N,N,N',N'-TETRAKIS(2-PYRIDYLMETHYL)ETHYLENEDIAMINE (TPEN) is a heavy metal chelator with strong affinities for Zn2+, Fe2+, and Mn2+. TPEN inhibits lamin assembly, destabilizes nuclear architecture and may independently protect nuclei from apoptosis in vitro. TPEN prevents HIF-1alpha from interacting with CBP, so reducing expression of HIF-1alpha target genes. TPEN was able to pass through the blood-brain barrier and the neuronal membrane, leading to successful intracellular zinc chelation - zinc chelation could be a potentially effective way for ischemic stroke treatment. TPEN exhibits robust anti-tumor activity in vivo in colon cancer mouse xenografts. In vivo experiments show that TPEN-loaded, aptamer-targeted liposomes reduce tumor growth in a human prostate cancer xenograft model.

N,N,N',N'-TETRAKIS(2-PYRIDYLMETHYL)ETHYLENEDIAMINE (TPEN) is a heavy metal chelator with strong affinities for Zn2+, Fe2+, and Mn2+. TPEN inhibits lamin assembly, destabilizes nuclear architecture and may independently protect nuclei from apoptosis in vitro. TPEN prevents HIF-1alpha from interacting with CBP, so reducing expression of HIF-1alpha target genes. TPEN was able to pass through the blood-brain barrier and the neuronal membrane, leading to successful intracellular zinc chelation - zinc chelation could be a potentially effective way for ischemic stroke treatment. TPEN exhibits robust anti-tumor activity in vivo in colon cancer mouse xenografts. In vivo experiments show that TPEN-loaded, aptamer-targeted liposomes reduce tumor growth in a human prostate cancer xenograft model.