hd 1

PRO-HD1, a PROTAC (proteolysis-targeting chimera) HDAC6 degrader, effectively degrades HDAC6 in A549 cells and inhibits Jurkat cell proliferation with an IC50 of 5.8 µM [1].

SJ44236 is a BET PROTAC degrader capable of degrading BRD2 (DC50 = 0.127 nM), BRD3, and BRD4. It shows cytotoxicity in MV4-11 and HD-MB03 cells with IC50 values of 0.12 nM and 0.92 nM, respectively. The compound downregulates c-Myc expression and upregulates p53 expression. In mice, SJ44236 demonstrates good oral bioavailability (45%). [Pink: ligand for target protein JQ-1 carboxylic acid; Black: linker; Blue: ligand for E3 ligaseCereblonE3ligaseLigand 54]

HD-TAC7 is a PROTAC degrader targeting HDAC, with IC50 values of 3.6/4.2/1.1 μM for HDAC1/HDAC2/HDAC3. It can reduce the expression of NF-κB p65 in RAW 264.7 macrophages and can be used in inflammatory diseases such as asthma and chronic obstructive pulmonary disease (COPD).