A steroidal saponin that displays cytotoxicity against a range of cancer cells in vitro, including leukemia, colon cancer, and prostate cancer cells (GI50 ≤ 2 µM).

An antitumor antibiotic that crosslinks double stranded DNA and is widely used as a tool to selectively inhibit DNA synthesis and mutagenensis, to stimulate genetic recombination, chromosome breakage and sister chromatid exchange, and to induce DNA repair.

A selective L-type calcium channel blocker with long-acting antihypertensive activity; relaxes depolarization-induced contractions of rabbit aorta (EC₅₀ = 1.4 nM) and reduces the rate of spontaneously beating guinea pig right atria (EC₂₅ = 0.45 nM); attenuates β-amyloid…

An isomer of 17-phenyl trinor PGF2α, characterized by an inverted (β) hydroxyl group at C-15.

GSK2578215A is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC₅₀ = 8.9 nM) that also inhibits the G2019S mutant of LRRK2 (IC₅₀ = 10.1 nM). It displays selectivity for LRRK2 over a panel of 460 other kinases. GSK2578215A prevents phosphorylation of both wild-type…

A naturally occurring diterpene that directly activates adenylyl cyclase to raise levels of cAMP in a wide variety of cell types; binds to type 1 adenylyl cyclase membranes with an IC50 value of 41 nM and demonstrates an EC50 value of 0.5 μM in an activation assay.

A purine nucleoside analog that irreversibly inhibits adenosine deaminase (Ki = 0.9 pM) and thus interrupts DNA synthesis in dividing cells; displays strong efficacy in the clinical treatment of hairy cell leukemia as well as relapsed chronic lymphocytic leukemia.

NVP-TAE226 is an inhibitor of focal adhesion kinase (FAK; IC₅₀ = 5.5 nM) and the related proline-rich tyrosine kinase 2-β (PYK2β; IC₅₀ = 5 nM). It can also inhibit the insulin-like growth factor 1 receptor (IC₅₀ = 0.16 µM) as well as the activity of…

A selective inhibitor of RNA polymerase I-driven transcription of rRNA (IC₅₀s = 142, 113, and 54 nM in HCT116, A375, and MIA PaCa-2 tumor cells, respectively); demonstrates in vivo antitumor activity against human solid tumors in mouse xenograft models.

A plant alkaloid that demonstrates cytotoxicity against leukemia P-388 cells (IC₅₀ = 2.3 µM) through a mechanism that involves stabilizing the DNA topoisomerase I-DNA complex.

A naturally occurring metabolite of bile acid that is produced by the conjugation of cholic acid and sulfate, predominantly in the liver and gut.

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 natural sesquiterpene lactone that reduces growth (EC₅₀ = 3-35 μM) and induces apoptosis in assorted cancer cell lines; inhibits the activation of Akt (15 μM) in endometriotic epithelial cells and STAT3 activation in THP-1 cells (EC₅₀ = 10 μM); inhibits telomerase…

Activates the aryl hydrocarbon receptor (Ki = 5.4 µM), inducing the expression of both detoxifying enzymes, resulting in pyocyanin degradation, and cytokines that facilitate the clearance of bacteria; accelerates neutrophil apoptosis, resulting in resolution of acute inflammation.

A chromogenic substrate for N-acetyl-D-galactosaminidase that generates a yellow solution upon cleavage.

A plant growth regulator that activates various signal transduction pathways with both growth promoting and inhibitory functions, perhaps in response to stress; initially synthesized as (+)7-epi jasmonic acid, a more active and biologically relevant form of the hormone, but quickly epimerizes to…

An inhibitor of PDGF-BB tyrosine kinase with an IC50 value of 4.2 nM when tested in human coronary artery smooth muscle cells.

D-erythro-Sphinganine is a precursor of ceramide and sphingosine as well as a substrate of sphingosine kinases, which generate sphinganine-1-phosphate. Sphinganine levels increase significantly in response to certain mycotoxins, including fumonisins, as well as in some cancers. Sphinganine can…

A reversible inhibitor of the cis-Golgi ArfGEF, GBF1 (IC₅₀ = 3.3 µM); induces rapid dissociation of COPI vesicle coat protein from Golgi membranes and disassembly of the Golgi and trans-Golgi network, preventing bidirectional transport of endocytic cargo.

A major milk oligosaccharides that avidly bind several viral strains, including strains of influenza, HIV-1, reovirus, and polyomavirus; used to differentiate and characterize the binding domains of viruses that recognize N-acetylneuraminic acid-capped cell surface receptors; also used as an…

A cell-permeable, competitive, and irreversible inhibitor of all caspases, inhibiting cleavage of PARP and preventing apoptosis when used at 10-50 µM; blocks caspase-mediated apoptosis in vivo; effectively prevents caspase action in inflammasomes.

A potent and selective EP1 receptor antagonist (IC₅₀ = 2.5 nM), with >400-fold selectivity relative to EP2, EP3, EP4, DP1, and IP; has 30-fold selectivity over TP; shows complete anti-hyperalgesic activity in a rat model of chronic inflammatory joint pain.

A potent, bioavailable JAK inhibitor with preference for JAK2 (IC₅₀ = 2 nM) over JAK1 and JAK3 (IC₅₀s = 130 and 250 nM, respectively); effective against JAK2V617F as well as JAK2 and inhibits phosphorylation of STAT5 in vivo.

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…

Linolein hydroperoxides are a mixture of 132 possible isomers of mono-, di-, and tri-hydroperoxides produced from the autoxidation of trilinolein. Autoxidation of linoleic acid containing triglycerides (for example, trilinolein) in vivo could result in the formation of these hydroperoxides. Unlike…

A dipeptide boronic acid derivative that reversibly inhibits the 20S proteasome (Ki = 0.6 nM); drives cell cycle arrest and apoptosis in cancer cell lines and has applications in multiple myeloma and certain lymphomas, as well as other types of cancer.

A selective inhibitor of 15-hydroxy PGDH (IC₅₀ = ~10 µM).

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…

A cardiotonic steroid that inhibits theNa+/K+-ATPase transporter (Kds = 42, 45, and 40 nM for the α1, α2, and α3 subunits, respectively); inhibits SRC-1 and SRC-3 at doses as low as 5 nM, promotes the degradation of SRC-3 protein, and inhibits cancer cell growth both in vitro and…

An inhibitor of EGFR and VEGFR tyrosine kinases (IC₅₀s = 2, 6, 77, and 59 nM for EGFR, ErbB2, KDR, and FLT1, respectively); demonstrates antitumor activity and anti-angiogenic activity in numerous in vitro and in vivo models.

A rotenoid compound with chemopreventive and chemosensitizing effects in models of skin, mammary, colon, and lung carcinogenesis; inhibits cell growth (IC50 = 8 M), blocks PI3K/Akt signaling, suppresses COX-2 expression, and induces apoptosis of premalignant and squamous HBE cells without affecting…

A calcimimetic compound that can allosterically activate or positively modulate the human CaSR; dose-dependently decreases circulating levels of PTH in both normal individuals and patients with primary hyperparathyroidism in clinical trials.