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.

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 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 NSAID that inhibits COX-1 and -2 activity with IC₅₀ values of 17.4 and 13.1 µM, respectively.

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 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 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 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 potent, competitive inhibitor of HO activity in vitro (Ki = 14 nM); inhibits hepatic, renal, and splenic HO activity in vivo for extended periods of time; blocks bilirubin production in vivo, decreasing HO activity in animal models of hyperbilirubinemia.

An abundant oligosaccharide in the milk of many mammals, including cows and humans, particularly postpartum; avidly binds several viral strains, including strains of influenza, HIV-1, reovirus, and polyomavirus, in some cases altering viral infectivity.

A small molecule pan activator of Ras-related GTPases, activating cdc42, Ras, and Rac1 with EC₅₀ values of 102, 109, and 151 nM, respectively.

A nonaminoglycoside that has been reported to selectively induce ribosomes to read through premature nonsense stop signals on mRNA, thus allowing the production of full-length, functional proteins (IC₅₀ = 7 nM); 60 mg/kg s.c. injection or 0.3-0.9 mg/ml orally has been shown to restore…

Functions as a potent laxative by inducing chloride secretion in colonic mucosa and releasing acetylcholine, which stimulates contraction of intestinal smooth muscle; also demonstrates anti-tumor activity (ED50s = 1-13 µM), inducing apoptosis in various cancer cells.

ICI 192605 is a potent antagonist of the thromboxane A₂ receptor (TP) that blocks contraction of isolated guinea pig trachea induced by U-46619 (Item No. 16450; K_d = 0.398 nM). It is used to study the role of TP signaling in tissues and animals.

A potent LTB4 receptor antagonist that inhibits the specific binding of [3H]-LTB4 to isolated human neutrophils with an IC50 value of 13.2 nM; inhibits the LTB4-induced aggregation of guinea pig and human neutrophils with IC50 values of 74 and 100 nM, respectively.

An orally active inhibitor of PI3Kg that suppresses joint inflammation in mouse models of rheumatoid arthritis; inhibits human recombinant PI3Kg, a, b, and d in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.

A reversible inhibitor of Lp-PLA2 (IC₅₀ = 0.25 nM) that produces sustained inhibition of plasma Lp-PLA2 activity in humans.

A potent inhibitor of the Wnt response, blocking a cell-based Wnt/β-catenin pathway reporter response (IC₅₀ = 180 nM); inhibits Wnt-induced accumulation of β-catenin, leading to proteasomal degradation of this protein.

A selective, orally available inhibitor of MEK1 (IC₅₀ = 4.2 nM); induces differentiation and apoptosis in cancer cells lines.

A stable, monomethoxylated resveratrol derivative that at 0.1-10 μM reduces neurotoxicity in SH-SY5Y cells induced by the parkinsonian mimetic 6-OHDA and scavenges DPPH radicals (IC₅₀ = 47.1 μM).

A cell-permeable inhibitor of SCF-mediated c-kit activation, completely blocking phosphorylation of c-kit in human melanoma cells at a concentration between 1 and 5 µM; prevents SCF-mediated downstream phosphorylation of p44/p42 ERK.

A selective inhibitor of BAZ2A (Kd = 109 nM; IC₅₀ = 130 nM) and BAZ2B (Kd = 170 nM; IC₅₀ = 180 nM) bromodomains.

An aminopyrimidine derivative that inhibits GSK3α and GSK3β (IC50s = 10 and 6.7 nM, respectively); activates glycogen synthesis in CHO-IR cells (EC50 = 0.8 μM) and in isolated type 1 diabetic rat skeletal muscle; has been shown to promote self-renewal of embryonic stem cells.

A noncompetitive nicotinic acetylcholine receptor antagonist with preferential activity at the α3β4 subtype (IC₅₀ = 90-640 nM) compared to α4β2, α3β2, and α7 subtypes (IC₅₀s range from 1-7 μM).

An unsaturated fatty acid found in royal jelly produced from honeybees; demonstrates longevity-promoting effects in C. elegans, down regulates matrix metalloproteinases (MMPs) in rheumatoid arthritis, inhibits VEGF-induced angiogenesis in HUVECs, facilitates differentiation of neurons from neural…