Brief Description

I-BET151(GSK1210151A) is a BET bromodomain inhibitor(pIC50=6.1,BRD4); I-BET151 blocks recruitment of BET to chromatin .
IC50 value: 6.1(pIC50)
Target: BET bromodomain
I-BET151 induces apoptosis and G0/G1 cell cycle arrest in MLL-fusion leukemic cell lines in vitro (IC50 values are 15, 26, 120 and 192 nM for NOMO1, MV4;11, MOLM13 and RS4;11 cell lines respectively). I-BET151 reduces BCL2 expression in NOMO1 cells. I-BET151 improves survival in two rodents models of MLL-fusion leukemia in vivo.

Solubility

DMSO 100 mM Ethanol 100 mM

Melting point

Boiling point

Density

Formula Weight:

Flash point

Storage conditions

Store at -20°C 2 years

Appearance:

White to off-white solid