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.…

A cell-permeable mycotoxin which binds to the barbed end of actin, reversibly inhibiting the elongation and shortening of actin filaments; blocks diverse cellular functions, including cell division, migration, phagocytosis, exocytosis, chemotaxis, and glucose transport.

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…

An active, deacetylated metabolite of T-2 toxin; inhibits protein synthesis and cell proliferation in plants; causes acute and chronic toxic effects in animals that ingest contaminated plant materials.

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…

A mycotoxin that inhibits RNA polymerase II and III but not RNA polymerase I or bacterial RNA polymerase, thus preventing mammalian protein synthesis.

The less predominant-occurring (~20%) stereoisomer of the endogenous oxysterol 27-hydroxy cholesterol.

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 potent and selective EP4 receptor antagonist (Ki = 24 nM); reverses the anti-inflammatory action of PGE2 in LPS - activated human macrophages at 100 nM.

A FAHFA in which palmitic acid is esterified to 9-hydroxy palmitic acid.

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 microbial metabolite isolated from Streptomyces that is widely used as a selective inhibitor of the 20S proteasome.

A regioisomeric resveratrol metabolite that may be used as a reference standard for accurate determination of the metabolic profile of resveratrol.

A cell-permeable and selective inhibitor of PIKfyve (IC₅₀ = 33 nM); reversibly impairs endosomal trafficking in NIH3T3 cells and blocks retroviral exit by budding from cells; inhibits basal and insulin-activated 2-deoxyglucose uptake (IC₅₀ = 54 nM) in adipocytes.

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 glutamine analog that irreversibly inhibits glutamine-dependent amidotransferases involved in nucleotide and amino acid biosynthesis (Kis = 10 and 560 μM for anthranilate synthase and glutamate synthase, respectively); reversibly inhibits γ-glutamyl transpeptidase.

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 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.

A major metabolite of sulforaphane that has been shown induce ARE-driven gene expression with roughly 8-fold less potency than sulforaphane.

A natural oxidative metabolic of the mycotoxin aflatoxin B1; produced from aflatoxin B1 in mammals and then secreted in milk.

Bromosporine is an inhibitor of BET bromodomains (BRDs) BRD2, BRD4, BRD9, and CECR2; it may exhibit anticancer potential.

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.

An antagonist of the EP4 receptor (Ki = 1.3 nM) that less potently affects EP3, FP, and TP receptors (Kis = 30, 790, and 2,400 nM, respectively) and is without effect on other prostanoid receptors; implicates EP4 signaling in immune and autoimmune responses, inflammation, and cancer.

A trichothecene mycotoxin that can infect grain crops causing alimentary toxic aleukia in humans and animals; inhibits protein synthesis, disrupts membrane phospholipid metabolism, increases lipid peroxides in the liver, and is highly cytotoxic to macrophages (IC50 = 19.47 nM), altering the…

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).

A potent, ATP-competitive inhibitor of ROCKs including p160ROCK (Ki = 140 nM) and ROCK-II (IC50 = 800 nM); also inhibits PRK2 with an IC50 value of 600 nM.

A β3-adrenergic receptor agonist (EC₅₀ = 22.4 nM) that displays potent selectivity for β3 compared to the β1 and β2 receptor subtypes (EC₅₀s ≥ 10 µM); relaxes rat and human bladder strips precontracted with carbamoylcholine (EC₅₀s = 5.1…

A staurosporine derivative that binds to dephosphorylated c-Met kinase and to the colchicine binding site of tubulin; promotes mitotic arrest and apoptosis of various human tumor cell lines (EC₅₀s ranging from 60-600 nM).

A selective and competitive inhibitor of NAD+-dependent type-I 15-PGDH (IC₅₀ = 26.4 nM; Ki = 5 nM).

A naturally-occurring macrocyclic lactone that is a potent insecticide; acts as an agonist of insect nicotinic acetylcholinesterase receptors (nAChRs), which differ both structurally and functionally from nAChRs in vertebrates.