Territorial Availability: Available through Bertin Technologies only in France
- Correlated keywords
- kits assays measures measurements chromatin histones DNA posttranslational lysine methylation epigenetic regulations genomes Dot1 methyltransferases domains SET S-adenosyl-L-methionine SAM AdoMet epsilon aminos trithorax trxG Set1-like Set1 genes H3 loci Hox leukemias fluorescence polarization fluorescent probes binds binding molecules pockets inhibitors inhibits inhibition inhibiting sinefungin peptides substrates high-throughput screening SAM screener
- Product Overview:
Most histone lysine methyltransferases contain a conserved domain (SET) that utilizes S-adenosyl-L-methionine (SAM or AdoMet) as a co-factor to catalyze the methylation of the epsilon amino group of lysine. Mixed-lineage leukemia (MLL1) is a member of the trithorax group (trxG)/Set1-like family of gene activators that contains histone methyltransferase activity specific for lysine 4 of histone H3. This methylation plays an important role in gene activation at various developmentally regulated loci, such as the Hox gene loci. This fluorescence polarization assay is based upon a proprietary small molecule fluorescent probe* that binds to the SAM binding pocket in MLL1. Binding of the small molecule probe to MLL1 induces an increase in fluorescence polarization. Binding of the probe can be competed with the endogenous cofactor SAM or by the inhibitor sinefungin, but is unaffected by the histone H3 peptide substrate. The MLL1 SAM-Screener™ Assay is robust (Z’ >0.6) and exhibits a greater than 100 mP shift over a range of 0-500 nM MLL1. The assay is suitable for high-throughput screening in the provided 384-well plate or can be scaled to higher density plate formats (e.g., 1,536-well) if desired. *United States Patent 9,120,820
Cayman Chemical’s mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.
Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.
Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.
Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.
Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009
Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.