• Detection method- Fluorescence (Ex/Em 400/505) • Species reactivity- Mammalian • Kit size- 100 assays • Applications- Effective means for screening caspase inhibitors using fluorometric methods.
Cell samples treated with Caspase inhibitor drugs
Features & Benefits
• Simple one-step procedure; takes only 1-1.5 hours • Fast and convenient • Inhibition of caspase-8 activity can be determined by comparison of the fluorescence intensity in samples with and without the testing inhibitors.
Caspases have been shown to play a crucial role in apoptosis induced by various deleterious and physiologic stimuli. Inhibition of caspases can delay apoptosis, implicating a potential role in drug screening efforts. The Caspase-8 Inhibitor Drug Screening Kit provides an effective means for screening caspase inhibitors using fluorometric methods. The assay utilizes synthetic peptide substrate IETD-AFC (AFC, 7-amino-4-trifluoromethyl coumarin). Active caspase-8 cleaves the synthetic substrate to release free AFC which can then be quantified by fluorometry. Compounds to be screened can directly be added to the reaction and the level of inhibition of caspase-8 activity can be determined by comparison of the fluorescence intensity in samples with and without the testing inhibitors.
Human and some mouse caspases are active in apoptosis and cell death and even in necrosis and inflammation. CASP Gene and orthologous enzymes have been identifies successfully in the signal transduction cascade and pathways.Tissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.
Alternative to gene target
v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog, C-Kit and CD117 and PBT and SCFR, KIT and IDBG-18980 and ENSG00000157404 and 3815, transferase activity, Extracellular, Kit and IDBG-172083 and ENSMUSG00000005672 and 16590, KIT and IDBG-642326 and ENSBTAG00000002699 and 280832