Nexturastat A is a selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 value of 5.2 nM [1].
Nexturastat A is a HDAC inhibitor. It was developed by structural modification of aryl urea HDACIs. The inhibitory activity of Nexturastat A is most potent against HDAC6 with IC50 value of 5.2 nM. Besides that, Nexturastat A also shows inhibition of other HDACs with IC50 values of 3.02, 6.92, 6.68, 9.39, 11.7, 4.46, 0.954, 6.72, 7.57 and 5.14 μM for HDAC1, 2, 3, 4, 5, 7, 8, 9, 10 and 11, respectively. Nexturastat A has been shown to suppress cell proliferation and promote apoptosis in B16 murine melanoma cells [1, 2].
References:
[1] Kalin J H, Bergman J A. Development and therapeutic implications of selective histone deacetylase 6 inhibitors. Journal of medicinal chemistry, 2013, 56(16): 6297-6313.
[2] Zhang L, Han Y, Jiang Q, et al. Trend of Histone Deacetylase Inhibitors in Cancer Therapy: Isoform Selectivity or Multitargeted Strategy. Medicinal research reviews, 2014.
