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).

A primary amide analog of (+)-JQ1 which has shown superior bioavailability with oral or i.p. administration; inhibits BRD4 binding and action in vitro or in cells; arrests the growth of leukemia T cells in vitro (EC₅₀ = 91 nM) and rapidly suppresses leukemia burden in mice.

An endogenous, maturation-inducing steroid that at 1 µg/ml induces germinal vesicle breakdown in oocytes from several teleost species; can also influence spermiation by stimulating milt production when administered at 5 mg/kg to various male teleosts.

A mixture of oligomycins A, B, and C

A potent lipid signaling molecule that exhibits a wide range of biological activities; it enhances cell growth and inhibits the normal apoptotic response to a variety of stimuli.

A selective, short-acting adenosine A2A receptor agonist (Ki = 1.1 nM for pig striatum A2A receptor); used to induce hyperemia, particularly in the context of myocardial perfusion imaging.

A dual inhibitor of COX and LOX pathways, that decreases levels of PGE2, LTB4, and lipoxins and prevents LPS-stimulated IL-1β expression.

Unoprostone isopropyl ester (Rescula) is the clinically approved, prodrug form of unoprostone, which is a free acid analog of PGF2α. Both latanoprost and Rescula have been approved for the treatment of ocular hypertension. Both analogs of PGF2α are believed to act by increasing the rate…

A cell-permeable inhibitor of HIF-1-mediated gene transcription which acts by intercalating into DNA in a sequence-specific manner, blocking the binding of either HIF-1α or HIF-1β to the HRE; reversibly inhibits hypoxia-induced HIF-1 transcription activity in U215 cells with an EC50…

A selective inhibitor of ASK1 (IC₅₀ = 3 μM; Ki = 500 nM); promotes survival of induced pluripotent stem cell populations and protects neurons from reactive oxygen species-induced apoptosis in a model of ischemia.

A water-soluble receptor antagonist which targets both AMPA- and kainate-sensitive glutamate receptors (IC₅₀ = 0.15 and 4.8 µM, respectively); does not block the NMDA-sensitive glutamate receptor (IC₅₀ = ≥ 90 µM).

A potent ER antagonist that works by both down-regulating and degrading ERα; efficacious in the treatment of estrogen-sensitive breast cancer; fully activates ER on hippocampal neurons.

An antagonist of the interaction between survivin and the apoptosis-promoting protein Smac/DIABLO with an IC₅₀ value of 2.2 µM; sensitizes cells to apoptotic stimuli.

A natural yellow carotenoid, which can be found in plants, egg yolks, and in the human retina; a lipid-soluble antioxidant that can circulate in the plasma and confer cardioprotective, anti-inflammatory, and anti-angiogenic effects.

A potent, reversible, and cell permeable proteasome inhibitor; inhibits cell growth in B16 and IPC227F cells with IC50 values of 42 and 77 nM, respectively; inhibits NF-κB activation, sensitizing a variety of carcinoma cell lines to apoptosis.

An anthracycline antitumor antibiotic agent that inhibits DNA topoisomerase II by inducing double-stranded DNA breaks; inhibits nucleic acid synthesis and induces apoptosis by intercalating within DNA.

A competitive inhibitor of nucleotide binding by Ras-related GTPases; binds Rab7 (Ki = 13 nM), preventing BODIPY-linked GTP and GDP binding with EC₅₀ values of 11.2 and 21 nM, respectively.

A panaxadiol that has diverse in vitro and in vivo effects, including anti-cancer, neuroprotective, anti-hypertensive, and anti-inflammatory actions; induces apoptosis and inhibits angiogenesis in a variety of cancer models.

A selective, cell permeable inhibitor of CaMKII (IC₅₀ = 900 nM).

A selective, cell-permeable EZH2 inhibitor (IC₅₀ = 2 nM) that has been shown to inhibit H3K27methylation in MCF10A cells with an IC₅₀ value of 124 nM.

An irreversible inhibitor of the chymotrypsin-like β5 subunit of the constitutive 20S proteasome (IC₅₀ = 5.2 nM) and the β5i subunit of the immunoproteasome 20Si (LMP7; IC₅₀ = 14 nM) with minimal cross reactivity to other proteases; induces cell cycle arrest and…

A potent, reversible, orally bioavailable inhibitor of Pim-1, -2, and -3 (IC₅₀s = 5, 25, and 16 nM, respectively); dose-dependently blocks the phosphorylation of the Pim targets Bad, 4E-BP1, and NKX3.1; acts synergistically with chemotherapeutic drugs.

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 sulfated form of taurocholic acid that may be involved in the elimination and detoxification of bile acids during hepatobiliary diseases.

GSK3β Inhibitor II is a potent inhibitor of glycogen synthase kinase-3β (GSK3β; IC₅₀ = 390 nM) that does not inhibit GSK-3α. Also referred to as tip-oxadiazole, this compound blocks the functional regulation of p53 by GSK3β, decreasing levels of MDM2, p21, and…

A potent and selective inhibitor of the TGF-β1 receptor ALK5 (IC₅₀ = 94 nM), ALK4 (IC₅₀ = 140 nM) and, less effectively, ALK7; suppresses renewal in embryonic and induced pluripotent stem cells and promotes their differentiation.

A selective, irreversible inhibitor of IL-1b converting enzyme (ICE; Caspase-1); neuroprotective in a rat model of cerebral ischemia.

A sulfonyl hydrazide that inhibits BCATc (IC₅₀s = 0.81 and 0.2 µM in human and rat, respectively) with 15-fold selectivity over BCATm; blocks calcium influx into neurons (IC₅₀ = 4.8 µM) following inhibition of glutamate uptake and demonstrates neuroprotective…

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.

A cell-permeable carbazolic compound which directly interacts with and stabilizes CRY1 and CRY2, preventing ubiquitin-dependent degradation while lengthening the circadian period (IC₅₀ = 0.82-14 μM); inhibits glucagon-induced gluconeogenesis in primary hepatocytes.

A sulfated bile acid that is used to induce pancreatic acinar cell injury in models of pancreatitis and to study bile acid transport.

A selective CaMKII inhibitor (IC₅₀ = 40 nM) that was designed based on the sequence around the autophosphorylation site (Thr286/Thr287) in the autoinhibitory domain of the protein kinase.