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)
This product has met the following criteria to qualify for the following awards: