A substrate for polyamine oxidase that is oxidized to 3-acetamidopropanal and putrescine, a polyamine involved in the division, differentiation, and membrane function of cells; used to examine the interaction between DNA and polyamines during the cleavage of phosphodiester bonds at…

An analog of latanoprost in which the hydroxyl at C-15 is inverted relative to latanoprost; binds to the FP receptor in the cat iris sphincter muscle with an IC₅₀ value of 24 µM (tested as the free acid); potential impurity in latanoprost bulk drug preparations.

An anionic oligopeptide-based bola-amphiphile that contains a hexane moiety flanked by a glycylglycine group at each end, which creates distinct hydrophilic and hydrophobic regions.

A high affinity agonist of TSPO (Ki = 0.297 nM in rat whole brain) that exhibits IC₅₀ values of 2.73 and 3.04 nM, respectively, against human and rat glial TSPO; produces anxiolytic and antidepressant effects in various animal models, without inducing benzodiazepine-like adverse effects.

Treprostinil is a stable analog of prostacyclin (Item No. 18220) that is used clinically for the treatment of PPH under the trade name Remodulin™. The structural modifications in treprostinil compared to prostacyclin increase the plasma half-life from 2 minutes to 34 and 85 minutes for…

A benzimidazole analog that inhibits IKK-ε with an IC50 value of ~15.8 µM.

Allyl disulfide is an organosulfur originally found in garlic that exhibits antioxidative, antiviral, neuroprotective, anti-parasitic, anticancer, and anti-hyperlipidemic activities. Allyl disulfide induces phase II enzymes, inhibits lipid peroxidation, and acts as a radical scavenger. In vitro,…

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 yellow breakdown product of heme catabolism, formed when heme is cleaved by heme oxygenase; has key roles as a free radical scavenger with antioxidant and anti-inflammatory actions.

A synthetic analog of natural PIP3 with C6:0 fatty acids at the sn-1 and sn-2 positions; features the same inositol and diacylglycerol stereochemistry as the natural compound; the short fatty acid chains give it higher solubility in aqueous media, as compared to naturally-occurring PIP3.

An enantiomer of the short-lived oral anti-coagulant acenocoumarol with a longer plasma elimination half-life (6.6 hours) and slower plasma clearance (1.9 L/hour), compared to the (S)-enantiomer (1.8 hours, 28.5 L/hour); rapidly absorbed from the gastrointestinal tract with essentially complete…

Cisplatin is a platinum-based cross-linking agent that exhibits anticancer chemotherapeutic activity. Cisplatin induces crosslinks between guanine bases on DNA; it is clinically used to treat various forms of cancer. In lung cancer cells, cisplatin decreases phosphorylation of PI3K, Akt, and FOXO3a…

The product of nitration of linoleate by NO-derived reactive species; activates PPARγ (Ki = 133 nM), inducing CD36 expression in macrophages, adipocyte differentiation, and glucose uptake; can also be metabolized to produce nitrite derivatives which in turn form NO, leading to increased cGMP production.

A synthetic derivative of native coelenterazine that exhibits 16-fold higher luminescence intensity (emission maximum ~466 nm; half-total time of 0.6-1.2 sec) than native coelenterazine.

A natural flavonol and potent antioxidant with anti-inflammatory actions; activator of sirtuin 1, inhibitor of the spleen tyrosine kinase SYK, and suppressor of CD36 gene expression.

Angiotensin II is a hormone that plays an important role in regulating blood pressure. Elevated levels of angiotensin II are implicated in inducing and maintaining hypertension, and also in the development of atherosclerosis. Both of these effects are mediated by the angiotensin II type 1 (AT1)…

A potent anti-mitotic drug that is 100-fold more active than resveratrol at inhibiting the growth of human colon cancer Caco-2 cells; inhibits tubulin polymerization in a dose-dependent manner (IC₅₀ = 4 μM) and enzymes involved in the synthesis of the polyamines, putrescine, and spermidine.

8-iso PGE2 is one of several isoprostanes produced from arachidonic acid during lipid peroxidation. It is a potent renal vasoconstrictor in the rat. 8-iso PGE2 inhibits U-46619 or I-BOP-induced platelet aggregation with IC₅₀ values of 0.5 and 5 µM, respectively. When infused into…

CWHM12 is an analog of RGD peptide (Item No. 14501), a tripeptide that inhibits integrin-ligand interactions in studies related to cell adhesion, migration, growth, and differentiation. CWHM12 selectively inhibits αv integrins (IC₅₀s = 1.8, 0.8, 61, 1.5, and 0.2 nM for…

An orally active small molecule drug with antioxidant, anti-inflammatory, and anti-fibrotic effects; reduces inflammatory cytokine production, suppresses TGF-β expression, and lowers markers of oxidative stress; has effectiveness in IPF and other conditions with a significant fibrotic component.

An indole diterpene which potently and reversibly inhibits large conductance Ca2+-activated K+ (BKCa) channels, as shown in patch clamp (Ki = 1.9 nM) and whole smooth muscle cell studies (Ki = 35.7 nM).

A bacteriocin, a natural polycyclic antibacterial peptide, also called a lantibiotic; particularly effective against Gram-positive bacteria and commonly used as a food preservative.

A natural nitroaryl-substituted polyketide that exhibits antitumor, antifungal, and insecticidal activities; non-competitive inhibitor NADH:ubiquinone oxidoreductase of bovine heart, N. crassa, and E. coli (IC₅₀s = 0.07, 0.08, and 22 nmol/mg protein, respectively).

A selective α1A-adrenergic receptor agonist that is at least 35-fold more potent at α1A receptor sites than at α1B or α1D; increases the frequency of spontaneous Ca2+ transients in rat ventricular myocytes in vitro with 330-fold more potency compared to activation by phenylephrine.

The reduced form of the electron acceptor NADP+ and acts as an electron donor in various biological reactions.

A small molecule inhibitor of the TGF-β receptor type 1 kinase (IC₅₀ = 56 nM) that has been used to study the role of TGF-β signaling in triple negative breast cancer cells and hepatocellular carcinoma cells.

A potent and selective dual inhibitor of EGFR and HER2 (IC50s = 19 and 3 nM, respectively); used in combination therapy to prevent or suppress cancers where these kinases are over-expressed, including breast cancer.

Spontaneously hypertensive rats fed a diet which includes γ-tocotrienol show significant reduction of systolic blood pressure and an increase of nitric oxide synthase activity in blood vessels. γ-Tocotrienol at 20 µM induces apoptosis of malignant sympathoadrenal (+SA) murine…

3-Tert-butyl-5-methoxy-catechol exhibits anticancer activity, inhibiting proliferation of leukemia cells. This compound may also induce cellular differentiation in vitro.

A food contaminant produced by Aspergillus that is associated with toxicity and hepatocarcinogenicity in human and animal populations.

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…

Bromhexine is a synthetic derivative of vasicine that exhibits mucolytic and antioxidative activities. Bromhexine increases production of serous mucus, decreases mucus viscosity, and helps cilia transport mucus out of the lungs. Bromhexine is clinically used to treat respiratory disorders…