3-HPA is an analog of AM404, which is a selective inhibitor of carrier-mediated transport of AEA. 3-HPA is metabolized by both COX-1 and COX-2 and also selectively and irreversibly inhibits COX-2 with an IC50 value of 2 µM.

A potent inhibitor of PDE5 (IC50 = 1-5 nM) that also blocks the activity of PDE11 (IC50 = 10-33 nM); IC50 values against other isoforms of PDE are in the micromolar range; pharmacokinetics are highlighted by its prolonged duration of effect.

Carboxy-PTIO is a NO scavenger. It reacts stoichiometrically with NO and can be used for EPR detection of NO.

A potent, selective, and bioavailable inhibitor of the TRPA1 channel, with IC₅₀ values of 67 and 289 nM for the human and rat isoforms, respectively; attenuates cold allodynia following nerve injury and suppresses neuronal activity in response to mechanical stimulation.

5-Bromotetralone is a synthetic intermediate useful for pharmaceutical synthesis.

An activator of the HIF signaling pathway, as demonstrated by HRE reporter assay (EC₅₀ = 1.2 µM), HIF-1α nuclear translocation assay (EC₅₀ = 1.3 µM), and increased VEGF expression (EC₅₀ = 1.6 µM); activity is blocked by excess iron,…

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.

An orally active, selective inhibitor of p38α and p38β (IC₅₀s = 1 and 11 µM, respectively, in vitro); blocks the release of TNF-α and IL-1β from peripheral blood mononuclear cells stimulated with LPS (IC₅₀s = 3 and 11 nM, respectively) and inhibits…

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 full antagonist of RXR that demonstrates potent, nanomolar binding affinity; does not affect the corepressor interaction capacity of the RARα subunit in the RAR-RXR heterodimer configuration.

A broad-spectrum antibiotic that inhibits protein synthesis by inducing miscoding; commonly used as a dominant selection antibiotic for genetically modified bacteria, yeasts, fungi, protozoa, plants, and mammalian cells.

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…

An analog of dapagliflozin that displays similar selectivity for inhibiting SGLT2 over SGLT1 (Kis = 5.3 and 330 nM, respectively); significantly reduces phlorizin-sensitive sugar transport in COS-1 cells expressing human SGLT2.

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…

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.

One of the phenolic antioxidants present in extracts of rosemary; inhibits the formation of tumors derived using irritants such as TPA and DMBA.

A substrate for the synthesis of RNA during the transcription process and the synthesis of DNA during DNA replication; participates in G-protein-related signal transduction where it is converted to GDP through the action of GTPases.

A reversible inhibitor of cysteine, serine, and threonine proteases; inhibits cathepsin B (Ki = 6 nM), calpain (Ki = 10 nM), trypsin (Ki = 35 nM), plasmin (Ki = 3.4 μM), and kallikrein (Ki = 19 μM), and has no effect against chymotrypsin, elastase, renin, or pepsin.

ACAT is an intracellular cholesteryl ester synthase tied closely to the absorption of dietary cholesterol. Oleic acid-2,6-diisopropylanilide is an inhibitor of ACAT with an IC50 of 7 nM. When co-administered to rabbits or rats fed a high fat, high cholesterol diet, oleic acid-2,6-diisopropylanilide…

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.

A potent, selective antagonist of the H1 histamine receptor (Ki = 16-41.1 nM), with much lower affinities for the H2 and H3 receptors (Ki = 43.4 and 172 μM, respectively); effective in treating allergic rhinitis and conjunctivitis; does not cause cognitive or psychomotor impairment at…

An intermediate in the biosynthesis of NAD+ that has been used to enhance NAD biosynthesis and glucose-stimulated insulin secretion in Nampt+/- mice and high-fat diet-induced type 2 diabetes mice.

An inhibitor of HDAC, including HDAC1 (IC₅₀ = 0.1-0.2 μM); induces growth suppression and cell death of certain types of cancer cells in culture.

The ethanolamine amide of DHA that has been detected in both brain and retina at concentrations similar to those for AEA; binds to the rat brain CB1 receptor (Ki = 324 nM), which is approximately 10-fold higher than the Ki for AEA; inhibits shaker-related voltage-gated potassium channels in brain…

An activated fluorescent molecule (excitation: 494 nm, emission: 519 nm) used for labeling proteins; reacts optimally with sulfhydryl groups on cysteine side chains at pH 7, forming a stable thioether bond.

An agonist of dopamine D1A (D1R) and D1B (D5R) receptors (Kds = 17 and 11 nM, respectively); alters hemodynamic properties, including hypertension, in animals.

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.

The major metabolite of the gastric proton pump inhibitor, omeprazole; produced by CYP3A4 sulfoxidation of esomeprazole.

Selectively and reversibly blocks MAGL activity (IC₅₀s = 0.18 and 59 µM for MAGL and FAAH in mouse brain, respectively); does not inhibit ABHD6, ABHD12, CB1, or CB2 receptors (Kis > 10 µM); used to ameliorate disease progression in a mouse model of multiple sclerosis.

A small molecule that stimulates the expression of PGC-1α and downstream genes in skeletal muscle cells, improving glucose utilization and fatty acid oxidation at a concentration of 20 μM; 15 mg/kg/day administered to diabetic db/db mice improved glucose tolerance, pyruvate tolerance, and…

A brain-penetrant inhibitor of CSF1R, as well as c-Kit and FLT3 (IC₅₀s = 20, 10, and 160 nM in vitro, respectively); blocks macrophage recruitment in mammary tumor-bearing mice and blocks glioblastoma invasion in both cell culture and a mouse model of glioblastoma multiforme.

Inhibits Gli1-mediated transcription (EC₅₀ = 5 μM) in a variety of cell types disrupting the hh signaling pathway downstream of Smo and Sufu; displays antiproliferative and antitumor activity against Ewing sarcoma family of tumor cells.