An inhibitor of PLC-dependent processes by an undefined mechanism; inhibits platelet aggregation induced by collagen or thrombin with IC₅₀ values of 0.6 and 5 µM, respectively.

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 non-selective bromodomain inhibitor that at 1 µM has been shown to accelerate FRAP recovery of BRD4 and CREBBP bromodomains in HeLa cells.

A dual purpose probe; a chemiluminescent probe that detects superoxide production by enzymatic and cellular sources; a fluorescent chloride-sensitive indicator, with fluorescence being quenched by chloride (excitation: 455 nm; emission: 505 nm).

ß-Casomorphin is a peptide fragment of casein that exhibits antioxidative and anti-fibrotic activities. In vivo, ß-casomorphin improves high glucose-induced changes in oxidative enzyme secretion and activity. ß-Casomorphin also decreases urinary glucose and protein levels as well as serum creatine…

A major urinary metabolite of PGE2 that is excreted in guinea pig urine at a concentration range of 1.34-2.74.

A red/orange-colored fat-soluble terpenoid with antioxidant properties; can be cleaved to produce vitamin A and retinoic acid.

The major estrogen secreted by the premenopausal ovary.

A natural sesquiterpene that inhibits the proliferation of a wide range of tumors and enhances the effects of various chemotherapies; 10-40 µg/ml dose-dependently induces apoptosis and cell cycle arrest in the G2/M phase in HepG2 cells, upregulating Fas/FasL expression.

A potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC₅₀ = 70 nM), compared to PI3Kα (IC₅₀ = 240 nM), PI3Kβ (IC₅₀ = 1.45 μM), and PI3Kδ (IC₅₀ =1.70 μM); shows little or no activity against 38 other…

Adrenocorticotropic hormone (ACTH) is a peptide derived from proopiomelanocortin (POMC) processed and secreted in the pituitary gland. ACTH binds and activates melanocortin-2 (MC2) receptors, stimulating cortisol production in the adrenal cortex. ACTH exhibits anti-inflammatory and immunomodulatory…

Pargyline is an irreversible inhibitor of monoamine oxidase (MAO) that is used clinically to treat moderate hypertension. At 10 mg/kg iv, pargyline induces a moderate decrease of systolic blood pressure in unanaesthetized hypertensive rats but not normotensive WKR or Sprague-Daley rats. The…

A selective small molecule activator of SIRT1 that is 1,000-fold more potent than resveratrol; improves insulin sensitivity, lowers plasma, glucose and increases mitochondrial capacity in diet-induced obese and diabetic leptin-deficient ob/ob mice after one week of treatment with an oral dose of…

An activator of sGC, stimulating activity at concentrations as low as 10-100 nM; inhibits platelet aggregation (IC50 = 36 nM), induces relaxation of preconstricted aorta rings (IC50 = 304 nM); effective in vivo, decreasing mean arterial blood pressure in hypertensive rats.

An orally bioavailable, reversible inhibitor of JAK1 and JAK2 (IC₅₀s = 5.9 and 5.7 nM, respectively) that has been shown to inhibit cytokine-induced phosphorylation of STAT3 in healthy human volunteers.

An ATP/GTP-competitive inhibitor of CK2 (IC₅₀ = 900 µM for rat liver CK2); less potently inhibits CCK2/cyclin A, GSK3β, and phosphorylase kinase (IC₅₀ = 15.6, 11.2, and 8.7 mM, respectively); much less effective against a range of other kinases.

A pyrimadine analog that irreversibly inhibits thymidylate synthase, blocking the synthesis of thymidine which is required for DNA synthesis; widely used to treat many gastrointestinal tract adenocarcinomas.

A third generation fluoroquinolone with antibacterial activity; inhibits type II topoisomerases (IC₅₀s = 8.06 and 9.81 µg/ml for DNA gyrase and topoisomerase IV, respectively).

A mixture of at least four closely related components, polymyxin B1 to B4, with polymyxin B1 and B2 being the two major components; demonstrates rapid in vitro bactericidal activity against major multidrug-resistant Gram-negative bacteria, including P. aeruginosa, A. baumannii, and K. pneumonia.

A non-selective blocker of voltage-dependent K+-channels (Kv channels) that has greatest potency at Kv1 and Kv3 family members (IC₅₀s = 290, 590, 195, 13, 29, and 100 µM for subunits 1.1, 1.2, 1.3, 1.4, 3.1, and 3.2, respectively); also blocks Kv2 and Kv4 subunits at millimolar concentrations.

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.

An antagonist of CXCR4, blocking CXCR4-mediated HIV infection with an IC50 value of 19.3 nM; at 100 μg/ml, inhibits CXCL12-induced phosphorylation of p42/44 MAPK and STAT3; activates CXCR7 (EC50 = 350 nM), resulting in the recruitment of β-arrestin and Erk ½ phosphorylation.

Capsaicin is an agonist of transient receptor potential vanilloid (TRPV) channels that was originally found in peppers of the Capsicum genus. Capsaicin exhibits analgesic, anti-inflammatory, anti-obesity, and anticancer chemotherapeutic activity. Capsaicin also displays bronchoconstrictive activity…

A cell-permeable, selective inhibitor of calcineurin-mediated dephosphorylation of NFAT that does not disrupt other calcineurin-dependent pathways; disrupts NFAT-dependent expression of IL-2 and TNF-α when transfected in Jurak T cells and prevents the activation and proliferation of T cells…

An isoflavonoid phytoestrogenic compound found in soybeans, pea pods, clover, kudzu, and other legumes.

Benzyl isothiocyanate (BITC) is an isothiocyanate originally found in cruciferous vegetables that exhibits immunomodulatory, anti-parasitic, antibiotic, antioxidative, anti-atherosclerotic, anti-angiogenic, anti-metastatic, anticancer chemotherapeutic, and chemopreventive activities. BITC inhibits…

A non-nucleoside reverse transcriptase inhibitor that binds to viral reverse transcriptase and blocks polymerase activity by preventing RNA plus-strand initiation (IC₅₀s = ~ 0.45 to 0.9 μM).

An orally available, selective agonist of GPR120 (EC₅₀ = ~0.35 µm); exerts anti-inflammatory effects on macrophages in vitro and improves glucose tolerance, decreases hyperinsulinemia, increases insulin sensitivity, and decreases hepatic steatosis when included at 30 mg/kg body…

13(S)-HpODE is produced by the oxidation of linoleic acid by LO-1 in many plants including soybean, flaxseed, apples, and tea leaves, and by 15-LO in mammals. In plants, 13(S)-HpODE is the preferred substrate for the garlic bulb divinyl ether synthase. In mammalian tissues, 13(S)-HpODE is generally…

16,16-dimethyl PGF2β is a metabolically stable analog of PGF2β. It prevents bronchospasm in asthmatics but is less potent than PGE2.

A substrate for β-galactosidase, the lactose repressor, the galactose-binding protein, the β-methylgalactoside transport system, and thiogalactoside transacetylase.