5(6)-dihete

Eicosapentaenoic acid is an ω-3 polyunsaturated fatty acid that is abundant in marine organisms and fish oils. EPA is metabolized, in part, through cytochrome P450-catalyzed epoxidation followed by conversion to the vicinal diols by epoxide hydrolases. (±)5(6)-DiHETE is a possible metabolite produced from EPA following epoxidation of the α-5 double bond. The biological activity of (±)5(6)-DiHETE has not been documented.

Eicosapentaenoic acid is metabolized, in part, through cytochrome P450-catalyzed epoxidation followed by conversion to the vicinal diols by epoxide hydrolases. (±)5(6)-DiHETE is a possible metabolite produced from EPA following epoxidation of the α-5 double bond. (±)5(6)-DiHETE lactone is a 1,5 cyclic ester derived from (±)5(6)-DiHETE. While its biological activity is unknown, the selective capacity of (±)5(6)-DiHETE to form this lactone can be utilized to specifically quantify (±)5(6)-DiHETE in biological samples.

5(S),6(R)-DiHETE is a dihydroxy polyunsaturated fatty acid and a nonenzymatic hydrolysis product of leukotriene A4 (LTA4). Mouse liver cytosolic epoxide hydrolase catalyzes the conversion of LTA4 to 5(S),6(R)-DiHETE. It is a weak LTD4 receptor agonist in guinea pig lung membranes. It induces guinea pig ileum contraction with an ED50 value of 1.3 μM.

5(S),6(R)-11-trans DiHETE is a C-11 double bond isomer of 5(S),6(R)-DiHETE that is formed by the enzymatic isomerization of 5(S),6(R)-DiHETE by a membrane bound factor. 5(S),6(R)-11-trans DiHETE has been found in rat kidney homogenates and is potentially formed by the epoxide hydrolase pathway in this tissue. The isomerase activity responsible for the conversion of leukotriene B4 (LTB4) to 6-trans LTB4 in rat kidney homogenates has also been implicated in its formation. 5(S),6(R)-11-trans DiHETE is not a substrate for soybean lipoxygenase. The biological activity of 5(S),6(R)-11-trans DiHETE has not been reported.

5(S),6(S)-DiHETE is one of the four diastereomeric 5,6-dihydroxy acids produced from the non-enzymatic hydrolysis of LTA4. 5(S),6(S)-DiHETE does not have significant leukotriene-like activity.

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6 15 2 3 3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

Marimastat (BB2516) (BB-2516) is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor. MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM)and MMP-7 (IC50=13 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.

Phorbol 12-myristate 13-acetate (PMA), a member of the phorbol ester group of natural products, activates PKC, SphK, and NF-κB, and induces THP1 cell differentiation.

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

Capsaicin ((E)-Capsaicin) is a natural product extracted from Capsicum annuum, and is a TRPV1 agonist (EC50=0.29 μM). Capsaicin has antitumor, anti-inflammatory, antioxidant and neuroprotective activities.

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

Acetylcysteine (NAC) is an N-acetyl derivative of cysteine, a ROS inhibitor and mucolytic agent. Acetylcysteine induces apoptosis, can be used to reduce mucus thickness, and has anti-influenza viral activity.

Corticosterone (Kendall's compound B) is an adrenocortical steroid with salocorticoid and glucocorticoid activity that is orally active. Corticosterone is involved in the regulation of energy, immune responses, and stress responses in the body.

Balsalazide sodium hydrate (Balsalazide disodium) is an anti-inflammatory compound used in the treatment of Inflammatory Bowel Disease.Balsalazide sodium hydrate is a new 5-aminosalicylic acid (5-ASA) containing prodrug. High dose Balsalazide sodium hydrate(3.0 g twice daily) was superior in maintaining remission in patients with ulcerative colitis compared with a low dose (1.5 g twice daily) or a standard dose of mesalazine (0.5 g three times daily). All three treatments were safe and well tolerated [1]. Balsalazide sodium hydrate is approved for the treatment of mild-to-moderate active UC. It is efficacious for the induction of remission in mild to moderate UC and has a favorable safety profile, with the added advantages of greater efficacy of remission induction and rapidity of onset [2].

Gardenin A shows neurotrophic effects via activating MAPK ERK, PKC, and PKA. Gardenin A exhibits antidepressant, anticonvulsant and anxiolytic effects.

Prostaglandin E2 (PGE2) is a naturally occurring hormone involved in various physiological processes, such as smooth muscle contraction and relaxation, vasodilation and constriction, blood pressure regulation, and inflammatory regulation.

In the CNS, Kainic acid is an effective agonist at excitatory amino acid receptor subtypes.

6-Diazo-5-oxo-L-nor-Leucine (L-6-Diazo-5-oxonorleucine) is a glutaminase antagonist (Ki: 6 μM) and an antineoplastic antibiotic produced by an unidentified Streptomyces species from Peruvian soil.

LDN193189 (LDN-193189) (DM 3189) is a selective BMP signaling inhibitor, inhibiting the transcriptional activity of ALK2 and ALK3 (IC50s: 0.8 0.8 5.3 16.7 nM for ALK1 2 3 6).

5-A-RU hydrochloride (5-Amino-6-(D-ribitylamino)uracil hydrochloride) is an intermediate of bacterial riboflavin that activates mucosal-associated invariant T cells (MAIT).5-A-RU is used in the study of breast and prostate cancer.

Salvianolic acid A (Dan Phenolic Acid A) is a natural product and an inhibitor of matrix metalloproteinase 9 (MMP-9). Salvianolic acid A has antioxidant and anti-inflammatory activity and protects the blood-brain barrier.

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.

ACY-957 (HDAC Inhibitor C001) is an orally active and selective inhibitor of HDAC1 and HDAC2 (IC50s: 7 nM, 18 nM, and 1300 nM against HDAC1 2 3) and shows no inhibition on HDAC4 5 6 7 8 9.