A cyclic hexapeptide mycotoxin that binds β-tubulin in a vinca domain; blocks microtubule growth, modulates the dynamics of microtubules, and interferes with mitosis.

Blocks CYP17A1 by potently inhibiting both the 17α-hydroxylase and the 17,20 lyase activities (IC₅₀ = 18 and 17 nM, respectively); essentially eliminates plasma testosterone while producing a 3- to 4-fold increase in plasma luteinizing hormone.

An analytical reference material categorized as a phytocannabinoid; a precursor in the biosynthesis of tetrahydrocannabinolic acid, cannabidiolic acid, and cannabichromenic acid; intended for research and forensic applications

Selectively inhibits human NHE-1 with an IC₅₀ value of 14 nM; reduces infarct size in a rabbit myocardial ischemia-reperfusion model without adversely affecting hemodynamics or cardiac function.

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 small diffusible signaling molecule involved in quorum sensing in the model symbiont V. fischeri and the pathogens A. tumefaciens and P. aeruginosa.

A small molecule inhibitor of DNA ligase IV that prevents nonhomologous end-joining by interfering with the ligase binding and activating apoptosis; inhibits cancer cell growth in vitro (IC₅₀s = 8-120 µM) and in mouse models when co-administered with double-strand break-inducing…

A non-reducing inhibitor of 5-LO that shows selectivity for 5-LO over 12-LO or COX; inhibits topoisomerase II activity and arrests cell cycling or induces apoptosis in cancer cells.

A selective CaMKII inhibitor (IC₅₀ = 40 nM) that was designed based on the sequence around the autophosphorylation site (Thr286/Thr287) in the autoinhibitory domain of the protein kinase.

An F-series PG analog in which the C-1 carboxyl group has been modified to an N-diethyl amide; dialkyl amides such as a 17-p-PGF2α-NEt2 are inert to corneal amidase activity, and are not converted in any detectable amount to the corresponding free acids.

An inhibitor of S1P lyase; treatment of mice (50 µg/ml in drinking water) increases lymphoid tissue S1P concentrations 100-fold, reducing lymphocyte egress from thymus and peripheral lymphoid organs, resulting in reversible lymphopenia.

A cell-permeable ACL inhibitor (IC₅₀ = 0.13 µM) that has been reported to reduce weight gain and lower plasma cholesterol, triglycerides, and glucose in a mouse model of hyperlipidemia.

An FGFR inhibitor.

A naturally occurring metabolite of bile acid that is produced by the conjugation of cholic acid and sulfate, predominantly in the liver and gut.

A reversible inhibitor of the cis-Golgi ArfGEF, GBF1 (IC₅₀ = 3.3 µM); induces rapid dissociation of COPI vesicle coat protein from Golgi membranes and disassembly of the Golgi and trans-Golgi network, preventing bidirectional transport of endocytic cargo.

An endogenous agonist for LXRα (EC₅₀ = 325 nM) that can induce the expression of the ABCA1 reverse cholesterol transporter to inhibit the overall absorption of cholesterol; used as a substrate to monitor cholesterol transport or as an endogenous positive control for testing LXR agonists.

A potent inhibitor of 15-PGDH (Ki = ~0.1 nM) that has activity in vivo; rapidly increases the levels of PGE2 in bone marrow and other tissues in mice after intraperitoneal injection.

An inhibitor of β-catenin/Tcf-mediated transcription and an antagonist of ligand-dependent activation of PPARγ and PPARδ; blocks the recruitment of β-catenin and GRIP1 to PPARγ and PPARδ; selectively toxic to some carcinoma cell lines expressing the…

A potent, selective inhibitor of ATR (IC₅₀ = 5 nM); inhibits the growth of LoVo colorectal adenocarcinoma cells in vitro and significantly reduces the growth of LoVo xenografts in mice.

A cell-permeable bis-indolo (indirubin) compound that acts as a highly potent, selective, reversible, and ATP-competitive inhibitor of GSK3α/β (IC₅₀ = 5 nM); inhibition of GSK activates the Wnt-signaling pathway and sustains pluripotency in human and mouse ESCs; maintains…

A variety of natural products from plant sources, particularly flavonoids, have long been observed to have antioxidant activity with potential benefits for human health. Antioxidant triterpenes are less common. Celastrol is a triterpenoid antioxidant compound isolated from the Chinese thunder god…

A specific inhibitor of N-linked glycoslylation that blocks the first step of glycoprotein synthesis and induces protein unfolding; impairs the function of several receptor tyrosine kinases, including EGFR, ErbB2, ErbB3, IGF-IR, and ALK; radiosensitizes glioma and pancreatic adenocarcinoma cells to…

Myriocin is an amino fatty acid antibiotic derived from certain thermophylic fungi, in this case Mycelia sterilia. It is a potent immunosuppressant having 10- to 100-fold more activity than cyclosporin A. Myriocin is a potent inhibitor of serine palmitoyltransferase (Ki = 0.28 nM), the enzyme that…

An inhibitor of non-structural protein 5A of hepatitis C virus; effectively reduces or eliminates certain genotypes of hepatitis C virus in vivo, particularly when used in combination with other agents.

A non-lipid agonist of LPA2 (EC₅₀ = 0.10 µM) that is without effect at other LPA receptor subtypes; protects IEC-6 cells against caspase activation and apoptosis following irradiation; increases the survival of mice suffering from hematopoietic acute radiation syndrome after…

An inhibitor of SRE activation in PC3 cells (IC₅₀ = 6.4 μM), with 87% inhibition of SRE activation achieved at 100 μM; inhibits PC3 cell migration (IC₅₀ = 4.2 μM), as determined by a scratch wound assay; causes no cytotoxicity when evaluated by WST-1 assay.

A cell-permeable inhibitor that binds actin filaments, but not actin monomers, to inhibit polymerization at concentrations as low as 0.2 µM.

SC-560 is a member of the diaryl heterocycle class of COX inhibitors which includes celecoxib (Celebrex™) and rofecoxib (Vioxx™). However, unlike these selective COX-2 inhibitors, SC-560 is a selective inhibitor of COX-1. Using human recombinant enzymes, the IC₅₀ value for…

Reversibly inhibits dihyroorotate dehydrogenase, the rate-limiting step in the de novo synthesis of pyrimidines, preventing DNA synthesis of activated lymphocytes (IC₅₀s = 0.09, 3.5, and 12.5 μM for rat, mouse, and human, respectively); also inhibits tyrosine kinases responsible for…

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.

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…

A selective inhibitor of RNA polymerase I-driven transcription of rRNA (IC₅₀s = 142, 113, and 54 nM in HCT116, A375, and MIA PaCa-2 tumor cells, respectively); demonstrates in vivo antitumor activity against human solid tumors in mouse xenograft models.