HDAC Inhibitor XVII

A cell-permeable N-hydroxycinnamide derivative that acts a highly potent and HDAC8-selective histone deacetylase inhibitor (IC₅₀ = 27 nM), displaying much reduced or little potency against HDAC1/3 (IC₅₀ = 3.0 µM), HDAC2/4/6/10/11 (IC₅₀ >20 µM), or total HDAC activity in HeLa nuclear extract (IC₅₀ >10 µM). Reported to preferentially inhibit the proliferation of human lung cancer cells CL1-5, H1299, and A549 (IC₅₀ from 7 to 8 µM), while being much less toxic to normal human lung IMR-90 cells (73% inhibition at 40 µM).

A cell-permeable N-hydroxycinnamide derivative that acts a highly potent and HDAC8-selective histone deacetylase inhibitor (IC₅₀ = 27 nM), displaying much reduced potency against HDAC1/3 (IC₅₀ = 3.0 µM) and little or no activity toward HDAC2/4/6/10/11 (IC₅₀ >20 µM) or total HDAC activity in HeLa nuclear extract (IC₅₀ >10 µM). Reported to exhibit antiproliferative activity toward human lung cancer cells CL1-5, H1299, and A549 (IC₅₀ = 7.0, 7.2, and 7.9 µM, respectively), while being much less toxic to low HDAC8-expressing CL1-1 (IC₅₀ >10 µM) or normal human lung IMR-90 (73% inhibition at 40 µM) cells.

Cell permeable: yes

Primary Target
HDAC8 selective

Reversible: yes

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Huang, W. J., et al. 2012. ChemMedChem.7, 1815.

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