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, 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.

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.

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 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…

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.

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…

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…

An ATP/GTP-competitive inhibitor of CK2 (IC₅₀ = 900 µM for rat liver CK2); less potently inhibits CCK2/cyclin A, GSK3β, and phosphorylase kinase (IC₅₀ = 15.6, 11.2, and 8.7 mM, respectively); much less effective against a range of other kinases.

A cell permeable drug that inhibits cholesterol trafficking from late endosomes/lysosomes to the ER, but not to the plasma membrane.

N-Oleoyl glycine is a putative substrate for peptidyl glycine α-amidating enzyme in the biosynthesis of oleoyl amide.

An inhibitor of PAD4 deimination activity (IC50 = 5.9 μM) that also inhibits PAD1 and PAD3 (IC50 = 0.8 and 6.2 μM, respectively); dose dependently decreases the citrulline content in serum and joints and reduces the development of IgG autoantibodies in a CIA mouse model of inflammatory arthritis.

3-Tert-butyl-4-hydroxyanisole (3-BHA) is one component of butylated hydroxyanisole (BHA). This compound is commonly used as a food additive; it exhibits antioxidative and anticancer activities. In leukemia cells, 3-BHA decreases the mitochondrial membrane potential, inhibits mitochondrial oxidative…

A symmetric bis-glycolamide that inhibits the eIF2α phosphorylation-mediated unfolded protein response (IC₅₀ = 5 nM in a cell-reporter assay); passes through the blood-brain barrier and significantly enhances learning and memory in mice and rats.

A nonaminoglycoside that has been reported to selectively induce ribosomes to read through premature nonsense stop signals on mRNA, thus allowing the production of full-length, functional proteins (IC₅₀ = 7 nM); 60 mg/kg s.c. injection or 0.3-0.9 mg/ml orally has been shown to restore…

An elongation product of γ-linolenic acid (18:3), rapidly metabolized by fatty acid desaturases to produce arachidonic acid (20:4); metabolized through the cyclooxygenase pathway to produce 1-series prostaglandins; can reduce atopic dermatitis and atherosclerosis when added to the diet of mice.

GSK3β Inhibitor II is a potent inhibitor of glycogen synthase kinase-3β (GSK3β; IC₅₀ = 390 nM) that does not inhibit GSK-3α. Also referred to as tip-oxadiazole, this compound blocks the functional regulation of p53 by GSK3β, decreasing levels of MDM2, p21, and…

A selective inhibitor of PAD4 (IC₅₀ = 200 nM in the absence of calicum); inhibits the citrullination of PAD4 target proteins and diminishes NET formation in mouse neutrophils.

A γ-secretase inhibitor that blocks Notch processing (IC₅₀ = 1.7 nM); reduces Aβ40 levels by 71% in an APP transgenic mouse model within 4 hours after a single 100 μM/kg dose.