性能参数

产品名称

BET bromodomain inhibitor

规格

10mM (in 1mL DMSO) 10mg 50mg

货号

GOY-Y3544

 含量

>98.00%

CAS

1380087-89-7

别名

CPI-0610; CPI0610; CPI 0610

化学名

2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetimidic acid

分子式

C20H16ClN3O2

分子量

分子量 365.81

溶解度

≥ 18.3mg/mL in DMSO

储存条件

Store at -20°C

General tips

用途

仅供科研

价格

电询

详细内容

IC50: < 500 nM for BRD4

BET (bromodomain and extra-terminal) proteins regulate gene expression through their ability to bind to acetylated chromatin and subsequently activate RNA PolII-driven transcriptional elongation. The bromodomain (BRD) and extra-C terminal domain (BET) protein family consists of four members (BRD2, BRD3, BRD4 and BRDT).Small molecule BET inhibitors prevent binding of BET proteins to acetylated histones and inhibit transcriptional activation of BET target genes. BET inhibitors attenuate cell growth and survival in several hematologic cancer models, partially through the down-regulation of the critical oncogene, MYC. BET bromodomain inhibitor is a potent and selective inhibitor for BRD4.

In vitro: The most potent systhsized ompound presented is BET bromodomain inhibitor, which shows activity with IC50 < 500 nM against BRD4 [1].

In vivo: BET bromodomain inhibitor shows activity in vivo at < 10 mg/kg against BRD4 in rat [1].

Clinical trial: Up to now, BET bromodomain inhibitor is still in the preclinical development stage.

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十二烷基磺酸钠  2386-53-0  1-丁基磺酰氯  default-l

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