Vorinostat

Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC6 and HDAC7 (Class II) and HDAC11 (Class IV), with ID₅₀ values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis^[1][4]. Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification^[7]. IC50 & Target:ID50: 10 nM (HDAC1), 20 nM (HDAC3)^[3]
HDAC2, HDAC7^[1], HDAC11^[4] 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 p21^WAF1 expression and apoptosis in MES-SA cells^[1].
Vorinostat inhibits SK-N-SH and SK-N-Be(2)C with the IC₂₅ values of 1 µM and 0.5 µM, respectively^[2].
Vorinostat is an effective inhibitor of HPV-18 DNA amplification, reduces oncoproteins E6 and E7 activities and triggers apoptosis in HPV-infected, differentiated cells^[7]. In Vivo: Vorinostat (50 mg/kg/day) reduces tumor growth by more than 50% in nude mice injected with 5×10⁶ MES-SA cells^[1].