JPS014 is a PROTAC degrader targeting HDAC1 , HDAC2 and HDAC3 , with DC 50 values of 0.91 μM, 4.19 μM and 0.64 μM, respectively. JPS014 recruits the VHL E3 ligase to mediate the ubiquitination and proteasomal degradation of HDAC1 , HDAC2 and HDAC3 . JPS014 acts as a submicromolar inhibitor of the HDAC1-CoREST , HDAC2-CoREST and HDAC3-SMRT complexes in vitro. JPS014 increases the level of H3K56ac , reduces the stability of LSD1 and SIN3A , and induces cell apoptosis ( apoptosis ). JPS014 can be used for the research of colon cancer . (Pink: HDAC1 and HDAC2 and HDAC3 ligand ( HY-50934 ); Blue: VHL ligand ( HY-125845 ); Black: linker).
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