EC144 is a potent inhibitor of the heat shock protein 90.

  title={EC144 is a potent inhibitor of the heat shock protein 90.},
  author={Jiandong Shi and Ryan Van de Water and Kevin C. Hong and Ryan B Lamer and Kenneth W Weichert and Cristina M Sandoval and Srinivas Rao Kasibhatla and Marcus F. Boehm and Jianhua Chao and Karen Lundgren and Noelito Timple and Rachel Lough and Gerardo Ibanez and Christina Boykin and Francis J. Burrows and Marilyn R. Kehry and Theodore J. Yun and Erin K. Harning and Christine Ambrose and Jeffrey Thompson and Sarah A. Bixler and Anthone W. Dunah and Pamela Snodgrass-Belt and Joseph A Arndt and Istvan J. Enyedy and Ping Li and Victor Sukbong Hong and Andres McKenzie and Marco A Biamonte},
  journal={Journal of medicinal chemistry},
  volume={55 17},
Alkyne 40, 5-(2-amino-4-chloro-7-((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2-methylpent-4-yn-2-ol (EC144), is a second generation inhibitor of heat shock protein 90 (Hsp90) and is substantially more potent in vitro and in vivo than the first generation inhibitor 14 (BIIB021) that completed phase II clinical trials. Alkyne 40 is more potent than 14 in an Hsp90α binding assay (IC(50) = 1.1 vs 5.1 nM) as well as in its ability to degrade Her-2 in MCF-7 cells (EC… CONTINUE READING