A selective antagonist of BET bromodomains

RVX-208 – 10 mg

Brand:
Cayman
CAS:
1044870-39-4
Storage:
-20
UN-No:
Non-Hazardous - /

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}  

 

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Description

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), which causes selective release of BET proteins from chromatin; increases the expression of ApoA1 and reduces atherosclerosis in hyperlipidemic ApoE-deficient mice

Formal name: 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-4(3H)-quinazolinone

Synonyms: 

Molecular weight: 370.4

CAS: 1044870-39-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|MMPs||Research Area|Cardiovascular System|Cardiovascular Diseases|Atherosclerosis||Research Area|Epigenetics, Transcription, & Translation|Readers|Bromodomains

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