A selective inhibitor of mutant B-RafV600E (IC₅₀ = 0.8 nM), with 4- and 6-fold reduced potency against wild type B-Raf and c-Raf (IC₅₀s = 3.2 and 5 nM, respectively); studied in clinical trials in patients with B-RafV600E metastatic melanoma and other solid tumors.

An inhibitor of DPP-4 (IC₅₀ = 3.5-34 nM); also inhibits DPP-8 and DPP-9 (Ki = 810 and 95 nM, respectively) but not DPP-2 or FAPα; blocks the degradation of several circulating peptides, including incretins; reduces fasting and postprandial glucose levels and decreases inflammatory…

An intermediate produced from vitamin D2 by cytochrome P450 isoforms in vertebrates; subsequently metabolized to 1,25-dihydroxy vitamin D2, which is an agonist for the vitamin D receptor.

A major inactive metabolite of clopidogrel that is used as a reference standard for quantitative analysis of clopidogrel metabolism.

A neuroexcitatory amino acid that functions as a NMDA and metabotropic glutamate receptor agonist; used to induce brain lesions in animal models of cognitive dysfunction.

Aprotinin is a polypeptide that exhibits anti-fibrinolytic (pro-coagulant) activity. Aprotinin inhibits serine proteases such as trypsin, chymotrypsin, plasmin, and kallikrein. Inhibiting these proteases prevents formation of Factor XIIa and prevents breakdown of blood clots. Aprotinin is…

A toxin produced by cyanobacteria that inhibits the catalytic activity of protein phosphatases PP1C, PP1γ, and PP2A with Ki values of 0.15, 0.24, and 0.018 nM, respectively.

Reversibly binds tubulin and alters GTP hydrolysis as well as microtubule dynamics; nanomolar concentrations reduce both microtubule elongation and shortening velocities, resulting in arrest of cycling in a G2/M phase; also used to induce the formation of Golgi ministacks in eukaryotic cells.

Sodium butyrate is an inhibitor of histone deacetylases (HDACs) that exhibits antidepressant, immunomodulatory, and anticancer activities. In animals undergoing the light dark test, tail suspension test, and forced swim test, sodium butyrate decreases restraint stress-induced depression. In…

A nucleoside analog with antiviral activity, inhibiting thymidine kinases from herpes simplex virus types 1 and 2 with Ki values of 0.14 and 0.95 µM, while blocking green monkey Vero cell thymidine kinase less effectively (Ki = 53 µM).

PGF1β is the C-9 epimer of PGF1α. It was shown to enhance respiratory rate in experimental animals when administered intravenously.

Tris-HCl Stock Solution (1 M, pH 7.0) contains filtered Tris-HCl (1 M, pH7.0). It is ready to use as supplied.

A stable, cell-permeable molecule that generates free α-ketoglutarate upon hydrolysis by cytoplasmic esterases; used in experiments to increase levels of intracellular α-ketoglutarate and modulate a variety of enzymes, particularly in the context of glycolysis, hypoxia, and cancer.

A cell-impermeable, negatively charged tetrazolium dye that produces a water-soluble formazan when reduced at the cell surface by cellular-derived NADH and an electron mediator.

Benztropine is an inhibitor of the dopamine transporter (DAT); it potentiates dopamine overflow in rat brain slices.

The racemic version of a CYP450 metabolite of arachidonic acid that dose-dependently stimulates vasodilation of the rabbit kidney.

Formal Name: 3,4-dichloro-N-(1-methylbutyl)-benzamide CAS Number: 7497-07-6 Molecular Formula: C₁₂H₁₅Cl₂NO

3-Tert-butyl-4-hydroxyanisole (3-BHA) is one component of butylated hydroxyanisole (BHA). This compound is commonly used as a food additive; it exhibits antioxidative and anticancer activities. In leukemia cells, 3-BHA decreases the mitochondrial membrane potential, inhibits mitochondrial oxidative…

20-ethyl PGE2 is an analog of PGE2 in which the ω-chain has been extended by the addition of two methylene carbon atoms. The only well studied prostaglandin analog with this structural feature is unoprostone, an F-series prostaglandin that is clinically approved as a glaucoma medication.…

A potent blocker of small conductance Ca2+-activated K+ (SK, KCa2) channels that is more effective at SK2 than SK1 and SK3 (IC₅₀ values are 0.06-0.4, 1-12, and 1-13 nM, respectively); ineffective against SK4 at 1 µM.

A GABAA receptor agonist (IC₅₀ = 19 nM) that has been used as a photoaffinity label for the purification and identification of GABA binding sites within the GABAA receptor complex.

A phorbol ester that is commonly used to activate certain types of protein PKC and, indirectly, certain MAP kinase pathways; prolonged treatment with PMA produces various effects, ranging from tumorigenesis to hematopoietic differentiation.

Allicin is an thiocyanate found in garlic; it exhibits a wide variety of properties, including anticancer, antioxidative, antihypertensive, anti-arrhythmic, anti-parasitic, and anti-diabetic activities. In vitro, allicin binds cellular nucleic acid, primarily nitrogenous bases and phosphate…

ARRY-162 is an orally bioavailable noncompetitive inhibitor of MEK1/2 and ERK that shows anticancer chemotherapeutic activity. Inhibition of MEK inhibits downstream signaling by IL-1, IL-6, and TNF. ARRY-162 inhibits proliferation in melanoma, non-small-cell lung cancer (NSCLC), head/neck cancer,…

Bitertanol is an antifungal pesticide; it acts as a demethylation inhibitor, preventing sterol biosynthesis and disrupting membrane function. Bitertanol increases glutathione-S-transferase activity in the liver of rats, displaying potential antioxidative activity. Additionally, bitertanol alters…

A non-enzymatic hydrolysis product of LTA4 with reduced activity compared to LTB4; also produced by oxidative decomposition of CysLTs such as LTC4 in the presence of myeloperoxidase and hypochlorous acid.

A lipoic acid analog that inhibits α-ketoglutarate dehydrogenase, particularly in tumor cells; induces a strong mitochondrial burst of reactive oxygen species at 60-240 µM, resulting in cell death; demonstrates both in vitro and in vivo anti-tumor activity.

A fluorogenic substrate for human leukocyte and porcine pancreatic elastase; excitation: 355-380 nm; emission 440-460 nm.

A synthetic PGA1 analog with structural features similar to 15-deoxy-Δ12,14-PGJ2, a ligand for PPARγ.

A selective autotaxin inhibitor (IC50 = 5.7 nM) that has been shown to dose-dependently block thrombin-induced LPA secretion in platelets.

Thiazolidinediones (TZDs) are a group of structurally related PPARγ agonists with anti-diabetic actions in vivo. Rosiglitazone (BRL49653) is a prototypical TZD and has served as a reference compound for this class of PPARγ ligands. Pioglitazone is a closely related TZD which also…

An atypical, second generation antipsychotic compound that has effects at multiple receptors; antagonizes dopamine D1, D2, and D3 receptors, serotonin 5-HT1A, 5-HT2A, and 5-HT7 receptors, and α1A, α1B, and α2C adrenergic receptors.