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Biological Activity:

HPOB is a potent and selective HDAC6 inhibitor with IC50 of 56 nM. It has >30-fold selectivity over other HDACs. It causes growth inhibition of normal and transformed cells but does not induce cell death. It enhances the effectiveness of DNA-damaging anticancer drugs in transformed cells but not normal cells. HPOB does not block the ubiquitin-binding activity of HDAC6. In mice bearing CWR22 human prostate cancer xenografts, when in combination with SAHA, HPOB causes suppression of the growth of established tumors, while produces no significant suppression when used alone.

How to Use:

In vitro: HPOB was used at 10-30 µM final concentration in various in vitro assays.
In vivo: HPOB was dosed to mice bearing CWR22 human prostate cancer xenografts at 300 mg/kg once per day by IP injection.

Reference:

• 1. Lee JH, et al. Development of a histone deacetylase 6 inhibitor and its biological effects. (2013) Proc Natl Acad Sci USA. 110(39):15704-9.