Hydroxy linoleins are a mixture of 132 possible isomers of mono-, di-, and tri-hydroxy compounds produced by the autoxidation of trilinolein and subsequent reduction of the hydroperoxides. Autoxidation of linoleic acid containing triglycerides (i.e., trilinolein) in vivo could result in the…

A tumor-promoting teleocidin compound that activates PKC (Ki = 3.4 nM and 1 μM for PKCη and PKCγ, respectively); induces differentiation of human embryonic stem cells into pancreatic progenitors.

Initiates glycogen synthesis in hepatocytes by causing inactivation of phosphorylase a and activation of glycogen synthase a (maximal effects with ~20 µM Itu); potent inhibitor of ERK2 (Ki = 525 nM).

A TZD that increases the sensitivity of cells to insulin, stimulating insulin-induced PI3K activity at submicromolar concentrations; increases insulin effectiveness in obese NIDDM subjects; promotes adipocyte differentiation by up-regulating the expression of UCP-2.

An alkaloid metabolite of nicotine as well as a major product of its pyrolysis; binds comparably to CYP2A6 and CYP2A13 (Kis = 7.5 and 5.6 µM, respectively), but appears to more effectively inactivate CYP2A6.

An analog of wortmannin; irreversibly binds PI3K; inhibits recombinant PI3K and mTOR (IC₅₀ = 2.7 and 193 nM, respectively) and prevents the growth of LNCap cells (IC₅₀ = 1.46 μM).

A dual inhibitor of DNA-PK and PI3K.

A synthetic progestin that acts as a prodrug to norelgestromin and levonorgestrel; selectively binds the progesterone receptor and is androgenically neutral.

Active metabolite of lactacystin, a widely used selective inhibitor of the 20S proteasome, with at least 10 times better activity; irreversibly alkylates subunit X of the 20S proteasome.

A selective inhibitor of PI3Kα that is equipotent against both wild type and several mutant isoforms (IC₅₀s = 4.0-4.8 nM); dose-dependently inhibits the growth of PI3Kα-dependent xenograft tumors in mice, alone or in combination with other kinase inhibitors.

A synthetic prodrug which is converted to the vitamin D receptor agonist 1,25-dihydroxy vitamin D3 in vivo; suppresses the synthesis and secretion of parathyroid hormone in secondary hyperparathyroidism; supports bone growth; provides renal and cardiovascular protection during chronic kidney disease.

An orally-available, highly selective inhibitor of B-RafV600E (IC₅₀ = 13 nM); less effective against wild type B-Raf (IC₅₀ = 160 nM) as well as several other kinases; induces cell cycle arrest and apoptosis in cells and xenografts expressing the mutant of B-Raf.

An inhibitor of class III receptor tyrosine kinases (IC₅₀s = 0.3 µM for c-Fms, c-Kit, ITD-FLT3 and 1 µM for PDGFRβ); blocks the proliferation of leukemia cells stimulated with FLT3 ligand by preventing the activation of STAT5.

A naturally-occurring macrocyclic lactone that is a potent insecticide; acts as an agonist of insect nicotinic acetylcholinesterase receptors (nAChRs), which differ both structurally and functionally from nAChRs in vertebrates.

6β-PGI1 is a stable PGI2 analog resistant to hydrolysis in aqueous solutions. 6β-PGI1 has a much longer half-life than PGI2, but a greatly reduced molar potency for receptor mediated function. 6β-PGI1 has a Kact for adenylate cyclase in NCB-20 cells of 4.2 µM compared with 18…

A fluorogenic substrate of palmitoyl-protein thioesterase.

An internal standard for the quantification of (±)-β-hydroxybutyrate (sodium salt) by GC- or LC-MS.

An internal standard for the quantification of 17β-estradiol by GC- or LC-MS.

11-deoxy PGF1β is a synthetic analog of PGF1β. In contrast to PGF2α and PGF1α, 11-deoxy PGF1β exhibits vasodepressor and bronchodilator activities in guinea pigs at a dose of 500 µg/kg.

Bicyclo PGE2 is a stable, base-catalyzed transformation product of 13,14-dihydro-15-keto PGE2. 13,14-dihydro-15-keto PGE2 itself is a metabolite of PGE2 found in human plasma at a median level of 20-25 pg/ml. Due to the inherent instability of 13,14-dihydro-15-keto PGE2, it is advisable to quantify…

A melatonin metabolite first identified in rat brain that has antioxidant and free radical scavenging activities in several experimental models; may be measured in plasma as an index of melatonin synthesis and metabolism.

Ro 3-1314 is an inhibitor of both COX and lipoxygenase. Ro 3-1314 inhibits ram seminal vesicle COX with a Ki of 0.6 µM. It is a more effective inhibitor of COX-1 than of 15-LO, inhibiting 95% and 68%, respectively, of these enzymatic activities when used at a concentration of 48 µM.

DAN-1 EE is a fluorescent indicator for the bioimaging of NO. DAN-1 EE is a cell permeable derivative of DAN, a molecule which has been used extensively in the quantitation of nitrate and nitrite using fluorescence spectroscopy. Upon entry into the cell, DAN-1 EE is transformed into the less cell…

An inhibitor of p53-HDM-2 interaction that can reactivate the tumor suppressor function of wild-type p53; binds to p53 with an apparent Kd value of 1.5 nM and prevents interaction with HDM-2 resulting in p53 stabilization, accumulation, and activation.

Molecular Formula: C₂₈H₂₄F₃N₇O₂

A selective inhibitor of the TGF-β type1 receptor ALK5 (IC₅₀s = 4, 18, and 23 nM for ALK5 autophosphorylation, TGF-β cellular assay, and ALK5 binding in HepG2 cells, respectively); used to induce stem cell pluripotency by replacing the reprogramming transcription factor Sox2…

β-Gal-NONOate is a nitric oxide (NO) donor which releases NO following activation by β-galactosidase. β-Gal-NONOate is stabile in aqueous solution at neutral and acidic pH for several hours, exhibits good water solubility, and is able to cross the cell membrane. Following enzymatic…

A potent, ATP-competitive inhibitor of ROCKs including p160ROCK (Ki = 140 nM) and ROCK-II (IC50 = 800 nM); also inhibits PRK2 with an IC50 value of 600 nM.

An antifungal antibiotic that selectively inhibits succinate dehydrogenase (complex II; IC50s = 12 and 3.7 nM in nematode and mammalian mitochondria, respectively, versus IC50s > 100 μM for inhibition of complex I and complex III enzymes); has cardioprotective effects against simulated…

11β-PGF2α-EA is the theoretical hepatic metabolite of PGD2-EA, produced during COX-2 metabolism of the endogenous cannabinoid AEA which is found in brain, liver, and other mammalian tissues. AEA can be used directly by COX-2 and specific PG synthase to produce ethanolamide congeners of…

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 thioester substrate analog of 2-AG that can be utilized for the measurement of MAGL activity; hydrolysis of the thioester bond by MAGL generates a free thiol that reacts rapidly with the chromogenic reagent DTNB resulting in a yellow product with an absorbance maximum at 412 nm.