HNHA is a cell-permeable inhibitor of histone deacetylase (HDAC) activity (IC50 = 100 nM). In human fibrosarcoma HT1080 cells, it induces histone hyperacetylation and p21 transcription with concomitant inhibition of cell cycle progression (IC50 ~ 7.5 μM). HNHA is at least as effective as SAHA in inhibiting tumor growth in a murine xenograph model in vivo. HNHA also blocks the growth of human umbilical vein endothelial cells (HUVECs) and prevents tube formation and migration of HUVECs in response to vascular endothelial growth factor (VEGF). It also blocks retinal neovascularization and choroidal angiogenesis in mice.
A cell-permeable hydroxyamide-based SAHA analog that potently inhibits histone deacetylase (HDAC) activity
ChEBI: N-hydroxy-7-(2-naphthalenylthio)heptanamide is a member of naphthalenes.
previous study found that hnha was able to inhibit in-vitro hdac enzyme activity as well as proliferation of human fibrosarcoma cells (ht1080). in addition, treatment of cells with hnha could elicite histone hyperacetylation resulting in an up-regulation of cell cycle arrest, p21 transcription, and an inhibition of ht1080 cell invasion [1].
the effects of hnha on human cancer cells bearing xenograph mice was examined. results showed that as expected, hnha could dramatically reduce tumor volume as to (vehicle) control. in addition, hnha had a stronger potency than that of saha, which implied that the pharmacological potency of hnha was better than saha in vivo [1].
1. kim, d.h.,lee, j.,kim, k.n., et al. anti-tumor activity of n-hydroxy-7-(2-naphthylthio) heptanomide, a novel histone deacetylase inhibitor. biochemical and biophysical research communications 356, 233-238 (2007).
