A potent and selective farnesyltransferase (FTase) inhibitor with anti-tumor activity: inhibits rat brain FTase with a Ki value of 1.2 µM, thereby preventing Ras activation; inhibits IKK in an number of cells types.

A selective, reversible, and ATP-competitive inhibitor of the ATPase p97 (Ki = 3.2 μM; IC₅₀ = 1.5 μM); blocks endoplasmic reticulum-associated degradation, impairing the autophagy pathway and promoting the activation of caspase-3 and -7 in cancer cells.

A potent, selective, and bioavailable inhibitor of the TRPA1 channel, with IC₅₀ values of 67 and 289 nM for the human and rat isoforms, respectively; attenuates cold allodynia following nerve injury and suppresses neuronal activity in response to mechanical stimulation.

A natural alkaloid that inhibits protein synthesis at low micromolar concentrations; immobilizes ribosomes immediately after the initiation of translation.

A small molecule, multi-targeted receptor tyrosine kinase inhibitor; potently inhibits signaling through PDGFR, VEGFR, KIT, and FLT3; inhibits both tumor cell growth and angiogenesis; approved by the FDA for the treatment of gastrointestinal stromal tumor and metastatic renal cell carcinoma.

An inhibitor of mitochondrial F1FO ATP synthase that induces apoptosis in a variety of cell types (average GI50 = 270 nM); exhibits antifungal, antitumor, and nematocidal activities, but has poor solubility in water and other biocompatible solvents.

A natural bicyclic depsipeptide that, following reduction, selectively inhibits class I HDACs (IC₅₀s = 53, 39, 53, and 26 nM, for HDACs 1, 2, 3, and 8, respectively); has anti-cancer activities, particularly against certain T cell lymphomas.

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 potent peptide agonist of the GLP-1 receptor (Ki = 136 pM); stimulates glucose-induced insulin secretion in isolated rat islets and proinsulin expression in mouse insulinoma βTC-1 cells, supporting efficacy in type 2 diabetes; protects hippocampal neurons against glutamate-induced apoptosis.

A divalent cation ionophore, commonly used to facilitate the movement of Ca2+ into cells, triggering the activation of intracellular calcium-dependent pathways; also used to produce apoptosis through calcium overload, as occurs during hypoxic or oxidative stress.

An orally active, allosteric Akt inhibitor (IC50s = 5, 12, and 65 nM for Akt1, 2, and 3, respectively); inhibits cell proliferation of human cancer cell lines synergistically in combination with other topoisomerase inhibitors, antimetabolites, antimicrotubule agents, DNA cross-linkers or growth…

A metabolite of vinclozolin, a dicarboximide fungicide, that acts as an effective antagonist of the androgen receptor (Ki = 9.7 µM in rat).

CZC-54252 is an inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC₅₀s = 1.28 and 1.85 nM for wild-type and G2019S mutant forms of LRRK2, respectively). It has been shown to protect against neuronal injury induced by Parkinson’s disease-related LRRK2-G2019S mutant activity in…

An active, estrogenic metabolite of daidzein; has vasodilatory action on rat isolated aortic rings at 1 µg/ml; stimulates the estrogen receptor-dependent growth of breast cancer MCF-7 cells at micromolar concentrations.

A highly selective, non-ATP competitive inhibitor of p38/mitogen-activated protein kinase-activated protein kinase 2 (IC₅₀ = 0.11 μM); inhibits TNF-α (IC₅₀ = 4.4 μM) and IL-6 (IC₅₀ = 5.2 μM) secretion from the human THP-1 acute monocytic leukemia cell line.

A selective β₃-adrenergic receptor antagonist.

Initiates glycogen synthesis in hepatocytes by causing inactivation of phosphorylase a and activation of glycogen synthase a (maximal effects with ~20 µM Itu); potent inhibitor of ERK2 (Ki = 525 nM).

A cell-permeable inhibitor of Arp2/3 complex action that inhibits actin polymerization in vitro, using human, bovine and fission yeast proteins (IC₅₀s = 4, 32, and 24 µM, respectively); prevents the formation of actin filament comet tails by Listeria in infected SKOV3 cells…

A nitroimidazole with radiosensitizing and antineoplastic properties; metabolites accumulate in hypoxic cells and can themselves be cytotoxic or they can increase the chemosensitivity and radiosensitivity of the target cells; used in the imaging of hypoxic regions in tumors and in the…

A small molecule pan activator of Ras-related GTPases, activating cdc42, Ras, and Rac1 with EC₅₀ values of 102, 109, and 151 nM, respectively.

A TZD that increases the sensitivity of cells to insulin, stimulating insulin-induced PI3K activity at submicromolar concentrations; increases insulin effectiveness in obese NIDDM subjects; promotes adipocyte differentiation by up-regulating the expression of UCP-2.

Formal Name: 6-amino-1,4-dihydro-1,3-dimethyl-4-[4-(trifluoromethyl)phenyl]-pyrano[2,3-c]pyrazole-5-carbonitrile CAS Number: 1637739-82-2 Molecular Formula: C₁₆H₁₃F₃N₄O Formula Weight: 334.3

A potent, selective antagonist of σ1 receptors (Ki = 17 nM) that weakly binds σ2 receptors (Ki = 9,300 nM); dose-dependently inhibits neuropathic pain in several animal models, including formalin-induced nociception and capsaicin-induced mechanical hypersensitivity.

A nonselective inhibitor of the mitochondrial F1FO ATP synthase that can reduce the rate of ATP depletion in myocardial ischemia and decrease calcium-induced calcium release oscillation frequency of rat sensory neurons.

A fluorescent probe commonly used to measure pH.

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

Inhibits ALK5- (IC50 = 47 nM), ALK4- (IC50 = 129 nM), and ALK7-dependent activation of downstream SMAD2 and SMAD3 and TGF-β–induced MAP kinase pathway components without altering ALK1-3 or ALK6-induced SMAD signaling.

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.

8-iso PGF1β is a potential autoxidation product of DGLA. There are no published reports on its isolation from any biological source or on its biological activity.

A synthetic thyroid hormone mimetic that lowers total and LDL cholesterol up to 40% when administered to humans at a dose of 50-200 µg once daily for 14 days; stimulates cholesterol catabolism to bile acids without affecting cholesterol synthesis.

A first generation cephalosporin antibiotic that is broadly effective against gram-negative and gram-positive bacteria; mainly used in veterinary medicine for intramammary treatment of mastitis and intrauterine treatment of endometritis in cattle.

A potent inhibitor of all HDACs, with Ki values ranging from 0.6 to 31 nM for HDAC1-11; leads to acetylation of a range of cellular proteins, resulting in cell cycle arrest and apoptosis in cancer cells; has potential applications in spinal muscular atrophy and HIV therapy.