A selective NMDA receptor antagonist (Kd = 1.4 μM) that competitively inhibits the glutamate binding site of NMDA receptors; widely used to study the activity of NMDA receptors particularly in regard to researching synaptic plasticity, learning, and memory.

CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.

A potent, selective antagonist of the serotonin 5-HT6 receptor (pKi = 8.53); has been used in cells and in animals.

A naturally occurring agonist for the nuclear receptor Nur77 (IC₅₀ = 0.278 nM); induces apoptosis in cancer cells and retards xenograft tumor growth; induces genes related to gluconeogenesis and decreases atherosclerosis progression in mice fed a high fat/high cholesterol diet.

A synthetic H2S donor that can be readily esterified with other moieties, including therapeutics and targeting motifs; used both in cells and in animals for comparative studies with derived chimeras.

A-77-01 is a potent inhibitor of the TGF-β1 receptor ALK5 (IC₅₀ = 25 nM). It has no effects on BMP-regulated transcriptional activity or MAPK pathways. A-77-01 efficiently prevents the growth inhibitory effects of TGF-β on lung epithelial Mv1Lu cells. It completely blocks…

A mycotoxin produced by A. ochraceus, A. carbonarius, and P. verrucosum that is commonly found as a food contaminant (Tolerable Weekly Intake = 100 ng/kg body weight per day); triggers nephropathy, induces renal adenomas, and initiates skin tumors through events involving oxidative stress,…

Best known as a potent dual inhibitor of c-Src and Abl (IC50 = 1.2 and 1.0 nM, respectively); can be effective in regulating tumor growth and differentiation; also inhibits other members of the Src and TEC families and certain other kinases at nanomolar concentrations.

An inhibitor of Wnt production that impairs Wnt pathway activity (IC₅₀ = 27 nM in vitro) by inactivating Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins; used to suppress embryonic stem cell self-renewal and to decrease cancer cell proliferation,…

A DR5 agonist (Kd= 1.2 µM; IC₅₀ = 2 µM) that induces DR5 clustering, which leads to the initiation of FADD/caspase-8-dependent apoptosis in various cancer cells.

A nuclesoside analog that disrupts DNA synthesis in blood cells; effective in a number of animal tumor systems including LI210 leukemia, CD8F mammary adenocarcinoma, P388 leukemia, and human LX-1 lung tumor xenograft and displays anticancer activity against human hematological malignancies in vivo.

A microbial metabolite that binds the TCR on Vγ9Vδ2 peripheral blood lymphocytes with high affinity (EC50 = 0.39 nM); induces the expansion of human memory Vγ9Vδ2 T cells.

A potent and selective inhibitor of Wip1 (IC₅₀ = 6 nM); increases phosphorylation of Wip1 substrates and blocks cell cycling in cancer cells; orally bioavailable, causing inhibition of lymphoma xenograft growth in mice.

A fluorogenic substrate that can be cleaved specifically by group I caspases.

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

A selective inhibitor of 15-hydroxy PGDH (IC₅₀ = ~10 µM).

A potent and selective inhibitor of DGAT-1 (IC₅₀ = 19 nM); has high oral bioavailability (100%) in rats with a moderate half-life of 6.8 hours; significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats.

A potent inhibitor of PI3K isoforms α, δ, and γ (IC₅₀s = 0.28, 0.12, and 0.97 nM, respectively) that is 31 times less potent at PI3Kβ; has increased potency in cancer cell lines harboring PIK3CA-activating alterations, and is effective in vivo.

A selective slow off-rate inhibitor of Raf kinases (IC₅₀s = 8.3, 2.4, and 1.4 nM for wild type B-Raf, mutant B-RafV600E, and c-Raf, respectively); shows significant antiproliferative activity against mutated BRAF or mutated NRAS cancer cell lines and xenograft models.

A hybrid molecule of indomethacin and an NO donor which combines the anti-inflammatory properties of an NSAID with the gastrointestinal protective effects of NO.

A thiol-reactive probe that can be used to label proteins at cysteine residues.

A selective inhibitor of PI3Kγ

A colchicine derivative that inhibits tubulin polymerization (IC₅₀ = 2.1 μM) with low toxicity; suppresses microtubule dynamicity, inhibits cell migration, blocks microtubule assembly, and arrests cells in metaphase; used to synchronize cells and for karyotyping in cytogenetic studies.

A homolog of DHEA, characterized by the addition of an (S)-β-methyl group at the terminal ethanolamine carbon.

PGF2α 1,9-lactone is a lipid-soluble internal ester of PGF2α. It is resistant to hydrolysis by human plasma esterases even after incubation for 20 hours under physiological conditions. PGF2α 1,9-lactone exhibits little antifertility and vasoactivity compared to PGF2α.

A small molecule activator of AMPK that stimulates functional activation of AMPK in cultured muscle cells (EC50 = 4.3 μM), enhancing glucose uptake by 3.2-fold; 10 mg/kg up-regulates the activity of AMPK in the liver and muscle of diet-induced obese mice, enhancing insulin sensitivity and…

The major metabolite of the gastric proton pump inhibitor, omeprazole; produced by CYP3A4 sulfoxidation of esomeprazole.

A salen-manganese complex with catalase and SOD mimetic activity.

Selective inhibitor of aldo-keto reductase 1C1 (AKR1C1; Ki = 4 nM) versus AKR1C2, AKR1C3, and AKR1C4 (Ki = 0.087, 4.2, and 18.2 μM, respectively); potently inhibits the metabolism of progesterone in endothelial cells overexpressing AKR1C1 (IC₅₀ = 460 nM).

A stable analog of ATP that acts as a potent agonist of G protein-coupled P2Y2 and P2Y11 receptors (pEC₅₀ = 5.52 for P2Y11).

An inhibitor of HIF-1α protein translation; suppresses phosphorylation of two key regulators of protein synthesis, eukaryotic translation initiation factor 4E binding protein 1 (4EBP1) and p70 S6 kinase; cytotoxic to a variety of cancer cell lines with an IC₅₀ value of 15-25 µM.

An inhibitor of CETP; inhibits plasma CETP with an IC₅₀ value of 9 µM; in rabbits given an atherogenic diet, increases HDL, decreases VLDL, and attenuates induced atherosclerosis; in humans, inhibits CETP activity and increases HDL levels but does not reduce the risk of recurrent…