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.

A nitroimidazole with radiosensitizing and antineoplastic properties; metabolites accumulate in hypoxic cells and can themselves be cytotoxic or they can increase the chemosensitivity and radiosensitivity of the target cells; used in the imaging of hypoxic regions in tumors and in the…

ALA is an essential fatty acid found in leafy green vegetables. ALA, as part of a low saturated fat diet, helps prevent cardiovascular disease. ALA decreases blood pressure, serum cholesterol levels, and platelet aggregation.

DepNA is one of several nitroaniline fatty acid amides which can be used to measure FAAH activity.{8928} FAAH is a relatively unselective enzyme in that it accepts a variety of amide head groups other than the ethanolamine of its endogenous substrate AEA. It also will hydrolyze fatty acid amides…

N-4AIA is one of several aromatic amides of indomethacin reported to be potent and selective reversible inhibitors of COX-2. N-4AIA inhibits human recombinant and ovine COX-2 with IC₅₀ values of 0.1 and 0.625 µM, respectively. It is about 80 times less potent as an inhibitor of…

A potent inhibitor of all three human Pim kinases (IC₅₀s = 7, 363, and 69 nM for Pim-1, Pim-2, and Pim-3, respectively); induces apoptosis in lymphocytes from patients with CML or ALL; enhances the activity of sunitinib against renal cell carcinoma and resensitizes chemoresistant cancer…

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…

A substrate of cathepsin C that accumulates inside lysosomes causing lysosome degradation; 50 μM can inhibit the cathepsin-dependent activation of caspase-8.

An indole-based SERM that binds to both ERα (IC₅₀ = 26 nM) and ERβ (IC₅₀ = 99 nM); antagonizes 17β-estradiol-dependent and hormone-independent growth of breast cancer cell proliferation (80% reduction with 10 nM) in a manner related to cell cycle arrest and…

An ATP/GTP-competitive inhibitor of CK2 (IC₅₀ = 900 µM for rat liver CK2); less potently inhibits CCK2/cyclin A, GSK3β, and phosphorylase kinase (IC₅₀ = 15.6, 11.2, and 8.7 mM, respectively); much less effective against a range of other kinases.

A cell permeable drug that inhibits cholesterol trafficking from late endosomes/lysosomes to the ER, but not to the plasma membrane.

N-Oleoyl glycine is a putative substrate for peptidyl glycine α-amidating enzyme in the biosynthesis of oleoyl amide.

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…

A metabolite of vitamin A that acts as a ligand for both the RAR and the RXR.

An elongation product of γ-linolenic acid (18:3), rapidly metabolized by fatty acid desaturases to produce arachidonic acid (20:4); metabolized through the cyclooxygenase pathway to produce 1-series prostaglandins; can reduce atopic dermatitis and atherosclerosis when added to the diet of mice.

A second generation antiepileptic compound used to prevent convulsions in a variety of settings; binds the synaptic vesicle protein SV2A (pIC₅₀ = 5.7), presumably altering vesicle exocytosis; alters the metabolism and turnover of GABA.

A fluorescent indicator of peroxynitrite formation; neither NO, superoxide, nor hydrogen peroxide alone appear to oxidize DCFH.

An intermediate in the generation of adenine and methionine that is produced by the decarboxylation of SAM; a potent agonist of adenosine receptors (Kis = 0.15, 1.13, 13.9, and 0.68 μM for A1, A2A, A2B, and A3, respectively); inhibits several enzymes at higher concentrations.

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.

Molecular Formula: C₅₇H₉₂O₆ Formula Weight: 873.4

A selective, irreversible inhibitor of BTK (IC₅₀ = 0.5 nM in vitro in B cell lymphoma cell lines) that targets and covalently binds to BTK at cysteine-481; inhibits osteoclast function and reduces osteoclast-stimulated proliferation of multiple myeloma cells in animal models of…

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 selective agonist of S1P3 (EC₅₀ = 72-132 nM); less effectively activates S1P1 (EC₅₀ = 28-38 µM) and is ineffective at S1P2, S1P4, and S1P5 as well as a panel of other receptors, ion channels and transporters.

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 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 =…

A fluorescent probe commonly used to identify dead cells; excitation at 488-535 nm and emission maximum of 617 nm.

A hybrid molecule of indomethacin and an NO donor which combines the anti-inflammatory properties of an NSAID with the gastrointestinal protective effects of NO.

A cell-permeable, selective inhibitor of N-WASP (IC₅₀ = ~ 10 μM); directly associates with the GTPase-binding domain of N-WASP, preventing its activation by Cdc42 and PIP2; interferes with membrane transport, endocytosis, and neurological development.

A non-nucleoside reverse transcriptase inhibitor that binds to viral reverse transcriptase and blocks polymerase activity by preventing RNA plus-strand initiation (IC₅₀s = ~ 0.45 to 0.9 μM).

A blocker of KCNQ channels that potently inhibits KCNQ1 and 2 homomeric channels (IC₅₀ = 0.75 and 0.71 µM, respectively) as well as KCNQ2+3 heteromultimers (IC₅₀ = 0.6 µM); shows good in vivo potency and duration of action.

A nitrogen mustard β-chloro-nitrosourea compound used as an alkylating agent to form interstrand crosslinks in DNA, which leads to cancer cell cytotoxity and apoptosis; also reported to inhibit glutathione reductase, thioredoxin reductase, and lipoamide dehydrogenase.

A potent inhibitor of serotonin and norepinephrine reuptake (Kis = 4.6 and 15.6 nM, respectively, for rat synaptosomes); less effectively inhibits dopamine reuptake (Ki = 369 nM); effective in cells, tissues, and in vivo.