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GSK2879552
GSK2879552

Basic Information
English Name 4-((4-((((1R,2S)-2-phenylcyclopropyl)amino)methyl)piperidin-1-yl)methyl)benzoic  
Synonym GSK2879552  
CAS 1401966-69-5  
Molecular Formula C23H28N2O2  
Molecular Weight 364.48  

Physical And Chemical Properties bp
nD20  
density  
fp  
Apperance yellow  

Transportation Information
UNNumber  
Class  
PG  
Dangerous Description  
Safe Description  

Usage
GSK2879552是组蛋白去甲基化酶LSD1口服活性不可逆抑制剂,具抗癌活性,临床1期。  

Other Infomation

GSK2879552 is an orally available, irreversible, inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.
IC50 value:
Target: LSD1 inhibitor
Upon administration, GSK2879552 binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the dimethylated form of lysine at position 4 of histone H3 (H3K4) to mono- and unmethylated H3K4. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor-suppressor genes. This may lead to an inhibition of cell growth in LSD1-overexpressing tumor cells. LSD1, overexpressed in certain tumor cells, plays a key role in tumor cell growth and survival.

[1]. Mohammad HP, et al. A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC. Cancer Cell. 2015 Jul 13;28(1):57-69



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