Nexturastat A

Light pink solid. Soluble in DMSO. Slightly soluble in methanol or ethanol (1mg/ml). Almost insoluble in water. Cell permeable, potent and selective class IIb HDAC6 inhibitor (IC50 =5.02nM). Displays high selectivity over all other HDACs (IC50=3-10µ,M), Suppresses cell proliferation and promotes apoptosis in B16 cells (GI50=14.3µ,M) and human lymphoma cells HuT-78. Dose-dependently induces hyperacetylation of alpha-tubulin in B16 murine melanoma cells without elevating histone H3 acetylation, Induces cell cycle arrest in G1, HDAC6 deacetylates tubulin, HSP90 and the core histones (H2A, H2B, H3, H4). Histone deacetylases act via the formation of large multiprotein complexes. HDAC6 plays an important role in microtubule-dependent cell motility, transcriptional regulation, degradation of misfolded proteins and cell cycle and is involved in autophagy, inflammation, cancer and neurodegeneration.