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 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 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…

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…

The L isomer of the biologically important D-myo-inositol-1,4,5-triphosphate; does not evoke a rise in intracellular calcium when added to cells.

A dietary carotenoid present in the macula region of the eye; high dietary intake correlates with reduced risk of age-related macular degeneration.

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 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 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.

An internal standard for the quantification of estriol by GC- or LC-MS.

A inhibitor of Epac1 and Epac2 (IC₅₀s = 3.2 and 1.4 µM, respectively); blocks Akt phosphorylation and insulin secretion in pancreatic β cells and inhibits the migration of AsPC-1 and PANC-1 pancreatic cancer cells in vitro.

A γ-secretase inhibitor that blocks Notch processing (IC₅₀ = 1.7 nM); reduces Aβ40 levels by 71% in an APP transgenic mouse model within 4 hours after a single 100 μM/kg dose.

An irreversible inhibitor of EGFR sensitizing and T790M resistance mutations (IC₅₀s = 15-17 nM) while sparing the wild-type EGFR (IC₅₀ = 480 nM); inhibits tumor growth in a xenograft mouse model at oral doses of 5-10 mg/kg.

A selective BRD9 bromodomain inhibitor (pIC₅₀ = 7.3; pKd = 8.7); used to identify genes regulated by BRD9 in Kasumi-1 cells involved in cancer and immune response signaling.

A decomposition product of the macrolide antibiotic, erythromycin A that has been identified as a β-turn mimic of the peptide hormone motilin; used to determine the binding characteristics of ligands of the motilin receptor.

An analog of latanoprost in which the hydroxyl at C-15 is inverted relative to latanoprost; binds to the FP receptor in the cat iris sphincter muscle with an IC₅₀ value of 24 µM (tested as the free acid); potential impurity in latanoprost bulk drug preparations.