产品名称

OTX015

一般描述

OTX015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays.

别 称

Birabresib; MK-8628

纯 度

≥98.5%(HPLC)

CAS NO.

202590-98-5

分子式

C²⁵H²²ClN⁵O²S

分子量

491.99

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

白色至浅棕色固体

溶解性(25°C)

DMSO

≥50mg/ml

乙醇

≥50mg/ml

水

Very slightly soluble

l  生物学信息

生物活性/药理作用

Birabresib is a synthetic, small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins 2, 3 and 4 with potential antineoplastic activity. Upon administration, birabresib 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, including c-Myc-dependent target genes, may lead to an inhibition of tumor cell growth. Characterized by a tandem repeat of bromodomain at the N-terminus, the BET proteins BRD2, BRD3, BRD4 are tranional regulators that play an important role in cellular growth.

l  存储

存储温度

-20°C

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