(S)-HDAC-42 is a potent inhibitor of HDAC (IC50 = 16 nM in vitro). (S)-HDAC-42 decreases the viability of prostate cancer cell lines (IC50 = 0.40 μM), increasing the expression of p21 and the acetylation of histone H3 while decreasing the phosphorylation of Akt and the expression of Bcl-XL. (S)-HDAC-42 also strongly suppresses the growth of PC-3 tumor xenografts, reducing levels of phospho-Akt and Bcl-XL protein in tumors.
1 Lu, Q., Wang, D., Chen, C., et al. Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors. J Med Chem 48 5530-5535 (2005). 2 Kulp, S.K., Chen, C., Wang, D., et al. Antitumor effects of a novel phenylbutyrate-based histone deacetylase inhibitor, (S)-HDAC-42, in prostate cancer. Clin Cancer Res 12(17) 5199-5206 (2006).
Estado de Materia
Soluble in 1:1 DMSO:PBS (pH 7.2) (~0.5 mg/ml), ethanol (~20 mg/ml), DMF (~20 mg/ml), DMSO (~20 mg/ml), and water (<1 mg/ml) at 25 °C.
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