A selective inhibitor of BET family proteins that binds BRD2

I-BET726 – 10 mg

Brand:
Cayman
CAS:
1300031-52-0
Storage:
-20
UN-No:
Non-Hazardous - /

I-BET726 is an inhibitor of BET family proteins that binds BRD2, BRD3, and BRD4 with high affinity (IC50s = 41, 31, and 22 nM, respectively) and competes with tetra-acetylated histone 4 peptides for binding to the bromodomains of these proteins.{27166,33208} It exhibits >1,000-fold selectivity for these proteins over other bromodomain-containing homologs.{33208} I-BET726 inhibits cell growth and induces cytotoxicity in neuroblastoma cell lines by modulating the expression of genes involved in apoptosis and Myc signaling.{33208} I-BET726 can be administered orally to animals, and it reduces tumor growth in mouse xenograft models of human neuroblastoma.{33208}  

 

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Description

A selective inhibitor of BET family proteins that binds BRD2, BRD3, and BRD4 with high affinity (IC50s = 41, 31, and 22 nM, respectively); inhibits cell growth and induces cytotoxicity in neuroblastoma cell lines, in vitro and in vivo

Formal name: 4-[(2S,4R)-1-acetyl-4-[(4-chlorophenyl)amino]-1,2,3,4-tetrahydro-2-methyl-6-quinolinyl]-benzoic acid

Synonyms:  GSK1324726A

Molecular weight: 435

CAS: 1300031-52-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Chromatin Reader Interactions||Research Area|Epigenetics, Transcription, & Translation|Readers|Bromodomains

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