MX1013, a dipeptide caspase inhibitor with potent in vivo antiapoptotic activity

@article{Yang2003MX1013AD,
  title={MX1013, a dipeptide caspase inhibitor with potent in vivo antiapoptotic activity},
  author={Wu Yang and John Guastella and Jincheng Huang and Yan Wang and Li Zhang and Dong Xue and Minhtam B. Tran and Richard Woodward and Shailaja Kasibhatla and Ben Tseng and John A. Drewe and Sui Xiong Cai},
  journal={British Journal of Pharmacology},
  year={2003},
  volume={140}
}
Caspases play a critical role in apoptosis, and are considered to be key targets for the design of cytoprotective drugs. As part of our antiapoptotic drug‐discovery effort, we have synthesized and characterized Z‐VD‐fmk, MX1013, as a potent, irreversible dipeptide caspase inhibitor. MX1013 inhibits caspases 1, 3, 6, 7, 8, and 9, with IC50 values ranging from 5 to 20 nM. MX1013 is selective for caspases, and is a poor inhibitor of noncaspase proteases, such as cathepsin B, calpain I, or Factor… Expand
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