A selective antagonist of BET bromodomains, binding with 10-100-fold higher affinity for BD2 (IC₅₀ = 0.04-0.28 µM) over BD1 (IC₅₀ = 1.8-3.1 µM), which causes selective release of BET proteins from chromatin; increases the expression of ApoA1 and reduces…

A potent, selective inhibitor of PKG (in vitro IC50 = 234 nM); cell-permeable and often used in intact cells to assess the role of PKG in signaling.

Naturally occuring mycotoxin and food contaminant that induces the transversion of G to T at codon 249 of the p53 tumor suppressor gene and is a likely pathogen that causes hepatocellular carcinoma.

A potent, selective, and bioavailable inhibitor of the TRPA1 channel, with IC₅₀ values of 67 and 289 nM for the human and rat isoforms, respectively; attenuates cold allodynia following nerve injury and suppresses neuronal activity in response to mechanical stimulation.

An intermediate in the HMG-CoA reductase pathway derived directly from farnesyl pyrophosphate and used in the biosynthesis of terpenes and terpenoids; also serves as a substrate in the prenylation of a variety of critical intracellular proteins including small GTPases.

A fluoroquinolone antibiotic widely used as an antimicrobial and immunomodulatory agent; functions by inhibiting DNA A fluoroquinolone antibiotic widely used as an antimicrobial and immunomodulatory agent; functions by inhibiting DNA gyrase (a type II topoisomerase) and topoisomerase IV, the…

A nitroimidazole with radiosensitizing and antineoplastic properties; metabolites accumulate in hypoxic cells and can themselves be cytotoxic or they can increase the chemosensitivity and radiosensitivity of the target cells; used in the imaging of hypoxic regions in tumors and in the…

An ester of the free acid that is less water soluble, but more amenable for the formulation of stearidonate-containing diets and dietary supplements.

ALA is an essential fatty acid found in leafy green vegetables. ALA, as part of a low saturated fat diet, helps prevent cardiovascular disease. ALA decreases blood pressure, serum cholesterol levels, and platelet aggregation.

DepNA is one of several nitroaniline fatty acid amides which can be used to measure FAAH activity.{8928} FAAH is a relatively unselective enzyme in that it accepts a variety of amide head groups other than the ethanolamine of its endogenous substrate AEA. It also will hydrolyze fatty acid amides…

A potent, selective inhibitor of Stearoyl-CoA desaturase 1 that demonstrates IC50 values of 4.5 and 26 nM in mouse and human enzymatic assays, respectively.

An ATP-competitive, allosteric inhibitor of IRE1α RNase kinase activity (IC₅₀ = 0.6 µM); prevents IRE1α oligomerization and promotes cell survival under ER stress in rat models of retinal degeneration and diabetes.

N-4AIA is one of several aromatic amides of indomethacin reported to be potent and selective reversible inhibitors of COX-2. N-4AIA inhibits human recombinant and ovine COX-2 with IC₅₀ values of 0.1 and 0.625 µM, respectively. It is about 80 times less potent as an inhibitor of…

PGF1α is the putative metabolite of DGLA via the COX pathway. Both PGF1α and PGF2α have been shown to act as priming pheromones for male Atlantic salmon with a threshold concentration of 10−11 M. PGF1α binds to the ovine corpus luteum FP receptor at only 8% of the…

A potent inhibitor of all three human Pim kinases (IC₅₀s = 7, 363, and 69 nM for Pim-1, Pim-2, and Pim-3, respectively); induces apoptosis in lymphocytes from patients with CML or ALL; enhances the activity of sunitinib against renal cell carcinoma and resensitizes chemoresistant cancer…

A selective cell-permeable inhibitor of non-muscle myosin II ATPases, inhibiting Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB for several species (IC₅₀ = 0.5-5.0 μM), while poorly inhibiting smooth muscle myosin (IC₅₀ = 80 μM).

A selective allosteric inhibitor of Bcr-Abl (IC₅₀s = 4.52, 0.38, and 0.93 µM against Bcr-Abl mutants G250E, E255V, and M351T, respectively); displays additive inhibitory activity against T315I Bcr-Abl mutants both in in vitro assays and in a recalcitrant T315I Bcr-Abl mutant mouse…

A potent and selective farnesyltransferase (FTase) inhibitor with anti-tumor activity: inhibits rat brain FTase with a Ki value of 1.2 µM, thereby preventing Ras activation; inhibits IKK in an number of cells types.

A substrate of cathepsin C that accumulates inside lysosomes causing lysosome degradation; 50 μM can inhibit the cathepsin-dependent activation of caspase-8.

A potent α1A-adrenoceptor antagonist (Ki = 0.036 nM).

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.

A selective, nonpeptide antagonist of the vasopressin V1a receptor (Ki = 1.1-6.3 nM in human); inhibits arginine vasopressin-induced human platelet aggregation with an IC₅₀ value of 3.7 nM.

A natural and potent inhibitor of NEP and NEP2, with Ki values of 2 nM for both enzymes; also a weak inhibitor of the related zinc metalloprotease ECE (Ki = 3.5 µM); has little or no effect on a variety of other proteases.

An indole-based SERM that binds to both ERα (IC₅₀ = 26 nM) and ERβ (IC₅₀ = 99 nM); antagonizes 17β-estradiol-dependent and hormone-independent growth of breast cancer cell proliferation (80% reduction with 10 nM) in a manner related to cell cycle arrest and…

Microcystins are hepatotoxic cyclic heptapeptide toxins produced by cyanobacteria. They are responsible for periodic poisonings of humans and livestock drinking fresh water where the blue-green algae are endemic. Microcystin-LR is a selective inhibitor of protein phosphatase 2A (PP2A) (IC50= 0.04…

A cell-permeable inhibitor of sirtuin NAD+-dependent deacetylases, inhibiting the yeast sirtuin Sir2p with an IC50 value of 68 μM and the human sirtuins SIRT1 and SIRT2 with IC50 values of 131 and 38 μM, respectively; does not alter HDAC1 activity.

DAF-2 diacetate is a sensitive fluorescent indicator for the detection and bioimaging of NO. It is a cell-permeable derivative of DAF-2. Upon entry into the cell, DAF-2 diacetate is transformed into the less cell-permeable DAF-2 by cellular esterases thus preventing loss of signal due to diffusion…

A synthetic thyroid hormone mimetic that lowers total and LDL cholesterol up to 40% when administered to humans at a dose of 50-200 µg once daily for 14 days; stimulates cholesterol catabolism to bile acids without affecting cholesterol synthesis.

PPHP is a substrate for the measurement of peroxidase enzymes. PPHP has been used to quantitate the peroxidase activity of COX-1 and COX-2.

A selective inhibitor of the β5i (LMP7) subunit of the immunoproteasome (IC₅₀s = 65 and 73 nM for mouse and human, respectively) that demonstrates significantly weaker activity at the β5 subunit of the constitutive proteasome (IC₅₀s = 0.92 and 1.04 µM for mouse…

The dihydro derivative of Aflatoxin B1.

PGA2 is a naturally occurring prostaglandin in gorgonian corals where it may function in self defense. It is generally not present in mammals. PGA2 has low biological potency in most bioassays, but it does show some antiviral/antitumor activity. At a 25 µM concentration, PGA2 blocks the cell…