Activators & Inhibitors

Activity: SOD mimetic . Function/Pharmacology: Superoxide dismutase (SOD) mimetic. Displays protective effects in CNS1 kidney2 and radiation damage3. Inhibits superoxide anion-induced inflammatory pain in mice.4 Blunts diabetes-induced upregulation of NADPH oxidase and ER stress in a rat model of diabetic nephropathy.5 Cell permeable Chemical Name: 4-Hydroxy-2,2,6,6-tetramethylpiperidine-1-oxyl

Cefuroxime Sodium is the sodium salt form of cefuroxime and a semi-synthetic, broad-spectrum, beta-lactamase resistant, second-generation cephalosporin antibiotic with bactericidal activity. Cefuroxime sodium (Cefuroxime sodium salt) inhibits bacterial cell wall synthesis by inactivating penicillin binding proteins (PBPs) thereby interfering with the final transpeptidation step required for cross-linking of peptidoglycan units which are a component of the cell wall. Lack of cross-linking results in a reduction of cell wall stability and leads to cell lysis.

Shield-1 is a specific, high-affinity, and cell-permeable ligand for FK506-binding protein 12 (FKBP) and reverses instability by binding to mutant FKBP (mtFKBP), allowing conditional expression of mtFKBP fusion proteins.

Apixaban (BMS-562247-01) is an orally active anticoagulant that inhibits coagulation factor Xa, directly preventing the conversion of prothrombin to thrombin and the formation of cross-linked fibrin clots.

PD 169316 is a potent, cell-permeable, and selective inhibitor of p38 MAP kinase.

Caffeic Acid Phenethyl Ester (Phenylethyl Caffeate) (CAPE) inhibits the activation of nuclear transcription factor NF-kappa B and may suppress p70S6K and Akt-driven signaling pathways, with antineoplastic, cytoprotective and immunomodulating activities. CAPE is the phenethyl alcohol ester of caffeic acid and a bioactive component of honeybee hive propolis. In addition, CAPE inhibits PDGF-induced proliferation of vascular smooth muscle cells through the activation of p38 mitogen-activated protein kinase (MAPK) and hypoxia-inducible factor (HIF)-1alpha and subsequent induction of heme oxygenase-1 (HO-1).

Activity: β3-adrenergic agonist / antiobesity . Function/Pharmacology: Potent and selective β-3 adrenergic receptor agonist. (EC50= 3 nM) Displays anti-obesity and anti-diabetic effects in mice. It increases brown fat thermogenesis and metabolic rate and decreases blood insulin and glucose levels1. Induces functionally active mitochondrial uncoupling protein (UCP) in white fat2. Active in vivo. Chemical Name: 5-[(2R)-2-[[(2R)-2-(3-Chlorophenyl)-2-hydroxyethyl]amino]propyl]-1,3-benzodioxole-2,2-dicarboxylic acid disodium salt

Activity: FGFR Phosphorylation inhibitor . Function/Pharmacology: Inhibits FGFR phosphorylation in vitro, in cell culture1, and in mouse tumor cell models2. SU-5402 can suppress ECP induced cardiomyocyte differentiation of P19CL6 embryonic carcinoma cells via an FGFR3 dependent pathway3. Chemical Name: 3-[4-Methyl-2-(2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-1H-pyrrol-3-yl]-propionic acid