An aminopyridazine derivative that acts as a GABAA receptor antagonist that can be used as an intermediate in the synthesis of SR 95531.

A potent and selective inhibitor of PLD1, both in vitro (IC₅₀ = 46 nM) and in cells (IC₅₀ = 11 nM); also effective as a PLD2 inhibitor at higher concentrations (IC₅₀ = 933 nM in vitro; 1,800 nM in cells); strongly inhibits the invasive migration of several breast…

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.

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.

A chromogenic substrate for N-acetyl-D-galactosaminidase that generates a yellow solution upon cleavage.

A sialic acid analog that inhibits neuraminidase release of newly replicated influenza virus particles; selectively inhibits the growth of influenza A and B viruses in plaque reduction assays (IC₅₀s = 5-14 nM) and to directly inhibit influenza A and B virus neuraminidases…

Major β-oxidation product resulting from peroxisomal metabolism of 12(S)-HETE

A chemical chaperone that rescues the trafficking of misfolded proteins and weakly blocks HDAC activity (IC50 = 0.4 mM), leading to cell cycle arrest, differentiation, and/or apoptosis of various tumors.

An inhibitor of γ-secretase, blocking the production of total Aβ in human primary neuronal cultures with an IC₅₀ value of 115 nM and Aβ42 with an IC₅₀ value of 200 nM; reduces brain levels of Aβ in vivo when given orally; indirectly inhibits Notch,…

A potent inhibitor of VEGF receptors, inhibiting VEGFR1, 2, and 3 with IC₅₀ values of 130, 23, and 18 nM, respectively; orally bioavailable in vivo, blocking VEGF-induced angiogenesis and preventing the growth of primary tumors and spontaneous peripheral metastases in mice.

Guaiacol is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. Guaiacol is readily oxidized by the heme iron of peroxidases including the peroxidase of COX enzymes. It can therefore serve as a reducing co-substrate for COX reactions. The one-electron oxidation…

AFC is a synthetic substrate for the isoprenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase). Because it is able to serve as a substrate for the methyltransferase, it effectively functions as an inhibitor of methylation of endogenous isoprenylated proteins.

A selective, potent inhibitor of ERK2 (Ki = 2 nM); inhibits proliferation of COLO 205 cells (IC50 = 0.54 µM).

A small molecule pan activator of Ras-related GTPases, activating Rac1, cdc42, Ras, and Rab-2A with EC₅₀ values of 20, 100, 141, and 355 nM, respectively.

A natural polymethoxylated flavonoid and potent antioxidant with good bioavailability; has anti-inflammatory effects that are relevant to a host of diseases, including cancer, arthritis, and neurodegeneration; inhibits P-glycoprotein and BCRP (IC₅₀ = 11.5 and 4.9 μM, respectively).

ACAT is an intracellular cholesteryl ester synthase tied closely to the absorption of dietary cholesterol. Oleic acid-2,6-diisopropylanilide is an inhibitor of ACAT with an IC50 of 7 nM. When co-administered to rabbits or rats fed a high fat, high cholesterol diet, oleic acid-2,6-diisopropylanilide…

A synthetic intermediate useful for pharmaceutical synthesis.

A selective inhibitor of PFKFB3 (IC₅₀ = 207 nM); rapidly induces apoptosis in transformed cells, suppresses glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and yields antitumor effects in human xenograft models of cancer in athymic mice.

A platinum-containing compound that acts as an alkylating agent; used alone or in combination therapy in the treatment of several types of cancer; inhibits the RecA recombinase of M. tuberculosis (IC₅₀ = 2 µM), blocking protein splicing and cell growth.

An analog of MAFP, which has been widely studied as an inhibitor of phospholipases, FAAH, and as a CB receptor ligand; pharmacology of the α-linolenyl analog of MAFP has not been completely investigated.

A pyrimadine analog that irreversibly inhibits thymidylate synthase, blocking the synthesis of thymidine which is required for DNA synthesis; widely used to treat many gastrointestinal tract adenocarcinomas.

Enzymatically-derived PGE2 is an optically pure compound whereas PGE2 derived from the free radical-catalyzed peroxidation of arachidonate is a racemic mixture. Ent-PGE2 is the opposite enantiomer of PGE2. Significant amounts of racemic PGE2 (rac-PGE2) are generated in vitro and in vivo in settings…

A polymer film used to manufacture high-performance membranes for dialysis, reverse osmosis, ion sensing, and separation; used in the production of photographic film and polarized film for liquid crystal displays.

A selective SGLT2 inhibitor (IC₅₀ = 3.1 nM) that has been shown in clinical trials of patients with type 2 diabetes to lower fasting and postprandial glucose levels by increasing total glucose excretion, improving β-cell function, and shifting substrate utilization from glucose to lipids.

A plant growth regulator with anticancer activity.

A selective, reversible inhibitor of vacuolar H+-ATPases (V-ATPases), blocking these proton pumps in mammalian, plant, or fungal cells with an IC50 value in the 4-400 nM range; also inhibits autophagy by preventing vacuolar acidification necessary for autophagosome maturation.

A first generation histamine H1 receptor antagonist (Ki = 2.6 nM) that also inhibits muscarinic acetylcholine receptors (Ki = 22 nM); penetrates the CNS, depressing central H1 receptor activity, which may relate to its sedative properties.

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.

A nucleoside analog with antiviral activity, inhibiting thymidine kinases from herpes simplex virus types 1 and 2 with Ki values of 0.14 and 0.95 µM, while blocking green monkey Vero cell thymidine kinase less effectively (Ki = 53 µM).

A potent, orally bioavailable, ATP-competitive small-molecule dual inhibitor of c-MET (IC₅₀ = 8 nM) and ALK (IC₅₀ = 20 nM) receptor tyrosine kinases; shows antitumor efficacy in multiple tumor models implanted in athymic mice that express activated c-MET or ALK fusion proteins…

TTP 22 is a thienopyrimidine compound that inhibits casein kinase 2 (CK2) with an IC₅₀ value of 100 nM (Ki = 40 nM). It displays selectivity for CK2 over JNK3, ROCK1, and MET with no inhibitory effects towards these kinases at 10 μM.

A dibenzoxazepine which acts as a selective antagonist of PGE2 at the human EP1 receptor (IC₅₀ = 6.7 µM); at doses between 0.3-300 µM, is a competitive antagonist of PGE2-induced smooth muscle contractions of guinea pig ileum and stomach and trachea.