12-hete

12-HETE ((±)12-HETE) is a modulator of PGE2, with both anti-thrombotic and pro-thrombotic effects, inducing PGE2 release and COX-2 expression via phospholipase A2 (sPLA2-IIA) inducers. It is also a neuroregulator activating retinal cell endothelial dysfunction in diabetic retinopathy.

12(S)-HETE, a 12-lipoxygenase metabolite of arachidonic acid, is mitogenic for cancer cell proliferation and enhances angiotensin II-induced contraction of BLT2 (type 2 receptor in arteries of leukotriene B4 mice) and TP (thromboxane receptor)-mediated mechanisms. 12(S)-HETE promotes superoxide and isothromboxane-like metabolites in arterial endothelial cells. production.

Biosynthesis of 12(R)-HETE in invertebrates is via lipoxygenation of arachidonic acid . In mammals, 12(R)-HETE can be produced by 12(R)-LOs and also by CYP450 oxidation. The activity of 12(R)-HETE in mammals is predominantly proinflammatory. 12(R)-HETE exhibits dose-dependent leukocyte chemotaxis at concentrations as low as 100 nM, and lowers intraocular pressure in rabbits.

12(S)-HETE is a product of arachidonic acid metabolism through the 12-lipoxygenase pathway. It is primarily found in platelets, leukocytes, and to a lesser extent in smooth muscle cells. It enhances tumor cell adhesion to endothelial cells, fibronectin, and the subendothelial matrix. tetranor-12(S)-HETE is the major β-oxidation product resulting from peroxisomal metabolism of 12(S)-HETE in numerous tissues, and Lewis lung carcinoma cells. No biological function has yet been determined for tetranor-12(S)-HETE. Some data indicate it may play a role in controlling the inflammatory response in injured corneas. In some diseases (e.g., Zellweger's Syndrome) peroxisomal abnormalities result in the inability of cells to metabolize 12(S)-HETE, which may be responsible for symptoms of the disease. The tetranor derivative of 12(S)-HETE is available as a research tool for the elucidation of the metabolic fate of its parent compound.

Metabolism of 12(R)-HETE in corneal tissue produces predominantly the compound resulting from the loss of four carbon atoms through β-oxidation from C-1. This metabolite is 8(R)-hydroxy hexadecatrienoic acid (8(R)-HHxTrE) or 2,3,4,5-tetranor 12(R)-HETE.

Gemcitabine (LY188011) is a synthetic cytosine nucleoside derivative and an inhibitor of DNA synthesis. Gemcitabine has antitumor and antimetabolic activities. Gemcitabine induces autophagy and apoptosis.

5-Fluorouracil (5-FU) is a uracil analog and inhibitor of DNA synthesis, exhibiting antitumor activity by affecting pyrimidine synthesis through thymidylate synthase inhibition; it induces apoptosis and autophagy.

Q-VD-OPH (Quinoline-Val-Asp-Difluorophenoxymethylketone) is a pan-caspase inhibitor with potent antiapoptotic properties.

Rutin (Quercetin 3-O-rutinoside), a flavonoid, has a variety of biological activities including antiallergic, anti-inflammatory, antiproliferative, and anticarcinogenic properties.

Dupilumab (REGN-668) is a fully human monoclonal antibody targeting the alpha subunit of the interleukin-4 receptor, thereby inhibiting IL-4 and IL-13 signaling. As a systemic immunomodulator, it has demonstrated efficacy in improving atopic dermatitis.

Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable, allosteric TYK2 inhibitor for the treatment of autoimmune diseases. It blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain, inhibiting IL-12 23 and type I IFN pathways. It selectively binds to the TYK2 pseudokinase (JH2) domain with an IC50 of 1.0 nM.

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.

TVB-3664 is an orally active, selective, reversible, and highly bioavailable fatty acid synthase inhibitor (FASN) with an IC50 for palmitate synthesis of 18 nM in human and 12 nM in mouse.Significantly inhibits microtubule protein palmitoylation and mRNA expression.

3-Methyladenine (3-MA) is a PI3K inhibitor that selectively inhibits class IB PI3Kγ (IC50 = 60 μM) and class III VPS34 (IC50 = 25 μM). 3-Methyladenine inhibits autophagy.

MK-2206 dihydrochloride (MK-2206 2HCl) is a variant Akt inhibitor that inhibits Akt1, Akt2, and Akt3 (IC50=8 12 65 nM) with orally active, highly potent and selective potency. MK-2206 dihydrochloride exhibits antitumor activity.

Tauroursodeoxycholate (UR 906), also known as ursodoxicoltaurine, is a highly hydrophilic tertiary bile acid that is produced in humans at a low concentration. Tauroursodeoxycholate is the more hydrophilic form of ursodeoxycholic acid, which is the more abundant naturally produced bile acid in humans.Tauroursodeoxycholate is being investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis.

Palmatine chloride an isoquinoline alkaloid, is an important medicinal herbal extract with diverse pharmacological and biological properties.

Ilomastat (GM6001) (GM6001, Galardin) is a broad spectrum matrix metalloprotease (MMP) inhibitor.

Astragaloside IV (AS-IV), an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1 2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells. Astragaloside IV is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine.1 It dose-dependently inhibits human adenovirus type 3 (HAdV-3) in A549 cells (IC50 = 23 μM; LC50 = 865 μM).It inhibits replication of HAdV-3 and decreases HAdV-3-induced apoptosis. It has diverse protective effects for the cardiovascular, immune, digestive, and nervous systems. In particular, it reduces myocardial infarct size in dogs when administered prior to coronary ligation and reduces reperfusion arrhythmias in isolated rat hearts.

A 83-01 (ALK5 Inhibitor IV) is an inhibitor of the TGF-β type I receptors ALK5, ALK4, and ALK7 (IC50=12 45 7.5 nM). A 83-01 promotes the reprogramming of mouse fibroblasts into iPSCs. A 83-01 can be used in organoid cultures.

Citronellol ((±)-β-Citronellol) is used in insect repellents and perfumes and as a mite attractant.

Resiniferatoxin ((+)-Resiniferatoxin) is a highly potent synthetic TRPV1 agonist that inhibits the production of Th1 cytokines and has anti-inflammatory activity, reducing serum levels of IL-12, INF-γ, IL-1β, TNF-α, NO, and PGE.

Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1) with potential antineoplastic activity. It specifically inhibits a mutated form of IDH1 in the cytoplasm, preventing the formation of the oncometabolite 2-hydroxyglutarate (2 hG), which may induce cellular differentiation and inhibit cellular proliferation in IDH1-expressing tumor cells.

C12-200 is a benchmark ionizable cationic lipidoid along with helper lipids and can be used in the delivery of mRNA.