A potent MAO inhibitor that preferentially targets MAO-A over MAO-B (Kis = 0.054 and 58 µM, respectively); also inhibits the sigma receptor σ1 on Jurkat human T lymphocyte cells (IC₅₀ = 31 nM).

An NSAID commonly used in animals to combat pain and inflammation, particularly as associated with osteoarthritis; inhibits both COX-1 and COX-2 (IC₅₀s = 22.3 and 3.9 µM, respectively) and also FAAH (IC₅₀ = 74 µM).

An amino-amide anesthetic that binds to the intracellular portion of voltage-gated sodium channels and blocks sodium influx into nerve cells, preventing the generation of an action potential; inhibits the uptake of dopamine in striatal synaptosomes by 47% at 100 µM.

An intermediate in the pathway leading to the production of 1,25-dihydroxy vitamin D3; plasma or serum levels are commonly used as an indicator of an individual’s vitamin D status.

Calcitriol is synthesized from 7-dehydrocholesterol in humans via a non-enzymatic photochemical reaction with 290-310 nm UV light in the skin. Hydroxylation of the resulting cholecalciferol in the liver produces 25-hydroxy Vitamin D3, the principal circulating form of Vitamin D. A second, tightly…

An inhibitor of protein synthesis in eukaryotes (IC₅₀ = 5-50 μM) that functions by interfering with translational elongation; can either induce or inhibit apoptosis depending on cell type.

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 synthetic prodrug which is converted to the vitamin D receptor agonist 1,25-dihydroxy vitamin D3 in vivo; suppresses the synthesis and secretion of parathyroid hormone in secondary hyperparathyroidism; supports bone growth; provides renal and cardiovascular protection during chronic kidney disease.

A triazole, antifungal agent that inhibits a broad range of pathogenic yeasts, including Candida (MIC = 0.03-8 µg/ml), and filamentous fungi such as Aspergillus, Scedosporium, and Fusarium by disrupting ergosterol synthesis.

A colchicine derivative that inhibits tubulin polymerization (IC₅₀ = 2.1 μM) with low toxicity; suppresses microtubule dynamicity, inhibits cell migration, blocks microtubule assembly, and arrests cells in metaphase; used to synchronize cells and for karyotyping in cytogenetic studies.

A cyanobacterial toxin that targets protein and glutathione synthesis in hepatocytes (IC50s = 1.3 and 2.4 µM, respectively), inhibits uridine monophosphate synthase complex activity (Ki = 10 µM), and induces DNA damage.

A natural fungal metabolite which reversibly interferes with protein trafficking and secretion mediated by the Golgi apparatus and endoplasmic reticulum; directly and reversibly inhibits Sec7 domain-containing GEFs which are necessary for Arf activation associated with vesicular transport (IC50 =…

A cyclododecadepsipeptide potassium-selective ionophore antibotic; induces apoptosis in several cell tyes, including CHO cells, by stimulating potassium efflux.

A DNA alkylating agents that induces DNA interstrand and intrastrand crosslinks, cytotoxicity, and apoptosis; inhibits the growth of PC-3 prostate cancer cells with IC₅₀ values of 0.074 or 0.77 μM for sequential dosing or single dosing, respectively.

A dipyridinyl compound that demonstrates high in vitro and ex vivo selectivity for COX-2 over COX-1.

An agonist of α2 adrenergic receptors (Ki = 194 nM); used for sedation, anesthesia, and analgesia in non-human mammals.

A neuroexcitatory amino acid that functions as a NMDA and metabotropic glutamate receptor agonist; used to induce brain lesions in animal models of cognitive dysfunction.

A non-selective COX inhibitor with IC₅₀ values for ovine COX-1 and -2 of 0.1 and 6 µM, respectively; IC₅₀ values for human recombinant COX-1 and -2 are 1.67 and 24.6 µM, respectively.

A potent, selective antagonist of TRPV4 channels, blocking the influx of calcium induced by the TRPV4 agonist GSK634775 with IC₅₀ values of 2, 5, and 40 nM for rat, mouse, and human isoforms, respectively; effective in vivo, as it resolves pulmonary edema resulting from myocardial…

A small molecule inhibitor of tankyrase 1 and 2 (IC₅₀ = 11 and 4 nM, respectively); increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin; inhibits colony formation of APC-deficient colorectal cancer cells at 0.33 µM.

Intended for use as an internal standard for the quantification of diclofenac by GC- or LC-MS.

A polypeptide antibiotic effective against Gram-negative bacteria, including P. aeruginosa, A. baumannii, and K. pneumoniae.

A thio analog of the purine base guanine that incorporates into DNA during replication, inducing double-strand breaks that destabilize its structure and result in cytotoxicity; used as a chemotherapeutic for acute leukemia and other types of cancer, including BRCA2-mutated tumors.

An alkaloid that inhibits the growth of mouse leukemia P388 cells (IC₅₀ = 1.8 μg/ml); binds to and stabilizes the topoisomerase I-DNA binary complex, leading to DNA breakage and cell death (IC₅₀ = 5.07-12.6 μM); selectively inhibits CYP1A1 and CYP1A2 (IC50 = ~6 μM for…

A macrolide that causes the formation of bundles of intracellular microtubules in non-mitotic cells, induces the formation of hyperstable tubulin polymers, and arrests cell cycling in mitosis; induces mitotic arrest at nanomolar IC50 values in cell lines from ovarian, breast, lung, colon, prostate,…

A polymethoxylated flavone that has been shown to enhance adipogenesis and lipolysis, to inhibit α-glucosidase and α-amylase activity, and to suppress the expression of genes associated with inflammation by regulating IκBα.

A cell-permeable, stable free radical that is commonly used to evaluate the ability of compounds to act as free radical scavengers or hydrogen donors and to measure the antioxidant activity of tissue extracts; followed by color change from purple (absorbance at 515-528 nm) to yellow.

A pyrimadine analog that irreversibly inhibits thymidylate synthase, blocking the synthesis of thymidine which is required for DNA synthesis; widely used to treat many gastrointestinal tract adenocarcinomas.

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…

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 orally active broad spectrum antifungal agent that blocks ergosterol biosynthesis by inhibiting the fungal CYP isoform CYP51; potently inhibits the mammalian analog CYP51A1 (IC₅₀ = 63.5 nM), as well as a variety of other CYP isoforms.

An analog of wortmannin; irreversibly binds PI3K; inhibits recombinant PI3K and mTOR (IC₅₀ = 2.7 and 193 nM, respectively) and prevents the growth of LNCap cells (IC₅₀ = 1.46 μM).