An orally bioavailable, specific, broad spectrum JAK inhibitor (IC₅₀s = 10, 18, 99, and 84 nM for JAK1, JAK2, JAK3, and JAK4, respectively); blocks cell-based JAK signaling induced by IL-2, IL-4, IL-6, IL-13, or IL-31 with IC₅₀ values ranging from 36 to 249 nM.

A non-nucleoside DNA methyltransferase inhibitor (IC₅₀ = 115 nM in vitro) that significantly reduces the methylation of genomic DNA in cells at 10 μM without detectable toxicity.

A plant hormone with diverse roles in disease resistance, plant development, and response to stresses; regulates gene expression and may contribute to epigenetic changes at the chromatin level.

EPA is an ω-3 fatty acid abundantly available in marine organisms. It is a poor substrate for COX-1. EPA has been shown to offer protection against coronary heart disease, thrombosis, ischemic brain injury, scaly dermatitis, and some inflammatory diseases.

CYP1B1 is mainly an extrahepatic enzyme which oxidatively metabolizes both endogenous (steroids; eicosanoids) and exogenous xenobiotics such as polyaromatic hydrocarbons. TMS is a potent and selective inhibitor of CYP1B1, with an IC50 of 6 nM. It is 50-fold selective for the inhibition of CYP1B1…

A cell-impermeable, negatively charged tetrazolium dye that produces a water-soluble formazan when reduced at the cell surface by cellular-derived NADH and an electron mediator.

A cell permeable, competitive inhibitor of HIF-PH with effective concentrations in the low µM range.

An inhibitor of SREBP activation, preventing SCAP-mediated escort of either SREBP-1 or SREBP-2 to the Golgi (IC₅₀ = 5.6 µM); blocks SREBP-mediated gene expression; inhibits high glucose-induced upregulation of TGF-β in primary rat mesangial cells; reduces hepatic fat…

A selective non-peptide inhibitor of CXCR2, inhibiting IL-8 binding to CXCR2 (IC₅₀ = 22 nM).

An antibacterial and coccidiostat compound that shows selective toxicity for HMLER breast cancer stem cells (IC₅₀ = ~24 μM); 8 μM treatment of 4T1 and MCF-7-Ras breast cancer cell lines decreases cancer stem cell growth ~2-fold and ~3-fold, respectively; 5 mg/kg inhibits mammary…

An analytical reference standard categorized as a phytocannabinoid; intended for research and forensic applications

A semisynthetic analog of taxol that inhibits microtubule disassembly (IC50 = 0.2 μM) and inhibits cell replication (IC50 = 0.13 μM); has applications in breast cancer and hormone-refractory prostate cancer; intended for research applications.

A potent uncoupler of oxidative phosphorylation in mitochondria that disrupts ATP synthesis by transporting protons across cell membranes.

A selective allosteric inhibitor of Bcr-Abl (IC₅₀s = 4.52, 0.38, and 0.93 µM against Bcr-Abl mutants G250E, E255V, and M351T, respectively); displays additive inhibitory activity against T315I Bcr-Abl mutants both in in vitro assays and in a recalcitrant T315I Bcr-Abl mutant mouse…

An N-acylethanolamide that inhibits dietary-restriction-induced lifespan extension in wild type and TOR pathway mutant nematodes; also has anti-inflammatory properties, suppressing the expression of IL-6 and MCP-1 in 3T3-L1 adipocytes in response to lipopolysaccharide.

An ATP-competitive inhibitor of JAK1 and JAK2 (IC₅₀s = 11 and 18 nM, respectively); causes growth suppression and apoptosis in JAK2-dependent hematopoietic cell lines; is efficacious in a mouse model of JAK2V617F-dependent myeloproliferative neoplasms.

A succinimide that is converted to N-desmethylmethosuximide, a channel blocker that targets low threshold calcium currents; inhibits CYP2C19-mediated metabolism of biguanides; has anticonvulsant properties in clinical trials.

A potent inhibitor of the CK1 isoforms CK1ε and CK1δ (IC₅₀ = 7.7 and 14 nM, respectively); less effectively inhibits a wide variety of related or common kinases; disrupts circadian rhythms in cells and animals; blocks the locomotor response to amphetamines in mice.

An inhibitor of p53-HDM-2 interaction that can reactivate the tumor suppressor function of wild-type p53; binds to p53 with an apparent Kd value of 1.5 nM and prevents interaction with HDM-2 resulting in p53 stabilization, accumulation, and activation.

A potent inhibitor that blocks dopamine uptake (IC₅₀ = 1-51 nM); effectively inhibits dopamine uptake in vivo, leading to consequent stimulation of dopamine receptors.

AMC-AA is one of several fatty acid amides which can be used to measure FAAH activity. Exposure of AMC-AA to FAAH results in the release of the fluorescent aminomethyl coumarin that absorbs at 360 nm and emits at 465 nm, allowing for fast and convenient measurement of FAAH activity using a simple…

An anti-inflammatory compound from the diaryl heterocycle class that selectively inhibits COX-2 (IC50s = 22.9 and 0.05 μM for COX-1 and COX-2, respectively; displays chemopreventive activity in multiple tumor types via proapoptotic effects independent of its capacity to block COX-2.

A benzothiadiazide that acts as a potentiator of AMPA receptors, positively modulating its response to glutamic acid (EC₅₀ = 3.8 µM); also a negative modulator of GABAA receptors, reversibly inhibiting both evoked and spontaneous inhibitory postsynaptic currents (IC₅₀ =…

WS3 is a non-specific proliferative molecule that modulates the activity of Erb3 binding protein-1 and the IκB kinase pathway. It has been used to mediate proliferation of primary retinal pigment epithelial cells ex vivo in order to provide a renewable source of cells for transplantation in a…

A homoserine lactone member that possesses a rare odd-numbered acyl carbon chain and may be a minor quorum-sensing signaling molecule in P. aeruginosa strains.

Zileuton (Zyflo™) is a reversible 5-LO inhibitor that was approved in 1997 for the prevention and treatment of asthma in the USA, but was withdrawn by Abbott Laboratories in 2003. Zileuton inhibits 5-LO from rat basophilic leukemia-1 (RBL-1) cells with an IC50 value of 0.5 µM. It is a…

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…

An analog of AEA that potentiates the activity of endogenous AEA by blocking its re-uptake into presynaptic neurons; selectively inhibits the carrier-mediated transport of AEA without affecting anandamide hydrolysis; inhibits the transport of AEA with an IC₅₀ value of 1 µM in rat…

An intravenous β-lactam antibiotic that is effective against Gram-positive and Gram-negative bacteria (MICs range from 0.008-0.13 µg/ml); highly resistant to degradation by β-lactamases.

A proapoptotic, antiproliferative compound that is able to arrest cell cycle progression in the G0-G1 phase; inhibits the growth of HL60, multidrug resistant HL60R, and K562 cells with IC50 values of 7.0, 23, and 20 µM, respectively.

A selective, ATP-competitive inhibitor of Cdk9, 2, and 7 with IC₅₀ values of 4, 38, and 62 nM, respectively; blocks the cell cycle, inhibits transcription, and induces apoptosis in multiple myeloma RPMI-8226 cells with an IC₉₀ value of 0.3 µM.

A reversible inhibitor of the H2S synthesizing enzyme cystathionine-γ-lyase; blocks H2S synthesis in rat liver preparations with an IC50 value of 6.5 µM.