DK1-04e

DK1-04e (DK1-04 prodrug) is the prodrug of DK1-04, a potent, selective, and cell-permeable small-molecule SIRT5 inhibitor with IC50 of 0.34 uM;DK1-04e inhibits the cellular growth of breast cancer cells by targeting SIRT5.DK1-04e impairs mammary tumor growth in MMTV-PyMT transgenic mice and human breast cancer mouse model.SIRT5 inhibition suppressed the transformed properties of cultured breast cancer cells and significantly reduced mammary tumor growth in vivo, in both genetically engineered and xenotransplant mouse models.

1. Yashira L Negrón Abril, et al. Oncogene. 2021 Mar;40(9):1644-1658.