HD-TAC7

HD-TAC7 is a proteolysis-targeting chimera (PROTAC) composed of a class I histone deacetylase (HDAC) inhibitor linked to the cereblon ligand pomalidomide (Cay19877). It binds to HDAC1, HDAC2, and HDAC3 (IC50s = 3.6, 4.2, and 1.1 µM, respectively) and induces degradation of HDAC3 in RAW 264.7 cells with a half-maximal degradation concentration (DC50) value of 0.32 µM, without inducing degradation of HDAC1 or HDAC2. HD-TAC7 (10 µM) increases acetylation of histone H3 lysine 27 (H3K27Ac) in RAW 264.7 macrophages but reduces the levels of NF-kappaB p65 and does not increase the expression of IL10 in LPS- and IFN-gamma-stimulated RAW 264.7 macrophages, effects attributed to the pomalidomide moiety.. SMILES: O=C(N1)CCC(N2C(C3=C(C=CC=C3NCC(NCCCCC(NC4=CC=C(C(NC5=CC=C(F)C=C5N)=O)C=C4)=O)=O)C2=O)=O)C1=O. InChi Code: InChI=1S/C33H32FN7O7/c34-19-9-12-23(22(35)16-19)39-30(45)18-7-10-20(11-8-18)38-26(42)6-1-2-15-36-28(44)17-37-24-5-3-4-21-29(24)33(48)41(32(21)47)25-13-14-27(43)40-31(25)46/h3-5,7-12,16,25,37H,1-2,6,13-15,17,35H2,(H,36,44)(H,38,42)(H,39,45)(H,40,43,46). InChi Key: AMBNMDIPGZXRRW-UHFFFAOYSA-N