lipoxygenase

5-Lipoxygenase-In-1 (compound example 4.10) is a 5-Lipoxygenase inhibitor.

15-Lipoxygenase Inhibitor 1 is a selective inhibitor of 15-lipoxygenase, with an IC50 of 18 μM. 4-MMPB (15-Lipoxygenase Inhibitor 1) has IC50s of 19.5 μM and 19.1 μM for soybean 15-lipoxygenase (SLO) and human 15-lipoxygenase-1 (15-LOX-1), respectively. 4-MMPB has potential for the research of prostate cancer.

A-69412 (N-1-(Fur-3-ylethyl)-N-hydroxyurea) is a reversible, specific inhibitor of the hydrophilic 5-lipoxygenase. It has the potential to treat ulcerative colitis and asthma, and possibly other inflammatory and allergic conditions.

RWJ 63556, an orally active inhibitor of COX-2 selective [5-lipoxygenase], exhibits anti-inflammatory activities.

PF-4191834 is a noniron chelating and non-redox inhibitor of the 5-Lipoxygenase (5-LOX) with an IC50 of 229 nM. PF-4191834 shows ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX and displays no activity toward the cyclooxygenase enzymes. PF-4191834

Bunaprolast (U66858) is a novel and potent leukotriene B4 (LTB4) inhibitor.Bunaprolast exhibits oxidative degradation activity and inhibits lipoxygenase and TXB2 release.

CJ-13,610 is an orally active and nonredox-type inhibitor of 5-lipoxygenase (5-LOX). CJ-13,610 inhibits the biosynthesis of leukotriene B4 and regulates the expression of IL-6 mRNA in macrophages.

Efletirizine (UCB-28754) is a histamine receptor antagonist with inhibitory effects on the enzyme 5-lipoxygenase (5-LO), and is useful in the topical treatment of allergic diseases.

ER-34122, a novel orally available dual 5-lipoxygenase/cyclooxygenase inhibitor, exhibits potent anti-inflammatory activity in an arachidonic acid-induced ear inflammation model.

Phenidone (1-phenyl-3-pyrazolidinone) is a dual inhibitor of cyclooxygenases and lipoxygenases that ameliorates rat paralysis in experimental autoimmune encephalomyelitis by suppressing its target enzymes[1]. The lipoxygenase inhibitor phenidone is a potent hypotensive agent in the spontaneously hypertensive rat[2].

Esculetin (Cichorigenin) is a coumarin derivative from various natural plant products with various biological and pharmaceutical properties including anti-edema, anti-inflammatory and anti-tumour effects. It inhibits lipoxygenases (LOs).

2,5-Di-tert-butylhydroquinone (BHQ) is an effective and selective endoplasmic reticulum Ca2+-ATPase inhibitor.

FPL 62064 is a potent dual inhibitor of 5-lipoxygenase (5-LOX) and COX (IC50 of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and prostaglandin synthetase, respectively).

PGS-IN-1 (KME-4) is a potent inhibitor of prostaglandin synthetase (PGS, IC50: 0.28 μM) and 5-lipoxygenase (IC50: 1.05 μM).

AZD 4407 is a potent inhibitor of 5-lipoxygenase.

Cirsiliol is a 5-lipoxygenase (5-LOX) inhibitor and low affinity benzodiazepine receptor ligand.Cirsiliol inhibits cell proliferation and promotes apoptosis of OS cells.Cirsiliol shows antitumor activity against OS cells in an in situ xenograft tumor model and can be used to study colon cancer.

Enazadrem, a 5-lipoxygenase inhibitor, exhibits anti-inflammatory activities.

Lycopodine, a bioactive compound derived from Lycopodium clavatum spores, effectively inhibits the proliferation of HeLa cells through the induction of apoptosis. This process is mediated by caspase-3 activation. In refractory prostate cancer cells, Lycopodine triggers apoptosis by modulating 5-lipoxygenase and depolarizing the mitochondrial membrane potential, without altering p53 activity.

Terameprocol (EM-1421) is a synthetic tetra-methylated derivative of nordihydroguaiaretic acid (NDGA) and transcriptional inhibitor with potential antiviral, antiangiogenic, and antineoplastic activities. Terameprocol showed the strongest anti-HIV activity.

ML351 is a potent and selective inhibitor of human 15-lipoxygenase-1 (15 LOX)(IC50: 200 nM).

Balsalazide (Balsalazido) is an anti-inflammatory compound used in the treatment of Inflammatory Bowel Disease.

Indirubin-3'-monoxime (Indirubin-3'-oxime) is a potent inhibitor of GSK3β (IC50: 22 nM) and also inhibits CDKs ( (IC50s: 100/180/250 nM for Cdk5/p35, Cdk1/cyclin B, Cdk2/cyclin E).

5-O-Demethylnobiletin (5-DEMETHYLNOBILETIN) is a natual product, has anti-inflammatory activity, it may act through a direct inhibition of 5-LOX, without affecting the expression of COX-2.

S-(+)-Marmesin (marmesin) is a coumarin originally isolated from the mature bark of A. marmelos,exhibiting COX-2/5-LOX dual inhibitory activity.