U-73122 is an inhibitor of phospholipase C (PLC), phospholipase A2, and 5-LO (5-lipoxygenase).
AHR-5333 is a selective human blood neutrophil 5-lipoxygenase inhibitor. AHR-5333 exhibits potent, long-acting activity in rat and guinea pig in vivo models of immediate hypersensitivity[1].
Zileuton-d4 (A 64077-d4) is the deuterium labeled Zileuton. Zileuton (A 64077) is a potent and selective inhibitor of 5-lipoxygenase with antiasthmatic properties[1][2].
Murraol (CM-c2), a coumarin, can be isolated from the leaves of Madagascar pine cork (Apiaceae). Murraol has cyclooxygenase (COX) and lipoxygenase inhibitory properties and has an inhibitory effect on the growth of cancer cells[1].
2,3,4'-Trihydroxy-3',5'-dimethoxypropiophenone, isolated from Parinari hypochrysea (Chrysobalanaceae), exhibits antioxidant and lipoxygenase inhibition[1].
Xanthatin is isolated from Xanthium strumarium leaves. Xanthatin exhibits strong antitumor activities against a variety of cancer cells through apoptosis persuasion and shows anti-inflammatory activities by inhibiting PGE2 synthesis and 5-lipoxygenase activity[1]. Xanthatin is a potent and orally active inhibitor of VEGFR2 kinase activity with an IC50 of 3.8 μM and prominently blocks the phosphorylation of VEGFR2 at Tyr951 site. Xanthatin inhibits angiogenesis and has the potential for the investigation of breast cancer[2].
CCT 365623(CCT365623, CCT-365623) is a potent, orally active small molecule inhibitor of lysyl oxidase (LOX) with IC50 of 0.89 uM; inhibits LOX actvity in living cell system (MDCK cysts) at 5 uM, reduces EGFR retention at the cell surface, suppresses EGFR and AKT phosphorylation driven by EGF, also activates SMAD2 and downregulates MATN2; delays the growth of primary and metastatic tumour cells in vivo.
LP117 is a novel and potent inhibitor of 5-Lipoxygenase (5-LO) product synthesis with an IC50 of 1.1 μM.
RS4317 is a topically effective 5-lipoxygenase (5-LO) inhibitor.
Veliflapon (BAY X 1005; DG-031) is an orally active inhibitor of the synthesis of the leukotrienes B4 and C4[1]. Veliflapon is shown to be a selective inhibitor of the formation of 5-lipoxygenase-derived metabolites in vitro, without effects on other routes of arachidonic acid metabolism[2].
Nordihydroguaiaretic acid is a 5-lipoxygenase (5LOX) (IC50=8±3 μM) and tyrosine kinase inhibitor.
ALR-38 is a 5-lipoxygenase (5-LOX) inhibitor (IC50: 1.1 μM) with anti-inflammatory activity. ALR-38 effectively reduces ROS levels in neutrophils[1].
PGS-IN-1 is a potent inhibitor of prostaglandin synthetase (PGS) with an IC50 of 0.28 μM; also inhibits 5-lipoxygenase with an IC50 of 1.05 μM.
(-)-Dihydroguaiaretic acid is a Lipoxygenase inhibitor that has antioxidant activity. (-)-Dihydroguaiaretic acid inhibits the oxidation of unsaturated fatty acids and removes free radicals. (-)-Dihydroguaiaretic acid also has anticancer activity with an IC50 value of 7.49 μM (A549 cells)[1][2].
ML355 is a potent and selective inhibitors of 12-Lipoxygenase(12-LOX) with IC50 of 0.34 μM, excellent selectivity over related lipoxygenases and cyclooxygenases, and possess favorable ADME properties.IC50 value: 0.34 μM [1]Target: 12-LOXML355 inhibits PAR-4 induced aggregation and calcium mobilization in human platelets and reduce 12-HETE in β-cells.
RWJ 63556 is an orally active COX-2 selective/5-lipoxygenase inhibitor, with anti-inflammatory activities.
Cirsiliol is a potent and selective 5-lipoxygenase inhibitor and a competitive low affinity benzodiazepine receptor ligand.
4',5-Dihydroxyflavone is a soybean LOX-1 and yeast α-Glucosidase inhibitor, with an Ki of 102.6 μM for soybean LOX-1 and an IC50 of 66 μM for yeast α-glucosidase.
Phenethyl ferulate is a major constituent ofQianghuo, shows inhibitory activity against cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) with IC50 values of 4.35 μM and 5.75 μM, respectively[1].
Enazadrem is a 5-lipoxygenase inhibitor with antiinflammatory activities.
COX-2/5-LOX-IN-3 (compound 5b) is a potent and dual COX-2/5-LOX inhibitor with IC50 values of 45.73, 5.45 and 4.33 μM for COX-1, COX-2, and 5-LOX, respectively. COX-2/5-LOX-IN-3 has the potential for the research of inflammation diseases[1].
L 691816 is a potent, selective and orally active inhibitors of 5-lipoxygenase. L 691816 can be used for the research of allergies and asthma[1].
Wedelolactone, a natural product from Ecliptae herba, suppresses LPS-induced caspase-11 expression by directly inhibiting the IKK Complex[1]. Wedelolactone inhibits 5-lipoxygenase (5-Lox) (IC50~2.5 μM) activity by an oxygen radical scavenging mechanism. Wedelolactone induces caspase-dependent apoptosis in prostate cancer cells via downregulation of PKCε without inhibiting Akt[2]. Anti-cancer, anti-inflammatory, and antioxidant activities[3].
5-LOX-IN-2, an inhibitor of 5-lipoxygenase (5-LOX) with an IC50 of 0.33 μM, inhibits 5-LOX in a dose-dependent manner . 5-LOX-IN-2, reduces the cell viability of renal cancer cells and induces apoptosis, can be used for cancer research[1].
Docebenone (AA 861) is a potent, selective and orally active 5-LO (5-lipoxygenase) inhibitor.
YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC50=3.4 μM) and 5-lipoxygenase (5-LOX; IC50=6.5 μM). YS121 dose- dependently reduces PGE2 production with EC50=12 μM in IL-1β-stimulated A549 cells[1].
HZ52 is a potent, reversible 5-lipoxygenase inhibitor, blocking leukotriene synthesis with an IC50 of 0.7 μM in intact human polymorphonuclear leukocytes[1].
4-Nitrocatechol is a potent lipoxygenase inhibitor[1].
UCB-35440, a 5-lipoxygenase inhibitor and a histamine H1 receptor antagonist, is used potentially for the treatment of dermatitis.
BW 755C is a 5-lipoxygenase (5-LO) inhibitor with an IC50 of 5 μM. BW 755C also inhibits cyclooxygenase (COX) with IC50s of 0.65 and 1.2 μg/mL against COX-1 and COX-2, respectively[1][2].