HDAC6抑制剂

HPOB是一种有效的，选择性 HDAC6抑制剂，IC50为56 nM，选择性比对其它HDACs高30多倍。 In normal (HFS) and transformed (LNCaP, A549, and U87) cells, HPOB induces acetylation of α-tubulin, however, not histones, and inhibits cell growth, however, not viability. In HFS cells, HPOB enhances transformed cell death induced by etoposide, doxorubicin, or SAHA. HPOB also enhancing etoposide-induced transformed cell death via the apoptotic pathway in transformed cells. In mice bearing CWR22 human prostate cancer xenografts, HPOB (300 mg/kg/d i.p.), when in combination with SAHA, causes suppression of the growth of established tumors, while produces no significant suppression when used alone.