HPB is a cell-permeable, non-cytotoxic N-hydroxybenzamide derivative that acts as a HDAC6-selective deacetylase inhibitor (IC50 = 31/376/677/842/1133 nM against HDAC6/8/10/1/7, >2 μM against HDAC2/3/4/11/9/5). HPB treatment results in reduced growth, but not viability (up to 64 μM and 72 hrs), of LNCaP prostate cancer cells and non-cancer human foreskin fibroblasts (IC50 = 8 and 16-32 μM, respectively), causing upregulated acetylation levels of alpha-tubulin and peroxiredoxin, but not histones, both in cultures and in mice in vivo. Intraperitoneal injection is efficacious in suppressing the expansion of prostate cancer CWR22 xenograft-derived tumors in mice (by 73% in 4 wks; Five daily 300 mg/kg i.p. dosings a week) without detectable weight loss.
HPB is a cell-permeable, non-cytotoxic N-hydroxybenzamide derivative that acts as a HDAC6-selective deacetylase inhibitor.
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