An intermediate in the generation of adenine and methionine that is produced by the decarboxylation of SAM; a potent agonist of adenosine receptors (Kis = 0.15, 1.13, 13.9, and 0.68 μM for A1, A2A, A2B, and A3, respectively); inhibits several enzymes at higher concentrations.

Selectively and reversibly blocks MAGL activity (IC₅₀s = 0.18 and 59 µM for MAGL and FAAH in mouse brain, respectively); does not inhibit ABHD6, ABHD12, CB1, or CB2 receptors (Kis > 10 µM); used to ameliorate disease progression in a mouse model of multiple sclerosis.

A benzothiazinone compound that selectively inhibits both MAO-B activity (IC₅₀ = 34.9 nM in human) and adenosine A2A receptors (Ki = 39.5 nM in human); designed as a potential dopamine-sparing therapeutic in the treatment of Parkinson’s disease.

A metabolite of dimetridazole, the nitroimidazole-based antibacterial and anticoccidial agent suspected to be carcinogenic and mutagenic to humans.

A selective and irreversible inhibitor of the gastric H+/K+ ATPase pump (IC₅₀ = 1.1 μM).

A quinone derivative that inhibits red blood cell PLA2 with a Ki value of 130 µM.

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 potent TRPV1 antagonist that inhibits capsaicin-induced and acid-induced activation of rat TRPV1 with IC50 values of 35 and 6 nM, respectively.

A water-soluble, slow-releasing H2S donor which demonstrates vasodilator and anti-hypertensive activity in hypertensive rats when given intravenously; also protects against endotoxic shock in rats, inhibiting pro-inflammatory signaling.

An imidazobenzodiazepine derivative that competitively inhibits benzodiazepine binding to GABAA receptors (IC₅₀ = 2 nM); used to reverse sedation induced by benzodiazepine drugs and is effective in the treatment of benzodiazepine overdose or withdrawal.

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

An estrogen metabolite that acts as a substrate of MRP2 (Km = 75 µM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow.

A quinone which inhibits topoisomerase I at 25 μM and transglutaminase (IC₅₀ = 5 μM); reduced to β-lapachone hydroquinone by NQO1, generating ROS during its reversion to β-lapachone; sensitizes cancer cells to radiation, suppresses NF-κB activation, and drives apoptosis.

A natural triterpenoid carboxylic acid that is known to have antioxidative, antimicrobial, anti-inflammatory, and anticancer activities; inhibits Na+/K+-ATPase activity (IC50 = 24.7 μM) and blocks NF-κB activation in various human cancer cells lines (10-100 μM), inhibiting cell…

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…

An orally available, selective inhibitor of both free and prothrombinase-bound factor Xa (Ki = 0.8 nM); effective anticoagulant in both preclinical and clinical models of venous and arterial thrombosis.

An anti-inflammatory compound from the diaryl heterocycle class that selectively inhibits COX-2 (IC50s = 22.9 and 0.05 μM for COX-1 and COX-2, respectively; displays chemopreventive activity in multiple tumor types via proapoptotic effects independent of its capacity to block COX-2.

A non-ionic, water-soluble X-ray contrast agent for intravascular administration; can cause acute kidney injury and is used in animal models of contrast-induced nephropathy.

Mn(III)TBAP is a cell-permeable SOD mimic. At a concentration of 30 µM, it decreases the doubling time of SOD-null E. coli. by 2-fold.

A metabolite of epinephrine produced by the action of catechol-O-methyl transferase on epinephrine; detection is used in the clinical diagnosis of pheochromocytoma.

A long-acting muscarinic receptor antagonist that binds equally to human muscarinic M1, M2, and M3 receptors (Kds = 0.04, 0.02, and 0.01 nM, respectively); dissociates slowly from M1 and M3 receptors, which are located on bronchial smooth muscle and submucosal glands, and more rapidly from M2…

Furegrelate is a potent inhibitor of thromboxane synthase with little effect on other enzymes essential for arachidonate metabolism. The IC₅₀ value is 15 nM for human platelet microsomal thromboxane synthase.

A stable, cell-permeable dye employed to assay cell proliferation as it is partitioned with high fidelity between daughter cells for up to eight generational divisions.

An analog of 2-OG that has been developed as an inhibitor of HIF-PHs.

Spermine NONOate is a NO donor. It spontaneously dissociates in a pH-dependent, first-order process with a half-life of 39 minutes and 230 minutes at 37°C and 22-25°C, respectively, (pH 7.4) to liberate 2 moles of NO per mole of parent compound.

An orally active small molecule drug with antioxidant, anti-inflammatory, and anti-fibrotic effects; reduces inflammatory cytokine production, suppresses TGF-β expression, and lowers markers of oxidative stress; has effectiveness in IPF and other conditions with a significant fibrotic component.

An inhibitor of DPP-4 (IC₅₀ = 3.5-34 nM); also inhibits DPP-8 and DPP-9 (Ki = 810 and 95 nM, respectively) but not DPP-2 or FAPα; blocks the degradation of several circulating peptides, including incretins; reduces fasting and postprandial glucose levels and decreases inflammatory…

The major metabolite formed during the metabolism of the non-steroidal antiandrogen flutamide by cytochrome P450 isoforms CYP1A2 and CYP3A4; inhibits the binding of testosterone to the nuclear androgen receptor (IC₅₀ = ~300-900), blocking the expression of AR target genes.

A selective cholesterol transport inhibitor that targets the NPC1L1 (KDs = 12,000, 540, 40, and 220 nM for its glucuronide in mouse, rat, rhesus monkey, and human, respectively); blocks intestinal cholesterol absorption in various animal models (IC₅₀s = 0.0005-0.05 mg/kg).

A naturally occuring terpenoid that potently inhibits MAGL (IC₅₀ = 93 nM); at 1 µM, significantly inhibits endogenous MAGL in isolated rat neurons.

An orally bioavailable, selective inhibitor of EZH2 (Ki = 2.5 nM); blocks H3K27 trimethylation in both wild-type and mutant lymphoma cells (IC₅₀s range from 2-90 nM); induces apoptosis and differentiation specifically in SMARCB1-deleted malignant rhabdoid tumor cells and promotes their…

An active, estrogenic metabolite of daidzein; has vasodilatory action on rat isolated aortic rings at 1 µg/ml; stimulates the estrogen receptor-dependent growth of breast cancer MCF-7 cells at micromolar concentrations.