I-BET151

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

I-BET151 (GSK1210151A) is a potent, selective BET bromodomain inhibitor.

I-BET151 (GSK1210151A) is a potent, selective BET bromodomain inhibitor with IC50 of 0.5, 0.25 and 0.79 uM for BRD2, BRD3 and BRD4 in FP assays, shows no effect on the 23 other bromodomain proteins including MLL; demonstrates potent efficacy against cell lines harbouring different MLL-fusions (MOLM13 cell IC50=120 nM, MV4:11 cell IC50=26 nM), induices early cell cycle arrest and apoptosis, selectively abrogates BRD3/4 recruitment to chromatin;shows significant therapeutic value and survival benefit in mouse models of murine MLL-AF9 and human MLL-AF4 leukaemia.

GSK1210151A;I-BET 151;GSK-1210151A

Chromatin/Epigenetic

Bromodomain

BRD2;BRD3;BRD4

Cancer

——

1300031-49-5

415.44

C23H21N5O3

>98% (HPLC)

10 mM in DMSO

O=C(N1[C@@H](C2=NC=CC=C2)C)NC3=C1C4=CC(OC)=C(C5=C(C)ON=C5C)C=C4N=C3

2H-Imidazo[4,5-c]quinolin-2-one, 7-(3,5-dimethyl-4-isoxazolyl)-1,3-dihydro-8-methoxy-1-[(1R)-1-(2-pyridinyl)ethyl]-

(-20℃)

With Ice Pack

≥ 2 years