T3618

GSK-2881078 is a selective androgen receptor modulator (SARM) that is being evaluated for effects on muscle growth and strength in subjects with muscle wasting to improve their physical function.

Azelaoyl PAF is a potent PPARγ agonist that competitively binds thiazolidinediones with potency comparable to rosiglitazone. In atherosclerosis studies, Azelaoyl PAF promotes the uptake of oxidized low-density lipoprotein (oxLDL) by macrophages by upregulating CD36 expression. In fibroblasts from Friedreich's ataxia (FRDA) patients, Azelaoyl PAF significantly increased mRNA and protein levels of ferritin.

Quinaldopeptin is a quinomycin antibiotic. It is active against a variety of bacteria, including S. pyogenes, S. aureus, C. perfringens, S. faecalis, E. coli, and K. pneumoniae (MICs = 0.2, 0.4, 0.8, 1.6, 3.1 and 6.3 μg/ml, respectively). It is cytotoxic to B16/F10 and Moser cells (IC50s = 0.0008 and 0.04 μg/ml, respectively) and increases survival in a P388 leukemia mouse model. Quinaldopeptin is a bis-intercalator depsipeptide (NPBID) that binds to and intercalates into DNA (Kd = 32 nM).

Neamine tetrahydrochloride is a broad-spectrum aminoglycoside antibiotic with antibacterial, antitumor and neuroprotective activities, inhibits the growth of pancreatic cancer cells, and inhibits the proliferation of oral cancer cells. Neamine tetrahydrochloride inhibits xenogeneic human tumor growth and angiogenesis in athymic mice and can be used to study oral and pancreatic cancer.

Famoxadone (DPX-JE874) is a chiral bactericide with antifungal activity, induces hepatic steatosis, lipid metabolism disorders and hepatic oxidative stress, and induces thyroid gland dysfunction.

Globotriaosycleramides are glycosphingolipids found in mammalian cell membranes that are synthesized from lactosylceramides . They act as receptors for Shiga and Shiga-like toxins in vitro and in vivo. Globotriaosylceramides accumulate in endothelial cells, pericytes, vascular smooth muscle cells, renal epithelial cells, dorsal ganglia neuronal cells, and myocardial cells in patients with Fabry disease, a lysosomal storage disorder characterized by a deficiency in the enzyme α-galactosidase A. Globotriaosylceramides act as natural resistance factors to HIV infection, interacting with HIV gp120 to prevent its interaction with chemokine co-receptors and subsequent fusion of HIV to host cell membranes. This product contains a mixture of hydroxy and non-hydroxy fatty acid-containing globotriaosylceramides isolated from porcine red blood cells (RBCs).

Ceramide phosphoethanolamine (CPE) is an analog of sphingomyelin that contains ethanolamine rather than choline as the head group. It is the principal membrane phospholipid in invertebrates such as Drosophila, which lacks sphingomyelin. It is only produced in small amounts in mammalian cells, accounting for approximately 0.02 mol% of total phospholipids in mouse testis and brain. In Drosophila, CPE is biosynthesized by CPE synthase from ceramide and cytidine diphosphate-ethanolamine in the Golgi lumen. In mammals, it is biosynthesized by sphingomyelin synthase 2 (SMS2) in the plasma membrane and by sphingomyelin synthase-related protein (SMSr) in the endoplasmic reticulum (ER). In Drosophila, CPE has a role in glial ensheathment of axons. Disrupting CPE synthesis by depleting SMSr in vitro in mammalian cells leads to an accumulation of ER ceramides, which are then mislocalized to the mitochondria, inducing apoptosis. However, ceramide levels are not altered in transgenic mice lacking SMSr catalytic activity. CPEs (bovine) is a mixture of CPEs with variable N-acyl chain lengths.

NPX800 is an inhibitor of heat shock factor 1 (HSF1) and can be used in studies about the treatment of cancer.