lox-2

Compound 10 (h15-LOX-2 inhibitor 2) suppresses h15-LOX activity, exhibiting IC 50 and K i values of 26.9 μM and 16.4 μM, respectively.

Compound 13, identified as h15-LOX-2 inhibitor 3, exhibits inhibitory activity against h15-LOX, with IC50 and Ki values of 25 μM and 15.1 μM, respectively.

Compound 105 (h15-LOX-2 inhibitor 1) is a potent inhibitor of human epithelial 15-lipoxygenase-2 (h15-LOX-2), exhibiting an IC50 of 0.34 μM [1].

ABT-963 is a potent and selective inhibitor of disubstituted pyridazinone cyclooxygenase-2 (LOX2) that dose-dependently reduces injury perception in a carrageenan model of nociceptive sensitization.ABT-963 is used in the study of arthritis.

Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.

S-2474, an inhibitor of COX-2 and 5-lipoxygenase, has anti-inflammatory and neuroprotective activities and inhibits Abeta (25 - 35) and Abeta (1 - 40) induced cell death.

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

6-Hydroxyflavanone, extracted from the leaves of Acorus calamus, exhibits anti-inflammatory and anti-neuropathic pain activity by targeting cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), as well as opioid and GABA-A receptors. 6-Hydroxyflavanone has anti-injury sensory properties in a streptozotocin-induced diabetic neuropathy model. in a streptozotocin-induced diabetic neuropathy model with anti-injury sensory properties.

5-amino-1-[4-(trifluoromethyl)phenyl]-1H-pyrazole-4-carbonitrile is a compound used as a molecular structural unit and is considered to be an inhibitor of enzymes such as COX-2, 5-LOX, etc., and possesses a wide range of biochemical and physiological effects including antitumor activity, anti-inflammatory effects and antioxidant activity.

5-LOx-in-2 is a 5-lipoxygenase inhibitor (5-LOX) with an IC50 value of 0.33 μM. 5-lox-in-2 inhibits 5-LOX action IN a dose-dependent manner. 5-LOX-IN-2 can reduce the cell activity of kidney cancer cells and induce apoptosis, and can be used in cancer research.

12R-LOX-IN-2 is an inhibitor of 12R-lipoxygenase (12R-LOX).12R-LOX-IN-2 inhibits imiquimod (IMQ)-induced hyperproliferation of psoriatic keratinocytes and inhibits colony formation.12R-LOX-IN-2 also decreases the protein level of Ki67 and the mRNA expression of IL-17A in IMQ-induced cells. 12R-LOX-IN-2 may be useful in the study of psoriasis and other skin-associated inflammatory diseases.

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).

CAY10698 is a 12-lipoxygenase inhibitor (12-LO; IC50 of 5.1 µM).

COX/5-LO-IN-1 is a cyclooxygenase and 5-lipoxygenase (5-LO) inhibitor, and used for inflammatory and allergic disease states.

HPGDS inhibitor 1 is a novel and selective inhibitor for Hematopoietic Prostaglandin D Synthase (HPGDS) with an IC50 Value of 0.7 nM.

L-Homocysteine is a biological thiol involved in various diseases and pathological conditions. It is a marker for atherosclerosis and can exacerbate intestinal inflammation in inflammatory bowel disease (IBD) by promoting the expression of 5-LOX and COX-2, making it suitable for inducing vascular endothelial inflammation models.

TBHBA (2,4,6-Tribromo-3-hydroxybenzoic acid) is a brominated aromatic compound that inhibits the enzymes cyclooxygenase-2 (COX-2), lipoxygenase (LOX), 5-lipoxygenase (5-LOX), 5-alpha reductase, and tyrosinase, and exhibits a variety of anti-inflammatory and antioxidant effects.

PXS-4787 hydrochloride is a specific and potent pan-lysyl oxidase inhibitor that effectively eliminates the activity of lysyl oxidase. It exhibits varying IC50 values against different forms of the enzyme, including 2 μM (Bovine LOX), 3.2 μM (rh LOXL1), 0.6 μM (rh LOXL2), 1.4 μM (rh LOXL3), and 0.2 μM (rh LOXL4). In addition, PXS-4787 hydrochloride reduces the deposition and cross-linking of collagen I secreted by human fibroblasts.

COX-2/15-LOX-IN-6 (Compound 5l) is a dual inhibitor of COX-2 and 15-LOX with IC50 values of 0.201 μM and 11.723 μM, respectively. In serum, it suppresses the expression of PGE, TNF-α, IL-6, and iNOS, and demonstrates anti-inflammatory activity in a carrageenan-induced rat edema model.

LOX-IN-5 tosylate (compound 22) is a selective oral inhibitor of lysyl oxidase-like 2 (LOXL2) with an IC50 of less than 300 nM, and it exhibits anti-fibrotic properties.

AChE-IN-82 (compound 49) is an acetylcholinesterase (AChE) inhibitor. It inhibits eeAChE, eqBChE, hMAO-A, hMAO-B, and BACE-1 with IC50 values of 0.072, 9.81, 14.52, 0.024, and 2.42 μM, respectively. Additionally, AChE-IN-82 inhibits COX-1, COX-2, and 5-LOX with IC50 values of 60.41, 0.187, and 0.18 μM, respectively. The compound also demonstrates strong neuroprotective effects by significantly reducing H2O2-induced oxidative stress.

15-LOX-IN-2 (Compound 2a) is an orally active inhibitor of COX-2/15-LOX and a partial agonist of PPARγ. It exhibits anti-inflammatory activity by inhibiting levels of 20-HETE, IL-1β, and TNF-α in LPS-treated RAW 264.7 cells. Additionally, it significantly enhances glucose uptake without the presence of insulin and is applicable in metabolic disease research.

15-LOX-1 inhibitor 2 (Compound 5i) is a potent inhibitor of 15-lipoxygenase-1 (15-LOX-1), with an IC50 of 1.7 μM. By inhibiting the activity of the 15-LOX-1 enzyme, it reduces the production of lipid peroxides, thereby preventing lipid peroxidation and protecting cells from RSL3-induced cell death. This compound is valuable for research into cell death mechanisms and oxidative stress-related conditions.

Cbz-(S,S)-Pro-Pro-allyl (compound 1a) is a dual inhibitor of cyclooxygenase-2 and 5-lipoxygenase, with IC50 values of 0.146 nM, 0.003 nM, and 0.64 nM for COX-1, COX-2, and 5-LOX, respectively. Additionally, Cbz-(S,S)-Pro-Pro-allyl exhibits anti-inflammatory properties.