Vorinostat | HY-10221

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. Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification.

IC50 & Target:

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.

Molecular weight:

264.32

Formula:

C₁₄H₂₀N₂O₃

SMILES:

O=C(NC1=CC=CC=C1)CCCCCCC(NO)=O

Storage: