HDAC6 degrader-1(Tsinghua University)

The present article describes about developing potent PROTACs tools for selective degradation of HDAC6 protein.To evaluate the degradation capability of our PROTACs for HDAC6 protein, analyzed the cellular levels of HDAC6 in HeLa cells by Western blot after incubation with four different PROTACs.It was found that all PROTACs can effectively induce HDAC6 degradation after 24 h.Among them, NP8 was the most potent degrader which can significantly reduce the HDAC6 protein level at 100 nmol/L.Then went on to evaluate the degradation potential of NP8 in a panel of cell lines from different origin.NP8 consistently induced significant degradation of HDAC6 in all the cell lines we tested, while the multiple myeloma cell line MM.