CWHM12 is an analog of RGD peptide (Item No. 14501), a tripeptide that inhibits integrin-ligand interactions in studies related to cell adhesion, migration, growth, and differentiation. CWHM12 selectively inhibits αv integrins (IC₅₀s = 1.8, 0.8, 61, 1.5, and 0.2 nM for…

A naturally-occurring lipid which is produced by the enzymatic removal of the acylated group of sphingomyelin; serves as a substrate for autotaxin to produce sphingosine-1-phosphate; occurs naturally in plasma, is a constituent of lipoproteins, and is increased in some diseases.

A small diffusible signaling molecule involved in quorum sensing in the model symbiont V. fischeri and the pathogens A. tumefaciens and P. aeruginosa.

A purine derivative that reversibly antagonizes aryl hydrocarbon receptor signaling (IC₅₀ = 127 nM in CD34+ cells); induces a 50-fold increase in human embryonic stem cells expressing CD34 (EC₅₀ = 120 nM) and a 17-fold increase in stem cells that retain the ability to engraft…

A selective, reversible inhibitor of vacuolar H+-ATPases (V-ATPases), blocking these proton pumps in mammalian, plant, or fungal cells with an IC50 value in the 4-400 nM range; also inhibits autophagy by preventing vacuolar acidification necessary for autophagosome maturation.

An analog of MAFP, which has been widely studied as an inhibitor of phospholipases, FAAH, and as a CB receptor ligand; pharmacology of the γ-linolenyl analog of MAFP has not been completely investigated.

A Pim kinase inhibitor that blocks mTORC1 activity via activation of AMPK, killing a wide range of both myeloid and lymphoid cell lines (with IC50 values ranging from 0.8 to 40 μM); induces G1 phase cell-cycle arrest, dose-dependent induction of p27Kip1, apoptosis through the mitochondrial…

A hybrid molecule of indomethacin and an NO donor which combines the anti-inflammatory properties of an NSAID with the gastrointestinal protective effects of NO.

A DHA epoxygenase metabolite found in rat brain and spinal cord that acts as a preferred substrate for sEH (Km = 3.2 µM); demonstrates antihyperalgesic activity in inflammatory and neuropathic pain models and potently inhibits angiogenesis and tumor growth in in vitro assays.

A crosslinking reagent that contains NHS ester- and maleimide-reactive groups at the opposite ends of a 4.4 Å spacer arm; used for sequential, two-stage conjugation with amine and sulfhydryl functional groups in the preparation of protein-hapten or protein-protein conjugates.

A selective and competitive inhibitor of NAD+-dependent type-I 15-PGDH (IC₅₀ = 26.4 nM; Ki = 5 nM).

8-iso-17-phenyl PGF2β is an isomer of bimatoprost (free acid) that is epimerized at the 8 and 9 positions. There are no published reports on the biological activity of 8-iso-17-phenyl PGF2β.

A reversible and competitive inhibitor of type IV collagen-specific MMP-2 and MMP-9 with preference towards MMP-2 (IC50 = 4 and 20 µM, respectively).

Key urinary metabolite of PGD2; represents approximately 1% and 4% of the infused radiolabeled dose in monkeys and humans, respectively.

A cell-permeable, selective inhibitor of calcineurin-mediated dephosphorylation of NFAT that does not disrupt other calcineurin-dependent pathways; disrupts NFAT-dependent expression of IL-2 and TNF-α when transfected in Jurak T cells and prevents the activation and proliferation of T cells…

A mycotoxin produced by a variety of molds, including Aspergillus and Penicillium, commonly found in rotting apples; demonstrates an oral LD50 between 29 and 55 mg/kg body weight in rodents and 170 mg/kg body weight in poultry and has been shown to induce nephropathy and gastrointestinal tract…

A natural oxidative metabolic of the mycotoxin aflatoxin B1; produced from aflatoxin B1 in mammals and then secreted in milk.

PGF2α 1,11-lactone is a lipid-soluble internal ester of PGF2α. Hydrolysis of the lactone by plasma esterases readily produces free PGF2α in rats and monkeys, but not in humans. PGF2α 1,11-lactone is active as an antifertility agent with greatly reduced vasoactivity compared…

16,16-dimethyl PGF2β is a metabolically stable analog of PGF2β. It prevents bronchospasm in asthmatics but is less potent than PGE2.

An orally active broad spectrum antifungal agent that blocks ergosterol biosynthesis by inhibiting the fungal CYP isoform CYP51; potently inhibits the mammalian analog CYP51A1 (IC₅₀ = 63.5 nM), as well as a variety of other CYP isoforms.

A potent blocker of small conductance Ca2+-activated K+ (SK, KCa2) channels that is more effective at SK2 than SK1 and SK3 (IC₅₀ values are 0.06-0.4, 1-12, and 1-13 nM, respectively); ineffective against SK4 at 1 µM.

A high-affinity fluorescent calcium indicator (Kd = 115 nM for calcium) that is ideal for monitoring low levels of calcium, as are found in resting cells; may be used to buffer intracellular calcium transients.

A trypsin-like protease inhibitor known to inhibit trypsin and various inflammatory proteases including plasmin, kallikrein, and thrombin; used in the treatment of chronic pancreatitis and various manifestations of fibrosis.

A polysulfonated naphthylurea that inhibits the binding of calmodulin to recognition sites on the ryanodine receptor-1 (IC50 = 4.9 μM), blocks G protein coupling to GPCRs, and non-selectively antagonizes P2 purinergic receptors (10-100 μM); acts as a non-specific competitor of…

Biosynthesis of LTA3 occurs from 5,8,11-eicosatrienoic acid via the 5-LO pathway{689} and it is the putative intermediate in the biosynthesis of 3-series leukotrienes. LTA3 as a free acid is highly unstable. The methyl ester is stable and can be readily hydrolyzed to the free acid as needed.

A specific Akt inhibitor that has been shown to inhibit proliferation and to induce apoptosis of thyroid cancer cells (IC₅₀ = 30-60 nM in vitro); inhibits Akt, PDK1, and FLT3 in acute myelogenous leukemia cells, decreasing the colony-forming ability of these cells (IC₅₀…

A selective inhibitor of Δ6 desaturase (IC50 = 0.2 µM in a rat liver microsomal assay) that completely blocks the conversion of linoleic acid to AA; orally active in vivo, decreasing edema in the carrageenan paw edema model in mice.

A homolog of DHEA, characterized by the addition of an (R)-β-methyl group at the terminal ethanolamine carbon.

A classical inhibitor of complex I of the mitochondrial electron transport chain, inhibiting NADH/DB oxidoreductase and NADH oxidase with IC₅₀ values of 28.8 and 5.1 nM, respectively; used in animal models of Parkinson’s disease.

Misoprostol is a widely sold analog of PGE1 which has potent but relatively non-selective agonist activity with respect to the prostanoid EP receptor subgroup. Misoprostol has been used therapeutically for many years in humans for the treatment of gastric ulcer disease under the Searle tradename…

A cell permeable, competitive inhibitor of HIF-PH with effective concentrations in the low µM range.

A redox indicator used to detect cellular respiration; primarily reduced by Complex I in mitochondria and, under anaerobic conditions, is completely reduced to an insoluble red 1,3,5-triphenylformazan.