Off target protein and potency: HDAC1: 148 nM
Potency assay (off target):
In Reaction Biology biochemical assay, RGFP966 had no activity on HDACs other than HDAC3 up to 15 uM. The related compound (106): is 10-15-fold selective for HDAC3 > HDAC1 and HDAC2, and only weakly active against HDAC8. In experiments with recombinant HDAC1, IC50= 0.24 uM. Using a modified version of 106 for proteomic analysis after photo-crosslinking of recombinant HDACs (HDAC1, 2, 3, 4, 5, and 8), the compound was selective for HDAC3, with low level cross-linking with HDAC1.