Drug Discovery Research Screening Libraries
AdipoGen Aureothricin
Chemical. CAS 574-95-8. Formula C9H10N2O2S2. MW 242.3. Isolated from Streptomyces thioluteus. Antibiotic. Active against Gram-positive and Gram-negative bacteria, yeast, filamentous fungi, protozoa and insects. Potent bacterial and yeast RNA polymerases inhibitor. Inhibitor of fungal mannan and glucan formation. Similar to thiolutin. Antitumor compound.
AdipoGen Dimethyl fumarate
Chemical. CAS 624-49-7. Formula C6H8O4. MW 144.1. Immunomodulatory and anti-inflammatory agent used in patients with relapsing-remitting multiple sclerosis MS and psoriasis. Causes an immune switch characterized by induction of anti-inflammatory/regulatory innate and adaptive immune cell populations such as regulatory T cells Tregs and inhibition or apoptosis of pro-inflammatory cells, such as T helper 1 Th1 and Th17 subsets. Blocks immune cell activation through inhibition of glycolysis via post-transcriptional modification succination of glyceraldehyde 3-phosphate dehydrogenase GAPDH in vitro and in vivo and is therefore a useful agent for immunometabolism research. GAPDH catalyzes the conversion of glyceraldehyde 3-phosphate to 1,3-bisphosphoglycerate during glycolysis, an essential metabolic pathway where glucose is converted to pyruvate, to fuel the TCA cycle and oxidative phosphorylation OXPHOS for the production of adenosine triphosphate ATP as an energy source.
AdipoGen U-73122
Chemical. CAS 112648-68-7. Formula C29H40N2O3. MW 464.6. Gasdermin D N-terminal fragment GSDMD-N-induced pyroptosis inhibitor. Protects against GSDMD-N cytotoxicity in macrophages or against lethal infection in mice. Useful agent for inflammasome research. Potent cell permeable phospholipase C PLC , phospholipase A2 and 5-LO 5-lipoxygenase inhibitor. Affects the phospholipases by inhibiting the hydrolysis of PPI phosphatidylinositol to IP3 inositol triphosphate, which in turn leads to a drop in cytosolic Ca2. Potent inhibitor of the SERCA pump in smooth muscle. Potently inhibits Ca2-release from isolated smooth muscle cells independent of its effect on PLC. Inhibits agonist-induced platelet aggregation. Potently inhibits human polymorphonuclear neutrophil adhesion on biological surfaces and exhibits antinociceptive activity in vivo. Shown to inhibit agonist-induced down-regulation of muscarinic receptors in SK-N-SH neuroblastoma cells.
AdipoGen WZB117
Chemical. CAS 1223397-11-2. Formula C20H13FO6. MW 368.3. . GLUT inhibitor GLUT4 > GLUT1 = GLUT3. Fast-acting irreversible glucose transporter 1 GLUT1 inhibitor. Binds directly to GLUT1 involving three hydrogen bonds, one each with Asn34, Arg126, and Trp412. Blocks glucose transport in diverse cancer cells, reducing extracellular lactate and intracellular ATP levels and consequently decreases glycolysis. Anticancer agent in vitro and in vivo. Inhibits cancer cell proliferation, resulting in cell cycle arrest, senescence and necrosis or apoptosis. Inhibits the self-renewal and tumor-initiating capacity of cancer stem cells, blocking tumor initiation after implantation of cancer stem cells in mice.
AdipoGen STF-31
Chemical. CAS 724741-75-7. Formula C23H25N3O3S. MW 423.5. . Specific nicotinamide phosphoribosyltransferase NAMPT inhibitor IC50 = 19nM, consequently blocking the NAD⁺ salvage pathway and leading to blockage of GLUT1 expression. Glucose transporter 1 GLUT1 inhibitor IC50 ~1µM. Inhibits glucose uptake across the plasma membranes of mammalian cells and consequently decreases glycolysis. Anticancer agent. Shown to induce necrosis in cancer cells that lack the von Hippel-Lindau VHL tumor suppressor gene, which overexpress GLUT1. VHL-deficient cancer cells are dependent on the high affinity GLUT1 transporter and aerobic glycolysis for ATP production. Completely suppressed the glucose uptake activity and induced apoptosis in GLUT1 expressing myeloma cells as well. Useful agent for immunometabolism research. Toxic to human pluripotent stem cells hPSCs and used to selectively eliminate hPSCs from mixed cultures.
AdipoGen UK 5099
Chemical. CAS 56396-35-1. Formula C18H12N2O2. MW 288.3. . Potent and specific inhibitor of the mitochondrial pyruvate carrier MPC, blocking pyruvate from entering the mitochondria, consequently promoting lactate production. Inhibitor of tricarboxylic acid TCA cycle. Plasma membrane monocarboxylate transporters MCTs inhibitor, but with Ki values some two or three orders of magnitude higher than those for the inhibition of the MPC. Inhibits mitochondrial lactate and pyruvate transport. Decreases glycolysis. Useful agent for immunometabolism research.
AdipoGen 2-Deoxy-D-glucose
Chemical. CAS 154-17-6. Formula C6H12O5. MW 164.2. . Non-metabolizable glucose analog. An indirect inhibitor of hexokinase HK, inhibiting the rate limiting step of glycolysis and consequently decreases glycolysis. Inhibits phosphorylation of glucose by hexokinase, which consequently results in the depletion in cellular ATP, the inhibition of protein glycosylation and the disruption of ER quality control by inducing the unfolded protein response. Useful agent for immunometabolism research. Anticancer agent. Shown to cause cell cycle inhibition and cell death in in vitro models of hypoxia, induce autophagy, increase reactive oxygen species production, activate AMPK, and block tumor cell growth in animal models. Potential antiviral agent.
AdipoGen UK 5099
Chemical. CAS 56396-35-1. Formula C18H12N2O2. MW 288.3. . Potent and specific inhibitor of the mitochondrial pyruvate carrier MPC, blocking pyruvate from entering the mitochondria, consequently promoting lactate production. Inhibitor of tricarboxylic acid TCA cycle. Plasma membrane monocarboxylate transporters MCTs inhibitor, but with Ki values some two or three orders of magnitude higher than those for the inhibition of the MPC. Inhibits mitochondrial lactate and pyruvate transport. Decreases glycolysis. Useful agent for immunometabolism research.
AdipoGen 6-ECDCA
Chemical. CAS 459789-99-2. Formula C26H44O4. MW 420.6. Potent and selective FXR agonist EC50= 99nM. Induces SHP in HSCs to suppress TIMP-1 expression. Apoptosis inducer. Protects against liver fibrosis development in rat in vivo. Displays anticholeretic activity in rat in vivo. Promotes preadipocyte differentiation. Regulates adipogenesis and insulin signaling in vivo. Inhibits vascular smooth muscle cell inflammation and migration.
AdipoGen Ipragliflozin
Chemical. CAS 761423-87-4. Formula C21H21FO5S. MW 404.5. Ipragliflozin is an orally active, highly potent sodium glucose co-transporter 2 SGLT-2 inhibitor IC50 = 7.4nM, selective over SGLT-1, 3, 4, 5 and 6. SGLT-2 is one subtype of SGLTs found almost exclusively in the proximal tubules of nephronic components in kidneys, playing a key role in the re-uptake of glucose in the proximal tubule of the kidneys. Inhibition of SGLT-2 reduces blood glucose by blocking renal glucose reabsorption and thereby increasing urinary glucose excretion UGE. Anti-diabetic and anti-obesity agent. Shown to improve glycemic control and reduce body weight, furthermore, lowering hypoglycemic risk and abdominal symptoms. SGLT-2 inhibitors are likely to improve beta-cell function and insulin sensitivity and restore glucose homeostasis. Attenuates non-alcoholic steatohepatitis NASH development.
AdipoGen 5-Hydroxyindole-3-acetic acid
Chemical. CAS 54-16-0. Formula C10H9NO3. Molecular Weight 191.2. 5-hydroxy Indole-3-acetic acid 5-HIAA is the primary metabolite of serotonin, metabolized by monoamine oxidase and aldehyde dehydrogenase in the liver. As the catabolic end product of the serotonin pathway, 5-HIAA is present in body fluids like cerebrospinal fluid CSF, blood and urine. It can be used as an internal standard for the quantification of serotonin metabolism. 5-HIAA is a potent GPR35 receptor ligand, an inflammatory mediator for immune and non-immune cell populations. 5-HIAA is secreted by platelets and mast cells during inflammation and by binding to neutrophils has a chemoattractant role. 5-HIAA deficient mice show a loss of GPR35-mediated neutrophil recruitment to inflamed tissue. The chemoattractant GPR35-5-HIAA receptor-ligand system cooperates with other inflammation-induced factors in mediating neutrophil recruitment to sites of inflammation.
AdipoGen C75
Chemical. CAS 191282-48-1. Formula C14H22O4. MW 254.3. . Stable synthetic cerulenin derivative. Competitive irreversible fatty acid synthase FASN inhibitor that acts on KR, ACP and TE domains. Used to study fatty acid synthesis in metabolic disorders and cancer. Useful agent for immunometabolism research. Anorexigenic agent, activating CPT1 to accelerate fatty acid beta-oxidation. Shown to inhibit food intake through AMPK-related pathways. Cytotoxic to many cancer cell lines. Antitumor agent shown to suppress DNA replication and induce apoptosis.
AdipoGen Lac-Phe Acetate
Chemical. CAS 183241-73-8. Formula C12H15NO4 . C2H3O2. MW 237.3 . 59.0. Lac-Phe is an exercise-inducible metabolite, also called exerkine, that suppresses feeding and obesity. Lac-Phe is increased heavily with exercise in mammals and acts to reduce food intake and potentially decrease overall body weight and fat mass. In diet-induced obese mice, pharmacological administration of Lac-Phe led to decreased food intake, adiposity and body weight, as well as improved glucose homeostasis, while movement and energy expenditure were not affected. The biosynthesis of Lac-Phe from lactate and phenylalanine occurs in CNDP2 cells, including macrophages, monocytes and other immune and epithelial cells.
AdipoGen TOFA
Chemical. CAS 54857-86-2. Formula C19H32O4. MW 324.5. . Fatty acid synthase FASN inhibitor. Cell-permeable, potent, reversible and competitive inhibitor of acetyl-CoA carboxylase ACC consequently bocking the synthesis of malonyl-CoA. Useful agent for immunometabolism research. Anticancer agent. Induces apoptosis in a variety of tumor cell lines. Relatively non-cytotoxic to various cancer cell lines. TOFA-induced reduction in malonyl-CoA is reported to off-set the effect of C75 on food intake in fasted mice and on apoptosis in tumor cells. Hypolipidemic agent. Stimulates citrate accumulation in the cell, which leads to a suppression of glycolysis by citrate-induced inhibition of phosphofructokinase.
AdipoGen bpVHOpic
Chemical. CAS 722494-26-0. Formula K2VOO22C6H4NO3. MW 347.2. Potent protein phosphotyrosine phosphatase inhibitor. Insulin mimetic. PTEN inhibitor.