MK-0683 Vorinostat

Vorinostat, also known as suberanilohydroxamic acid, MK-0683 and SAHA, is a potent and selective inhibitor of histone deacetylases (HDACs). 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, including transcription factors crucial for the expression of genes needed to induce cell differentiation. Vorinostat was approved for the treatment of cutaneous T cell lymphoma (CTCL) when the disease persists, gets worse, or comes back during or after treatment with other medicines.

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[1]. Hrzenjak A et al. Histone deacetylase inhibitor vorinostat suppresses the growth of uterine sarcomas in vitro and in vivo. Mol Cancer. 2010 Mar 4;9:49.

[2]. Lautz TB, et al. The effect of vorinostat on the development of resistance to Doxorubicin in neuroblastoma. PLoS One. 2012;7(7):e40816.

[3]. Richon VM, et al. A class of hybrid polar inducers of transformed cell differentiation inhibits histone deacetylases. Proc Natl Acad Sci U S A. 1998 Mar 17;95(6):3003-7.