Overview:

A potent and selective non-hydroxamate HDAC inhibitor. Considered to be a class I selective inhibitor but displays some selectivity amongst class I members: HDAC1 (IC₅₀ = 0.3 uM); HDAC3 (IC₅₀ = 8 uM) with no inhibition of HDAC8 (at >100 uM)¹. Induces hyperacetylation of nuclear histones in tumor cells resulting in inhibition of proliferation of a variety of human tumor cell lines². Protects p53-deficient mice against ischemic injury³. Supresses the p38 MAP kinase pathway in rheumatoid arthritic synovial fibroblasts⁴. Active in vivo.

References:

1. E Hu et al. J. Pharmacol. Exp. Ther. 2003 307:720

2. A Saito et al. Proc. Natl. Acad. Sci. USA 1999 96:4592

3. SP Murphy et al. J. Neurochem. 2013 Oct 21 epub

4. QY Choo et al. Molecules 2013 18:14085