HDAC3/NCOR1 complex (human), (recombinant)

Approximately 1:1 stoichiometric complex of recombinant human HDAC3 (histone deacetylase 3) with a GST fusion protein comprising the Deacetylase Activation Domain (DAD) of human NCOR1 (amino acids 397-503; SANT1 domain plus amino flanking residues). Produced by coexpression of HDAC3 with a GST-NCOR1(DAD) construct in an insect cell system, the complex displays ~100-fold higher deacetylase activity than isolated HDAC3 (based on equal weights HDAC3 assayed at a saturating concentration (100µM) of a fluorogenic peptide substrate p53 379-382, K(Ac)382; Prod. No. BML-KI177).This HDAC3 preparation is active with various fluorogenic peptide substrates, including FLUOR DE LYS^® Substrate (Prod. No. BML-KI104) and FLUOR DE LYS^®-SIRT1 (p53 379-382, K(Ac)382; Prod. No. BML-KI177).

HDAC3, although a class I HDAC, is found in co-repressor complexes with the SMRT/N-CoR proteins, complexes distinct from than those comprising other class I enzymes. It has a unique domain structure, including both nuclear localization and nuclear export sequences and has been assigned to its own phylogenetic subclass.  Inhibition of HDAC3 may be the determining factor in the anti-proliferative effects of HDAC inhibitors on cancer cells and its caspase-dependent cleavage and relocation to the cytoplasm may be critical to the progression of apoptosis. It has been shown that HDAC3, rather than the class II HDACs 4 and 5, likely diretly deacetylates MEF2, implying an important role in pathways affecting heart disease.