一种选择性的HDAC3、HDAC6和HDAC8抑制剂, IC50分别为16.9 µM、2.47 µM和1.46 µM。
Droxinostat selectively inhibits HDAC3, 6, and 8, with IC50 values of 16.9 μM, 2.47 μM, and 1.46 μM, respectively Droxinostat is originally identified as a sensitizer of PPC-1 cells to FAS and TRAIL by down-regulating the expression of c-Fas-associated death domain-like interleukin-1-converting enzyme-like inhibitory protein (c-FLIP). In PPC-1 cells were cultured in suspension but not adherent conditions. Droxinostat also sensitizes other cancer cell lines including PC-3, DU-145, T47D, and OVCAR-3, but not LNCaP or MB-MDA-468, to anoikis or CH-11-induced apoptosis. In MCF-7 breast cancer cells, Droxinostat (10 μM–100 μM) sensitizes cells to apoptosis by decreasing c-FLIPL and c-FLIPS expression, reducing cell survival, and inducing apoptosis.