A GABAA receptor agonist whose potency varies depending on the receptor subunit composition (partial agonist at α1β2γ2 (ED50 = 143 µM), full agonist at α5 (ED50 = 28-129 µM), and super agonist at α4β3δ (ED50 = 6 µM)); acts as an antagonist…

Aflatoxins are mycotoxins found in foods and livestock feeds that were initially produced by species of Aspergillus. Aflatoxin G2 is cytotoxic; it inhibits DNA synthesis and induces cell cycle arrest.

Hydroxy linoleins are a mixture of 132 possible isomers of mono-, di-, and tri-hydroxy compounds produced by the autoxidation of trilinolein and subsequent reduction of the hydroperoxides. Autoxidation of linoleic acid containing triglycerides (i.e., trilinolein) in vivo could result in the…

A tumor-promoting teleocidin compound that activates PKC (Ki = 3.4 nM and 1 μM for PKCη and PKCγ, respectively); induces differentiation of human embryonic stem cells into pancreatic progenitors.

A membrane-permeable cationic dye that is a substrate for P-gp and is rapidly exported from cells with functional P-gp; also accumulates within mitochondria and can be used to both localize mitochondria and study their properties.

An antibacterial antibiotic that acts by interfering directly with the biosynthesis of peptidoglycan, which constitutes the major component of the bacterial cell wall, leading to structural instability and death of bacteria; used as a selective antibiotic for resistant bacteria.

A synthetic quinine derivative commonly used as an anti-malarial drug; also useful in managing SLE, rheumatoid arthritis, and other diseases; inhibits autophagy and induces autophagic cell death (IC₅₀ = 30 µM).

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.

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).

Cysteine conjugate of benzyl isothiocyanate, N-dimethylnitrosamine demethylase inhibitor. It induces apoptosis in bladder cancer cells and inhibits cell growth in leukemia cells. Grade: ≥98

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.

An apigenin flavone C-glycoside isolated from various tropical plant species that demonstrates broad antioxidant, anti-inflammatory, anticancer, and antinociceptive activities.

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.

A specific, cell-permeable inhibitor of S6K1 (IC₅₀ = 160 nM); does not inhibit S6K2, MSK, or RSK, or many other unrelated kinases, under conditions in which it inhibits S6K1 activity.

An alkaloid metabolite of nicotine as well as a major product of its pyrolysis; binds comparably to CYP2A6 and CYP2A13 (Kis = 7.5 and 5.6 µM, respectively), but appears to more effectively inactivate CYP2A6.

A HSL compound produced in the marine bioluminescence bacterium V. fischeri.

An analog of wortmannin; irreversibly binds PI3K; inhibits recombinant PI3K and mTOR (IC₅₀ = 2.7 and 193 nM, respectively) and prevents the growth of LNCap cells (IC₅₀ = 1.46 μM).

A non-selective, irreversible COX inhibitor with IC₅₀ values of 0.75 and 1.25 mM for ovine COX-1 and COX-2, respectively.

A dual inhibitor of DNA-PK and PI3K.

A synthetic progestin that acts as a prodrug to norelgestromin and levonorgestrel; selectively binds the progesterone receptor and is androgenically neutral.

6-Bromoisoquinoline is a synthetic intermediate useful for pharmaceutical synthesis.

Active metabolite of lactacystin, a widely used selective inhibitor of the 20S proteasome, with at least 10 times better activity; irreversibly alkylates subunit X of the 20S proteasome.

A potent inhibitor of several NHE isoforms, inhibiting NHE1, NHE2, NHE3, and NHE5 with Ki values of 0.02, 0.5, 2.4, and 0.42 μM, respectively; less effectively inhibits NHE4 (IC₅₀ ≥10 μM).

A selective inhibitor of PI3Kα that is equipotent against both wild type and several mutant isoforms (IC₅₀s = 4.0-4.8 nM); dose-dependently inhibits the growth of PI3Kα-dependent xenograft tumors in mice, alone or in combination with other kinase inhibitors.

A synthetic prodrug which is converted to the vitamin D receptor agonist 1,25-dihydroxy vitamin D3 in vivo; suppresses the synthesis and secretion of parathyroid hormone in secondary hyperparathyroidism; supports bone growth; provides renal and cardiovascular protection during chronic kidney disease.

An intermediate in several metabolic pathways, including glycolysis and gluconeogenesis.

An orally-available, highly selective inhibitor of B-RafV600E (IC₅₀ = 13 nM); less effective against wild type B-Raf (IC₅₀ = 160 nM) as well as several other kinases; induces cell cycle arrest and apoptosis in cells and xenografts expressing the mutant of B-Raf.

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).

An inhibitor of class III receptor tyrosine kinases (IC₅₀s = 0.3 µM for c-Fms, c-Kit, ITD-FLT3 and 1 µM for PDGFRβ); blocks the proliferation of leukemia cells stimulated with FLT3 ligand by preventing the activation of STAT5.

A thiazide-like diuretic that targets the Na+-Cl- cotransporter responsible for salt reabsorption in the distal convoluted tubule of the kidney (IC₅₀ = 0.3 µM in rat); inhibits human carbonic anhydrase isoforms VII, XII, and XIII (Kis = 2.1, 5.4, and 15 nM, respectively).

Bromhexine is a synthetic derivative of vasicine that exhibits mucolytic and antioxidative activities. Bromhexine increases production of serous mucus, decreases mucus viscosity, and helps cilia transport mucus out of the lungs. Bromhexine is clinically used to treat respiratory disorders…

A cell permeable analog of cAMP that activates PKA with a Ka value of 0.05 μM; more stable to hydrolysis and has increased membrane permeability compared to unmodified cAMP.