Biochem/physiol Actions

Reversible: yes

Cell permeable: yes

Primary TargetHDAC8 selective

General description

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.

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).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

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

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)