aladdin 阿拉丁 B414067 BI 894999 1660117-38-3 98%

中文名：BI 894999

英文名：BI 894999

纯度：≥98%

货号：B414067

Cas号：1660117-38-3

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

Information

BI 894999 BI 894999 is a potent and selective BET inhibitor with IC50 of 5 nM and 41 nM for the binding of BRD4-BD1 and BRD4-BD2 to acetylated histones, respectively. BI 894999 is highly selective for BRD2/3/4 and BRDT (Kd of 0.49-1.6 nM), with at least a 200-fold selectivity vs. BRD4-BD1.

Targets

BET ; BRD4-BD1 (Cell-free assay); BRD4-BD2 (Cell-free assay) ; 5 nM; 41 nM

In vitro

BI 894999 is highly active in AML cell lines, primary patient samples. BI 894999 targets super-enhancer-regulated oncogenes and other lineage-specific factors, which are involved in the maintenance of the disease state.

In vivo

BI 894999 is active as monotherapy in AML xenografts, and in addition leads to strongly enhanced antitumor effects in combination with CDK9 inhibitors.

Cell Research(from reference)

Cell lines：MV-4-11B, THP-1, MOLM-13 

Concentrations：10 nM, 100 nM, various concentrations 

Incubation Time：4h, 24h, 79 h, 96 h 

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