Drug Discovery Research Screening Libraries
AdipoGen Xamoterol hemifumarate
Chemical. CAS 73210-73-8. Formula C16H25N3O5 • 1/2C4H4O4. MW 339.4 . 58.0. Soluble in water 20mg/ml or DMSO 40mg/ml. A phenoxypropanolamine derivative that is a selective partial agonist of beta1-adrenergic receptors beta1-ARs pA2 values are 7.4 - 7.8 and 5.2 - 6.2 at beta1- and beta2-adrenoceptors, respectively, and has shown to improve systolic and diastolic function in studies with heart failure patients. It modulates the sympathetic control of the heart but has no agonist action on beta2-adrenoceptors. Xamoterol has an EC50 value of 80nM for the generation of cyclic AMP cAMP in neonatal rat cardiomyocyte cultures. It increases spontaneous contraction of isolated rat right atria EC50 = 4.67nM. In vivo, xamoterol increases heart rate, an effect that is reversed by the selective beta1-AR antagonist betaxolol but not the selective beta2-AR antagonist ICI 118551.
AdipoGen TEPP46 ML-265
Chemical. CAS 1221186-53-3. Formula C17H16N4O2S2. MW 372.5. . Potent and selective cell-permeable pyruvate kinase M2 PKM2 activator with little or no activity versus PKM1, PKL and PKR. Useful agent for immunometabolism research. Anticancer reducing tumor sizes in mice and anti-inflammatory agent. Shown to bind the enzyme PKM2 to promote formation of stable, enzymatically-active tetramers, thereby promoting the last rate-limiting step of glycolysis, converting PEP to pyruvate. In addition, it prevents PKM2 translocation to the nucleus resulting in reduced glycolysis and HIF-1alpha activation, causing diminished Warburg effect and IL-1beta production.
Enzo Life Sciences SCREEN-WELL Epigenetics library (500 µl/well)
The SCREEN-WELL Epigenetics library contains 43 compounds with defined activity against enzymes which carry out epigenetic modification of lysine. It also includes DNA methylation inhibitors. Compounds are dissolved in DMSO at 10mM and aliquoted into deep-well plates at 100 or 500µl per well. The library is a useful tool for chemical genomics, assay development and other pharmacological applications. The library contains inhibitors of these important enzymes: HDACs, SIRTs, Lysine demethylases, HATs, Histone methyl transferases, DNA methyltransferases as well as SIRT activators. A variety of structurally and mechanistically different compound classes are included. Long Term Storage: -80°C. Applications: HTS .
Apexbio Technology LLC DiscoveryProbe™ Neuronal Signaling Library, 250uL/well(10 mM solution),96 Well Racks With Screw Cap
A unique collection of 556 neuronal signaling-related small molecules for neuroscience reasearch. Other sizes are available. Please inqury us for quote.
Apexbio Technology LLC DiscoveryProbe™ PI3K/Akt/mTOR Compound Library, 100uL/well(10 mM solution), 96 Well Racks With Screw Cap
A unique collection of 178 PI3K/Akt/mTOR inhibitors for PI3K/Akt/mTOR signaling pathway research. Other sizes are available. Please inqury us for quote.
AdipoGen Bafilomycin A1 high purity
Chemical. CAS 88899-55-2. Formula C35H58O9. MW 622.8. Bafilomycin A1, a macrolide antibiotic, is a highly potent, selective inhibitor of vacuolar H-ATPases. Bafilomycin A1 is a potent inhibitor of cellular autophagy either by blocking autophagosome-lysosome fusion or by blocking lysosomal degradation. Bafilomycin A1 has several other biological properties. It induces apoptosis or acts as an ionophore, meaning it can transfer K ions across biological membranes. Bafilomycin A1 can induce mitochondrial swelling in the presence of K ions, stimulate the oxidation of pyrimidine nucleotides and uncouple oxidative phosphorylation. Inhibition of V-ATPase activity with bafilomycin A1 led to the exacerbation of NLRP3 inflammasome activation in human monocytes in response to LPS. Bafilomycin A1 also significantly inhibited SARS-CoV-2 replication. In cancer, bafilomycin A1 has been shown to inhibit the growth of tumor cells by blocking the acidification of lysosomes.
AdipoGen SB415286
Chemical. CAS 264218-23-7. Formula C16H10ClN3O5. MW 359.7. Synthetic. Potent and selective cell permeable, ATP-competitive inhibitor of GSK3alpha with an IC50 value of 78nM and similar potency for GSK3beta. DYRK1A inhibitor IC50=0.9µM. Stimulates glycogen synthesis in liver cells and induces beta-catenin-dependent gene transcription. Acts as neuroprotectant and prevents neuronal cell death induced by PI3-kinase pathway. Anticancer agent with antiproliferative activity. Glycogen synthase kinase 3 GSK3 is a serine/threonine protein kinase that is inhibited by an assortment of extracellular stimuli such as insulin, growth factors, cell specification factors and cell adhesion. Its activity regulates many cell functions including the control of cell division, apoptosis and inflammation.
AdipoGen 2-Fluoro-2-deoxy-D-glucose
Chemical. CAS 29702-43-0. Formula C6H11FO5. MW 182.15. 2-Fluoro-2-deoxy-D-glucose is a glucose analog that inhibits cellular glycosylation. It is the natural isotope-form of 18F-FDG that can be taken up by cells but does not undergo metabolic glycolysis. FDG uptake is closely related to the expression of the glucose transporter GLUT in malignant tumours. FDG is also a substrate of hexokinase isozymes and an inhibitor of cellular glycosylation. FDG is taken up by high-glucose-using cells such as brain, brown adipocytes, kidney and cancer cells, where phosphorylation prevents the glucose from being released again from the cell, once it has been absorbed. The 2-hydroxyl group –OH in normal glucose is needed for further glycolysis metabolism of glucose by splitting it, but FDG is missing this 2-hydroxyl and cannot be further metabolized in cells. FDG is used in positron emission tomography PET as contrast agent and is the most widely used PET marker. FDG-PET can be used fo
AdipoGen Glyburide USP
Chemical. CAS 10238-21-8. Formula C23H28ClN3O5S. MW 494. Antidiabetic compound. Binds to and activates the ATP-sensitive potassium channels KATP inhibitory regulatory subunit sulfonylurea receptor 1 SUR1. Causes cell membrane depolarization and opening of voltage-dependent calcium channel. Increases intracellular calcium and stimulates insulin secretion in beta cells NLRP3 inflammasome inhibitor. Broad-spectrum ATP-binding cassette ABC transporter inhibitor. Shown to have anti-leishmanial activity. Potential inhibitor of collagenases.
AdipoGen N1-Guanyl-1 7-diaminoheptane
Chemical. CAS 150417-90-6 parent 150333-69-0. Formula C8H22N4O4S. MW 270. Cell permeable competitive deoxyhypusine synthase DHPS inhibitor. Targets the spermidine-binding site of deoxyhypusine synthase Ki = 9.7 nM, and prevents the first step in the post-translational conversion of a single lysine to hypusine on eukaryotic initiation factor 5A eIF5A. The modification is essential for sustained cell growth and therefore eIF5A hypusination controls cell proliferation and has been linked to cancer. Hypusination of eIF-5aA in macrophages is required for the TCA/OXPHOS pathways by regulating the expression of the important enzymes of the pathways. GC7 blocks the expression of the key enzymes at the level of translation and blocks OXPHOS in macrophages. Useful tool for immunometabolism research. The polyamine spermidine as a substrate to generate hypusinated eIF5A. Elevated levels of polyamines are a hallmark of most tumor types.
AdipoGen 4-Methylumbelliferyl nonanoate
Chemical. CAS 18319-93-2. Formula C19H24O4. MW 316.39. Synthetic. Non-fluorescent lipase substrate conjugated with 4-methylumbelliferone. After lipolytic hydrolysed the highly fluorescent 4-methylumbelliferone is released and emitts strongly at 485 nm blue fluorescence ex = 366 nm.
Apexbio Technology LLC DiscoveryProbe™ Histone Modification Library, 250uL/well(10 mM solution), 96 Well Racks With Screw Cap
A unique collection of 157 histone modification-related compounds for histone research. Other sizes are available. Please inqury us for quote.
AdipoGen AZD 7545
Chemical. CAS 252017-04-2. Formula C19H18ClF3N2O5S. MW 478.9. . Potent and selective pyruvate dehydrogenase kinase 2 PDK2 inhibitor IC50=6.4nM, consequently increasing pyruvate dehydrogenase PDH activity. Less potent inhibitor towards PDK1 and PDK3 IC50=87 and 600nM, respectively. Inhibitor of glycolysis. Antiobesity and antidiabetic agent. Improves blood glucose control in obese fa/fa Zucker rats. Useful agent for immunometabolism research. To maintain a continuous and steady supply of ATP during the feed-fast cycle, cells must select fatty acid or glucose for fuel. This process is largely controlled by the pyruvate dehydrogenase complex PDC, which regulates the entry of glycolytic products into the tricarboxylic acid cycle by catalyzing the oxidative decarboxylation of pyruvate to acetyl-coenzyme A CoA in the mitochondria of mammalian cells.
AdipoGen Rebaudioside A
Chemical. CAS 58543-16-1. Formula C44H70O23. MW 967.01. Rebaudioside A is a glucosylated steviol glycoside studied and used as a non-glycemic sweetener. It is one of the predominant steviol glycosides isolated from S. rebaudiana leaves. Rebaudioside A is a alpha-glucosidase inhibitor with IC50=35µg/ml and can inhibit ATP-sensitive K-channels. In vitro rebaudioside A stimulated the insulin secretion from MIN6 cells in a dose- and glucose-dependent manner. It increases glucagon-like peptide 1 GLP-1 secretion in a 2-dimensional mouse intestine model. Rebaudioside A is metabolized by gut microbiota to steviol. Rebaudioside A shows antioxidant activity on reducing cellular reactive oxygen species. It is an activator of Nrf2 and is a potential candidate hepatoprotective agent.
Apexbio Technology LLC DiscoveryProbe™ Anti-infection Compound Library Plus, 250uL/well(10 mM solution),96 Well Racks With Screw Cap
DiscoveryProbe™ Anti-infection Compound Library Plus is a unique collection of 663 anti-infection small molecules for anti-infection reasearch. Available in stock with overnight delivery and free shipping over $500 Cost-effective and competitive price to save your findings Potent, selective and cell-permeable in inhibiting or activating target molecules Diverse in chemical structure and route of administration (oral/i.m/i.v injection etc.) Detailed files describing potency, selectivity and applications etc. Supported by published data from top peer-reviewed journals Guaranteed high quality with NMR and HPLC validation. Other sizes are also available. Please inqury us for quote.