EW-7197 is a potent inhibitor of activin receptor-like kinase 5 (ALK5, also known as TGF-β receptor type 1; IC₅₀ = 12.9 nM). It also inhibits ALK2 and ALK4 at nanomolar concentrations. EW-7197 blocks TGF-β/Smad signaling, cell migration, invasion, and lung metastasis in mouse…

A small molecule inhibitor of the TGF-β receptor type 1 kinase (IC₅₀ = 56 nM) that has been used to study the role of TGF-β signaling in triple negative breast cancer cells and hepatocellular carcinoma cells.

Piriprost is a structural analog of PGI2 with low IP receptor-mediated activity. Piriprost inhibits 5-LO with an IC₅₀ value around 100 µM, as measured by the release of 5-HETE from cultured myometrial cells. Piriprost inhibits the release of histamine and leukotrienes from isolated…

Butaprost is a structural analog of PGE2 with good selectivity for the EP2 receptor subtype. Butaprost has frequently been used to pharmacologically define the EP receptor expression profile of various human and animal tissues and cells. Serious confusion as to the structure of Butaprost was…

An ERα selective agonist with a 410-fold relative binding affinity for ERα versus ERβ.

Binds avidly and selectively to the structurally-similar bromodomains of SMARCA4 and PB1(domain 5) with Kd values of 89 and 48 nM, respectively; also interacts with the bromodomain of SMARCA2; does not interact with other bromodomains or with a panel of kinases.

A potent, non-ATP-competitive inhibitor of Plk1 (IC₅₀ = 9 nM); induces apoptosis in a wide array of tumor cell lines (GI50 = 50-200 nM); active in vivo when administered intraperitoneally and synergizes with chemotherapeutic agents.

A product of CYP2A6 metabolism of the primary nicotine metabolite, cotinine; as a biomarker of nicotine metabolism.

A potent, selective, and orally bioavailable inhibitor of PRMT5 (Ki = 5 nM); blocks the growth of mantle cell lymphoma Z-138 xenografts, without significant body weight loss, in mice.

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 potent inhibitor of tubulin polymerization with strong inhibitory activity on tumor cell growth.

A thiazolidinone that selectively blocks the CFTR channel (Ki = 300 nM) in a voltage-independent manner; prevents cholera toxin-induced fluid secretion in the small intestine, when given by intraperitoneal injection; can affect intracellular GSH concentration and ROS balance.

A naturally occurring phospholipid produced by cells upon inflammatory stimulation; less potent than PAF C-16 and PAF C-18 in the induction of neutrophil chemotaxis, but is equipotent to PAF C-16 and PAF C-18 in promoting eosinophil migration.

A natural benzoquinone which directly binds and inhibits XIAP (IC50 = 4.1 μM); blocks growth while activating caspases and promoting apoptosis in cancer cells expressing high levels of XIAP; prevents NF-κB activation by inhibiting IKK; protects against XIAP- and caspase-dependent inflammation.

A broad-spectrum antibiotic that inhibits protein synthesis by inducing miscoding; commonly used as a dominant selection antibiotic for genetically modified bacteria, yeasts, fungi, protozoa, plants, and mammalian cells.

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

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 small molecule that stimulates the expression of PGC-1α and downstream genes in skeletal muscle cells, improving glucose utilization and fatty acid oxidation at a concentration of 20 μM; 15 mg/kg/day administered to diabetic db/db mice improved glucose tolerance, pyruvate tolerance, and…

FR122047 is a selective inhibitor of COX-1. The IC50 values for inhibition of human COX-1 and COX-2 are 0.028 and 65 µM, respectively. In human platelet-rich plasma, FR122047 inhibits arachidonic acid, collagen, and ADP-induced platelet aggregation with an IC50 of 180-200 nM, which is nearly…

An inhibitor of PDKs, resulting in an increase in PDH activity (EC₅₀ = 5.2 nM for PDK2); less potently inhibits PDK1 and PDK3 (IC₅₀s = 87 and 600 nM, respectively).

An antibiotic which inhibits MetAp2 with an IC50 value of 10 nM; inhibits angiogenesis by impairing the growth of endothelial cells; impairs microsporidial replication and can be used to treat microsporidial infections in immunocompromised patients; reduces diet-induced adipose tissue formation in mice.

A macrolide that causes the formation of bundles of intracellular microtubules in non-mitotic cells, induces the formation of hyperstable tubulin polymers, and arrests cell cycling in mitosis; induces mitotic arrest at nanomolar IC50 values in cell lines from ovarian, breast, lung, colon, prostate,…

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 metabolite produced during GCDH deficiency and used as a biomarker of glutaric acidemia type 1.

Ameliorates depression, reduces dopamine-induced neurotoxicity, and attenuates damage in a model of stroke; blocks autophagy, reduces inflammation, and inhibits apoptosis in isolated neurons and in brains; induces apoptosis in colon cancer cells.

A selective, irreversible inhibitor of IL-1b converting enzyme (ICE; Caspase-1); neuroprotective in a rat model of cerebral ischemia.

The primary metabolite of PGE2 in plasma which is formed through the 15-hydroxy PGDH pathway.

An intermediate in several metabolic pathways, including glycolysis and gluconeogenesis.

A selective ERRβ/γ receptor agonist (EC₅₀ = 130 nM); used to potentiate ERRγ-induced growth inhibition in LNCaP and DU145 prostate cancer cell lines.

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 peptide that contains the sequence PVPPR, which corresponds to a region within human Sos1 that interacts with an SH3 domain of Grb2; specifically blocks the interaction of Sos1 with Grb2, preventing an interaction that is essential for Ras activation by receptor tyrosine kinases.

A selective IGF-1R inhibitor (IC₅₀ = 0.17 µM); inhibits tumor proliferation both in vitro and in a mouse model of multiple myeloma.