Territorial Availability: Available through Bertin Technologies only in France
- Synonyms
- 2,3-dihydro-5-[(2-hydroxy-1-naphthalenyl)methyl]-6-phenyl-2-thioxo-4(1H)-pyrimidinone
- Correlated keywords
- inhibitors inhibits inhibitions signals transductions hypoxia histones deacetylases cancers HDACs cell-permeable cells permeable SIRTs SIRT-1 SIRT-2 SIRT-5 1 2 5 SIRT1 SIRT2 SIRT5 SIRT-1/2 ½ blocking blocks NAD sensitizes H460 H-460 H 460 lungs G2 etoposide HepG2 NSCs NSC-112546 NSC112546 112546 II VI IV Nicotinamides adenines dinucleotides NAD+-dependent activity activities substrates competitive paclitaxel etoposide-induced arrest SIRT1-dependent hypoxic responses in vivo HIF-1a HIF-1alpha HIF-1.alpha. HIF-1? proteins accumulation EPO VEGF expressions HepG2 tumors mice mouse
- Product Overview:
SIRT1/2 inhibitor IV is a cell-permeable inhibitor of SIRT1 (IC50 = 56 µM) and SIRT2 (IC50 = 59 µM), blocking NAD+-dependent deacetylase activity in a substrate competitive manner.{22839} It less effectively inhibits SIRT5 (IC50 >300 µM) and has no effect on class I and II histone deacetylases.{22839} By inhibiting SIRT1, SIRT1/2 inhibitor IV sensitizes H460 lung cancer cells to etoposide and paclitaxel and enhances etoposide-induced G2 arrest.{22839} It also blocks a SIRT1-dependent hypoxic response in vivo, suppressing HIF-1? protein accumulation as well as EPO and VEGF expression in HepG2 tumors in mice.{22840}
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.