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.
Estado de Materia
Soluble in DMSO (49 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (49 mg/ml at 25 °C).
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