The in vivo anti-leukemia activity of N-(1-Pyrenlyl) maleimide in a bioluminescent mouse model

Chi Yuan Chen, Pei Chi Chang, Tong Hong Wang, Tzu Chien V. Wang*

*Corresponding author for this work

Research output: Contribution to journalJournal Article peer-review

4 Scopus citations


In a search for anticancer drugs by screening for inhibitors of telomerase, we have identified several small-molecule inhibitors that selectively inhibit telomerase in a cell-free system. Among these inhibitors, N-(1-pyrenyl) maleimide (NPM) induced apoptosis and displayed the greatest differential cytotoxicity against acute T cell leukemia-derived Jurkat cells cultured in vitro. In this work, the in vivo anti-leukemia activity of NPM was investigated using a bioluminescent mouse model. The luciferase–expressing Jurkat cells (Jurkat-Luc) were mixed with matrigel and injected subcutaneously into the nude mice. Drug treatment was commenced on day 7 after tumor implantation. The growth of xenografted tumors was significantly inhibited in the mice treated with NPM, which is comparable to the inhibitory effect of a classical anti-leukemia drug, cyclophosphamide. Combined treatment with NPM and cyclophosphamide further enhanced the growth inhibition of xenografted Jurkat-Luc cells. Immunohistochemistry staining with cleaved caspase 3 (cl-caspase 3) indicated a very heavy staining of cl-caspase 3 only in the tumor implants excised from the NPM-treated mice. We conclude that NPM induced apoptosis and inhibited the growth of xenografted Jurkat-Luc cells in nude mice, demonstrating that NPM displays anti-leukemia activity in vivo.

Original languageEnglish
Pages (from-to)64-69
Number of pages6
JournalLeukemia Research
StatePublished - 11 2017

Bibliographical note

Publisher Copyright:
© 2017 Elsevier Ltd


  • Anticancer drug
  • Bioluminescent mouse model
  • N-(1-Pyrenyl) maleimide
  • T-cell acute lymphoblastic leukemia
  • Telomerase inhibitor


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