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.

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 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 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.

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…

An analog of trimethoxy resveratrol; inhibits the growth of a variety of human tumor cell lines at concentrations form 0.4 to 2 µg/ml, which is 5-6 times more potent than resveratrol

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…

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…

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.

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.

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…

An oxidizing reagent that reacts with nitric oxide to form nitric dioxide and corresponding imino nitroxides.

L-Arginine serves as a common substrate for both NOS and arginase in the cell. NOS catalyzes the oxidation of arginine to citrulline and NO with Nω-hydroxy-L-arginine (NOHA) formed as an intermediate. Arginase, on the other hand, catalyzes the hydrolysis of arginine into urea and L-ornithine.…

Endogenous ligand of the APJ receptor, with an EC50 of 0.37 nM; acts primarily in the periphery and CNS, playing important roles in regulating cardiovascular function, fluid homeostasis, hypertension, and insulin sensitivity.

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 dual antagonist of TP and EP4 receptors; inhibits TxA2-induced platelet aggregation (IC₅₀ = 0.26 μM) and bronchial smooth muscle contraction; impairs PGE2-mediated relaxation of piglet saphenous vein, suppresses serum-induced proliferation of fibroblasts, and reduces metastasis in a…

n-Triacontanol is a plant growth regulator found in the plant cuticle waxes and in beeswax as the palmitate ester. n-Triacontanol has been reported to have growth enhancing properties when applied to the leaves of growing plants.

A cyanoquinoline that irreversibly inhibits the receptor tyrosine kinases EGFR (IC₅₀ = 39 nM) and HER2 (IC₅₀ = 1.2 μM); disrupts Akt and MAPK pathways, inducing apoptosis and suppressing the growth of tumor cell lines.

A photosensitizer used during photodynamic therapy to eliminate abnormal blood vessels in the eye that are associated with conditions such as macular degeneration; also inhibits autophagosome formation by directly targeting and modifying p62, a scaffold and adaptor protein that binds both…

A small molecule inhibitor of nucleophosmin dimers that can prevent cell proliferation and induce apoptosis in various cancer cell lines (IC₅₀s = 1.4-4 µM).

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.

An intravenous β-lactam antibiotic that is effective against Gram-positive and Gram-negative bacteria (MICs range from 0.008-0.13 µg/ml); highly resistant to degradation by β-lactamases.

An imidazotetrazine that is converted to a compound capable of alkylating DNA, thus interfering with DNA replication and leading to cytotoxicity in proliferating cells; rapidly and completely absorbed from the gastrointestinal tract after oral administration and readily crosses the blood-brain barrier.

An inhibitor of Wnt production that impairs Wnt pathway activity (IC₅₀ = 40 nM in vitro) by inactivating Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins; promotes stem cell differentiation.

NVP-TAE226 is an inhibitor of focal adhesion kinase (FAK; IC₅₀ = 5.5 nM) and the related proline-rich tyrosine kinase 2-β (PYK2β; IC₅₀ = 5 nM). It can also inhibit the insulin-like growth factor 1 receptor (IC₅₀ = 0.16 µM) as well as the activity of…

A selective, cell permeable inhibitor of CaMKII (IC₅₀ = 900 nM).