产品名称

I-BET-762

一般描述

Molibresib is an inhibitor for BET proteins.

别 称

2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide; GSK525762; GSK525762A; I-BET

纯 度

≥98.0%(HPLC)

CAS NO.

1260907-17-2

分子式

C²²H²²ClN⁵O²

分子量

423.9

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

固体

溶解性(25℃)

DMSO

≥50mg/mL

乙醇

≥40mg/mL(warmed)

水

Insoluble

l  生物学信息

生物活性/药理作用

Molibresib is a small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing  proteins with potential antineoplastic activity. Upon administration, molibresib binds to the acetylated lysine recognition motifs on the bromodomain of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histone peptides. This disrupts chromatin remodeling and gene . Prevention of the of certain growth-promoting genes may lead to an inhibition of tumor cell growth. Characterized by a tandem repeat of bromodomain at the N-terminus, BET proteins, comprising of BRD2, BRD3, BRD4 and BRDT, are tranional regulators that play an important role during development and cellular growth.

Molibresib is an inhibitor for BET proteins with IC50 of ~35 nM in a cell-free assay, suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation, highly selective over other bromodomain-containing proteins.

l  存储

存储温度

-20℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov