TPEN (16858-02-9) is a cell permeable metal chelator. Frequently used to study effects of zinc depletion on cellular processes.1,2
Membrane-permeable zinc chelator; decreased the intracellular level of zinc and induced apoptosis.
ChEBI: An N-substituted diamine that is ethylenediamine in which the four amino hydrogens are replaced by 2-pyridylmethyl groups.
N,N,N′,N′-Tetrakis(2-pyridylmethyl)ethylenediamine (TPEN) elicits pro-apoptotic effect in human acute promyelocytic NB4 cells by inhibiting nitric oxide signalling and Zn2+ signaling. In microglia pretreated with zinc, TPEN inhibits the interleukin 6 secretion and nitric oxide synthase (iNOS) mRNA expression. It induces damage on DNA structure by activating ATM (ataxia telangiectasia mutated) and ATR (ATM-Rad3-related) signaling in human colon cancer cells.
1) Chimienti et al. (2001) Role of cellular zinc in programmed cell death: temporal relationship between zinc depletion, activation of caspases and cleavage of Sp family transcription factors; Biochem. Pharmacol. 62 51
2) Meplan et al. (2000) Metalloregulation of the tumor suppressor protein p53: zinc mediates the renaturation of p53 after exposure to metal chelators in vitro and in intact cells; Oncogene 19 5227
