ML-204 selectively blocks transient receptor potential canonical 4 (TRPC4) channels (IC₅₀s = 0.96 and 2.6 μM in fluorescent and electrophysiological assays, respectively). It exhibits 19-fold selectivity against TRPC6 and 9-fold selectivity against TRPC5 and does not affect TRPV1,…

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 lipophilic, nontoxic, iron-chelating agent that shows high iron chelation efficacy both in vitro in cell culture models and also in vivo in rats and mice.

A melatonin receptor antagonist that preferentially targets MT1B over MT1A (Ki values = 10-27 and 158-513 nM, respectively); used both in vitro and in vivo to evaluate the roles of melatonin receptor signaling in diverse pathways.

A monobactam antibiotic that is effective against Gram-negative bacteria but inactive against Gram-positive bacteria.

A potent ER antagonist that works by both down-regulating and degrading ERα; efficacious in the treatment of estrogen-sensitive breast cancer; fully activates ER on hippocampal neurons.

A stable analog of PFT-α, formed by the condensation of PFT-α in solution; inhibits the growth of the cancer cell lines IGROV-1, A2780, and HCT116 (IC₅₀ = 23, 77, and 103 μM, respectively); induces autophagy in HCT116 cells and sensitizes IGROV-1 and H460 cells to…

A water soluble, irreversible, broad spectrum inhibitor of serine proteases, including trypsin, chymotrypsin, plasmin, thrombin, and kallikreins; also inhibits NADPH oxidase.

Linolein hydroperoxides are a mixture of 132 possible isomers of mono-, di-, and tri-hydroperoxides produced from the autoxidation of trilinolein. Autoxidation of linoleic acid containing triglycerides (for example, trilinolein) in vivo could result in the formation of these hydroperoxides. Unlike…

A glucosamine-nitrosourea which is commonly used to induce experimental diabetes in animals; specifically targets beta cells, entering via the glucose transporter GLUT2 and causing alkylation of DNA, leading to the destruction of beta cells.

A specific inhibitor of PI3K activity and a widely used inhibitor of the autophagy; at 5 mM, inhibits protein degradation in rat hepatocytes by 65% and blocks class I, II, and III PI3Ks, including some downstream targets.

A potent TRPV1 antagonist that inhibits capsaicin-induced and acid-induced activation of rat TRPV1 with IC50 values of 35 and 6 nM, respectively.

A hybrid molecule patterned after N-arachidonoyl serotonin; inhibits capsaicin-induced TRPV1 channel activation (IC₅₀ = 2.57 μM) without blocking FAAH-mediated hydrolysis of arachidonoyl ethanolamine (IC₅₀ > 50 μM).

O-ASHA is an irreversible, non-selective inhibitor of COX-1 and COX-2. Aspirin is the best-studied example of an irreversible COX inhibitor, acting via the acetylation of the active site serine residue 529 in human COX-1. O-ASHA inhibits ovine COX-1 in a time-dependent, irreversible manner with a…

A natural macrocyclic antibiotic that inhibits RNA polymerase with selectivity for Gram-positive bacteria over Gram-negative bacteria (IC₅₀s = 0.4 and 6 μM, respectively); has potent antibacterial activity against most Gram-positive bacteria and effectively targets the Gram-positive…

Selectively inhibits human NHE-1 with an IC₅₀ value of 14 nM; reduces infarct size in a rabbit myocardial ischemia-reperfusion model without adversely affecting hemodynamics or cardiac function.

TTP 22 is a thienopyrimidine compound that inhibits casein kinase 2 (CK2) with an IC₅₀ value of 100 nM (Ki = 40 nM). It displays selectivity for CK2 over JNK3, ROCK1, and MET with no inhibitory effects towards these kinases at 10 μM.

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

1-Oleoyl lysophosphatidic acid is a species of LPA containing oleic acid at the sn-1 position. Phosphatidic acid is produced either directly through the action of PLD or through a two step process involving liberation of DAG by PLC followed by phosphorylation of DAG by diglycerol kinase.{2656}…

Synonyms Ampakine CX-516 Ampalex CX-516

2-(hydroxymethyl)-Pyrimidine is a synthetic intermediate useful for pharmaceutical synthesis.

An HMG-CoA reductase inhibitor that is effective in treating hypercholesterolemia and certain dyslipidemias; reduces the production of LDL as well as inhibiting cholesterol synthesis; metabolized by CYP3A4, prodrug several metabolites that are important in the therapeutic actions attributed to atorvastatin.

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.

A protein cross-linking agent isolated from G. jasminoides Ellis; inhibits UCP2 activity; 5 µM genipin increases glucose-stimulated insulin secretion in isolated pancreatic islets chronically exposed to high levels of glucose; induces apoptosis in FaO rat hepatoma cells and human…

An antithrombic compound whose active metabolite is a selective, irreversible antagonist of the platelet purinergic P2Y12 receptor (IC₅₀ = 100 nM); inhibits ADP-induced platelet aggregation ex vivo; shown to be beneficial in the prevention of vascular ischemic events for patients without…

A monoacetylated derivative of spermine (Item No. 18041), an endogenous polyamine synthesized from spermidine (Item No. 14918), that displays lower Km and higher Vmax values than spermine, making it a better substrate of polyamine oxidase than the non-acetylated polyamine.

A natural sesquiterpene that inhibits the proliferation of a wide range of tumors and enhances the effects of various chemotherapies; 10-40 µg/ml dose-dependently induces apoptosis and cell cycle arrest in the G2/M phase in HepG2 cells, upregulating Fas/FasL expression.

An analog of trimethoxy resveratrol; inhibits the growth of a variety of human tumor cell lines at concentrations form 0.4 to 2 µg/ml, which is 5-6 times more potent than resveratrol

An irreversible inhibitor of the chymotrypsin-like β5 subunit of the constitutive 20S proteasome (IC₅₀ = 5.2 nM) and the β5i subunit of the immunoproteasome 20Si (LMP7; IC₅₀ = 14 nM) with minimal cross reactivity to other proteases; induces cell cycle arrest and…

A synthetic quinine derivative commonly used as an anti-malarial drug; also useful in managing SLE, rheumatoid arthritis, and other diseases; inhibits autophagy and induces autophagic cell death (IC₅₀ = 30 µM).

A potent inhibitor of both MEK 1 and 2 that works in an ATP-noncompetitive fashion (IC₅₀s = 0.7 and 0.9 nM, respectively); blocks dual phosphorylation of ERK1/2 and stops cell cycling in cancer cell lines, both in vitro and in multiple tumor models in mice.

An agonist of β-adrenergic receptors that activates the β1, β2, and β3 receptors with pEC₅₀ values of 7.5, 9.0, and 6.8 respectively; displays high selectivity for β-adrenoceptors in the trachea over those in atria; activity is retained in the airway for extended periods.