CBHA

Histone deacetylase (HDAC) inhibitors hyperacetylate histones and increase transcriptional activity in selected genes. Importantly, HDAC inhibitors induce apoptosis in some cancer cells and show promise in the treatment of certain forms of cancer. CBHA is a potent HDAC inhibitor, exhibiting ID₅₀ values of 0.01 and 0.07 μM in vitro for HDAC1 and HDAC3, respectively.¹ CBHA also induces apoptosis in nine different neuroblastoma cell lines in culture (0.5-4.0 μM)² and completely suppresses neuroblastoma tumor growth in SCID mice at 200 mg/kg.³ The efficacy of CBHA for suppressing tumor growth in mice is enhanced by the addition of retinoic acid.³

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1. Richon, V.M., Emiliani, S., Verdin, E., et al. A class of hybrid polar inducers of transformed cell differentiation inhibits histone deacetylases. Proc. Natl. Acad. Sci. USA 95(6), 3003-3007 (1998).

2. Glick, R.D., Swendeman, S.L., Coffey, D.C., et al. Hybrid polar histone deacetylase inhibitor induces apoptosis and CD95/CD95 ligand expression in human neuroblastoma. Cancer Res. 59(17), 4392-4399 (1999).

3. Coffey, D.C., Kutko, M.C., Glick, R.D., et al. The histone deacetylase inhibitor, CBHA, inhibits growth of human neuroblastoma xenografts in vivo, alone and synergistically with all-trans retinoic acid. Cancer Res. 61(9), 3591-3594 (2001).