vorinostat-saha-mk0683

Description: Vorinostat (formerly known as suberanilohydroxamic acid, MK-0683; CCRIS-8456; HSDB 7930; SAHA; trade name: Zolinza) is a potent, orally bioavailable and non-selective pan-inhibitor of histone deacetylases (HDACs) with antitumor activity. It inhibits HDACs (pooled HDACs with all isoforms) with IC50 of ca.10 nM in a cell-free assay. It inhibits HDAC1, HDAC2 and HDAC3 (Class I), HDAC7 (Class II) and HDAC11 (Class IV ) with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat has been shown to bind to the active site of histone deacetylases and act as a chelator for Zinc ions also found in the active site of histone deacetylases. Vorinostat's inhibition of histone deacetylases results in the accumulation of acetylated histones and acetylated proteins that are crucial for cell differentiation. In October 2006, SAHA (Vorinostat) was approved by FDA as the first HDAC inhibitor for treating rare cutaneous T-cell lymphoma.

References: Proc Natl Acad Sci U S A. 1998; 95(6):3003-7; Cancer Res. 2000; 60(18):5165-70; Proc Natl Acad Sci U S A.2004; 101(2):540-5.

Publications Citing Use of InvivoChem Vorinostat (SAHA; MK0683): Nature. 2021 Aug 25. doi: 10.1038/s41586-021-03850-3.