产品名称

E7449

一般描述

E7449 is an orally bioavailable, brain penetrable, small molecule dual inhibitor of PARP1/2 and also inhibits PARP5a/5b, otherwise known as tankyrase1 and 2 (TNKS1/2), important regulators of canonical Wnt/β-catenin signaling. It has IC50 values of 1.0 and 1.2 nM for PARP1 and 2, respectively.

别 称

11-(1,3-dihydroisoindol-2-ylmethyl)-2,3,10,12-tetrazatricyclo[7.3.1.0^{5,13}]trideca-1,5(13),6,8,11-pentaen-4-one

纯 度

≥97.0%(HPLC)

CAS NO.

1140964-99-3

分子式

C¹⁸H¹⁵N⁵O

分子量

317.34

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°C)

DMSO

~5mg/ml

乙醇

Insoluble

水

Very slightly soluble

l  生物学信息

生物活性/药理作用

PARP/Tankyrase Inhibitor 2X-121 is an orally available small molecule inhibitor of the nuclear enzymes poly (ADP-ribose) polymerase (PARP) 1 and 2, with potential antineoplastic activity. Upon administration, E7449 selectively binds to PARP 1 and 2, thereby preventing the repair of damaged DNA via the base excision repair (BER) pathway. This agent enhances the accumulation of single and double strand DNA breaks and promotes genomic instability eventually leading to apoptosis. PARP 1/2 inhibitor E7449 may enhance the cytotoxicity of DNA-damaging agents and of radiotherapy. PARP catalyzes post-translational ADP-ribosylation of nuclear proteins that signal and recruit other proteins to repair damaged DNA.

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