally derived from a combination of indole and quinoline, showcasing significant activity in disrupting leukotriene production. Research applications include studying inflammatory responses and evaluating the role of leukotrienes in various disease models, making L-669083 a valuable tool in pharmacological investigations related to inflammation and related pathologies.

L 689037 is a potent leukotriene biosynthesis inhibitor that targets the 5-lipoxygenase-activating protein (FLAP). This compound effectively disrupts the synthesis of leukotrienes, which are mediators of inflammation. L 689037 is valuable for research applications related to asthma and inflammatory bowel disease, aiding in the investigation of therapeutic strategies to mitigate these inflammatory conditions.

AM103 (free acid) is a selective inhibitor of 5-lipoxygenase activating protein (FLAP), effectively blocking the initial step of the leukotriene biosynthetic pathway. This compound demonstrates significant inhibition of leukotriene B4 and cysteinyl leukotriene production, exhibiting notable anti-inflammatory properties in murine models of chronic lung inflammation. Additionally, AM103 (free acid) has been shown to enhance survival in mice challenged with platelet-activating factor, making it a valuable tool for research into respiratory disorders, including asthma.

ALR-6 is a selective antagonist of the 5-lipoxygenase-activating protein (FLAP), known for its anti-inflammatory properties. This compound effectively inhibits the formation of 5-LOX products by more than 80% in pro-inflammatory M1 monocyte-derived macrophages (MDM), while demonstrating minimal direct inhibition of 5-LOX activity. ALR-6 is valuable for research applications aimed at exploring inflammatory pathways and potential therapeutic interventions in inflammatory diseases.

FLAP-IN-1 is a potent 5-lipoxygenase-activating protein (FLAP) inhibitor, exhibiting an IC50 value of 654 nM. This compound is useful for investigating the role of FLAP in inflammatory pathways and its potential implications in cardiovascular disease research. Researchers can leverage FLAP-IN-1 to explore therapeutic strategies targeting leukotriene biosynthesis and related conditions.

FEN1-IN-8 is a selective inhibitor of flap endonuclease 1 (FEN1), exhibiting an IC50 of less than 100 nM for FEN1 and a range of 100 nM to 1 μM for exonuclease 1 (EXO1). This compound serves as a valuable tool for studying the role of FEN1 in colorectal and gastric cancers, providing insights into tumor biology and potential therapeutic pathways. FEN1-IN-8 is suitable for research applications focused on understanding DNA repair mechanisms and their implications in cancer progression.

ALR-27 is a selective antagonist of the 5-lipoxygenase activating protein (FLAP), exhibiting significant anti-inflammatory properties. This compound effectively inhibits the formation of 5-LOX products by more than 80% in pro-inflammatory M1 macrophage-derived macrophages (M1-MDM), without directly inhibiting 5-LOX activity. Additionally, ALR-27 reduces the production of prostaglandins and leukotrienes in neutrophils while promoting the synthesis of specialized pro-resolving mediators in distinct human macrophage phenotypes. These characteristics make ALR-27 valuable for research in inflammation and immune response modulation.

Fiboflapon sodium is a potent inhibitor of the 5-lipoxygenase-activating protein (FLAP) with a binding affinity of 2.9 nM. It has an IC50 value of 76 nM for the inhibition of leukotriene B4 (LTB4) in human blood. This compound is valuable in research applications focused on inflammation and related diseases by modulating leukotriene synthesis. Its oral bioavailability makes it suitable for in vivo studies investigating FLAP-related pathways.

Veliflapon is a selective 5-lipoxygenase activating protein (FLAP) inhibitor. This compound effectively inhibits the synthesis of leukotrienes B4 and C4, thereby modulating inflammatory responses. Its primary application lies in research focused on asthma, allergies, and other inflammatory conditions, making it a valuable tool for studying leukotriene-mediated pathways.

(S)-Veliflapon is a potent inhibitor of leukotriene biosynthesis targeting the 5-lipoxygenase activating protein (FLAP). It effectively 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. Additionally, (S)-Veliflapon demonstrates enantioselectivity in human whole blood, making it a valuable reagent for research in inflammation and related biological processes.