Vorinostat

A potent HDAC inhibitor, inhibits the activities of HDAC1 and HDAC3 with IC50 of 10 nM and 20 nM, respectively; inhibits cell growth, induce terminal differentiation and prevent the formation of tumours in mice models.Blood Cancer Approved(In Vitro):Vorinostat efficiently suppresses MES-SA cell growth at a low dosage (3 μM) already after 24 hours treatment. HDACs class I (HDAC2 and 3) as well as class II (HDAC7) are preferentially affected by this treatment. Vorinostat significantly increases p21WAF1 expression and apoptosis in MES-SA cells.Vorinostat inhibits SK-N-SH and SK-N-Be(2)C with the IC25 values of 1 μM and 0.5 μM, respectively.Vorinostat is an effective inhibitor of HPV-18 DNA amplification, reduces oncoproteins E6 and E7 activities and triggers apoptosis in HPV-infected, differentiated cells.(In Vivo):Vorinostat (50 mg/kg/day) reduces tumor growth by more than 50% in nude mice injected with 5×106 MES-SA cells.