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RVX-208

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    RVX-<wbr/>208
  • RVX-<wbr/>208
Cat No: 16424
Biochemicals - Small Molecule Inhibitors
Cayman

The bromodomain and extra terminal (BET) proteins interact with acetylated lysine-containing sequences on target proteins via their bromodomains, commonly altering gene transcription.{19044} The human BET proteins contain two bromodomains, the first (B...

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This product can only be bought through Cayman Chemical. Please contact us.

Territorial Availability: Available through Bertin Technologies only in France
Synonyms:
  • 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-4(3H)-quinazolinone
Correlated keywords:
  • epigenetics atherosclerosis proteins bindings chromatins research BD1 BD2 BDs 1 2 ones twos BD-1 BD-2 RVXs RVX208 208 bromodomains selective antagonists BETs cells apolipoproteins ApoA1 A1 mice mouse monkeys humans hyperlipidemic ApoE deficient deficiency deficiencies 1246400-89-4 1431550-07-0 RVX 000222 biochemicals
Product Overview:
The bromodomain and extra terminal (BET) proteins interact with acetylated lysine-containing sequences on target proteins via their bromodomains, commonly altering gene transcription.{19044} The human BET proteins contain two bromodomains, the first (BD1) being closer to the N-terminus than the second (BD2). RVX-208 is a selective antagonist of BET bromodomains, binding with 10-100-fold higher affinity for BD2 (IC50 = 0.04-0.28 µM) over BD1 (IC50 = 1.8-3.1 µM).{26809,26810} RVX-208 causes the selective release of BET proteins from chromatin in cells.{26809,26810} It interferes with the BET protein BRD4, resulting in an increased expression of apolipoprotein (Apo) A1 in cells, mice, monkeys, and humans.{26807,26811} RVX-208 also reduces atherosclerosis in hyperlipidemic ApoE-deficient mice.{26811}
Size 1 mg
Shipping dry ice
CAS Number 1044870-39-4
Molecular Formula C20H22N2O5
SMILES O=C1C2=C(OC)C=C(OC)C=C2NC(C3=CC(C)=C(OCCO)C(C)=C3)=N1
Molecular Weight 370,4
Formulation A crystalline solid
Purity ≥98%
Custom Code 2922.19
UNSPSC code 12352100

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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.

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Cross selling for this product : RVX-<wbr/>208 There are 2 products.

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