CGK1026 6-(1,3-Dioxo-1H,3H-benzo[de]isoquinolin-2-yl)-hexanoic Acid Hydroxyamide Off-white Solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A relatively non-toxic, cell-permeable hydroxamic acid-containing histone deacetylase (HDAC) inhibitor. Facilitates transcriptional activation (TGFb/Smad4) in both stable and transient receptor assays in a concentration-dependent manner. At ~2 µg/ml (6-8 µM) concentrations, results in a greater than 100-fold increase in histone acetylation in PANC-1 cells. Reported to derepress hTERT by inhibiting the recruitment of HDAC into E2F-pocket protein complexes assembled on the hTERT promoter. Purity: ≥95% by HPLC. Ref.: Won, J., et al. 2004. Proc. Natl. Acad. Sci. USA 101, 11328. Su, G.H., et al. 2000. Cancer Res. 60, 3137. Sold under license of U.S. Patent 6,544,957. |