Ligand id: 8392

Name: DZNep

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 7
Hydrogen bond donors 4
Rotatable bonds 2
Topological polar surface area 117.42
Molecular weight 264.12
XLogP -0.77
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Mechanism Of Action and Pharmacodynamic Effects
Aberrant EZH2 activity (up-regulation, gain-of-function mutations and loss-of-function mutations) is observed in many types of cancer, where it dysregulates repression of genes (silencing genes whch act as tumour supressors for example). This transcriptional dysregulation can play a part in the development of cancer, by permitting unfettered cell growth. DZNep inhibits up-regulated EZH2 activity, reactivates PRC2-silenced genes, re-establishes transcriptional control and causes apoptosis selectively in cancer cells [2].