HDAC6 inhibitor,potent and selective
CAS：1310693-92-5
分子式：C20H21N3O2.HCl
分子量：371.86
纯度：98%
存储：Store at -20°C

Background:

Tubastatin A HCl is a selective inhibitor of HDAC6 with IC50 value of 15 nM [1].

HDAC6 (histone deacetylase 6) is an enzyme and plays an important role in a variety of processes, including transcriptional regulation, cell cycle preogression and developmental events. Abnormal expression of HDAC6 is correlated with many kinds of diseases, including Alzheimer's disease and cancers [1].

Tubastatin A HCl is a potent HDAC6 inhibitor and has the most selective compared with other HDAC isoforms. When tested with primary cortical neuron cells, Tubastatin A HCl treatment protected HCA-induced neuronal cell death in a dose range from 5 μM to 10 μM [1]. In HaCaT cells, administration of Tubastatin A HCl prevented sodium arsenite from inducing association of Nrf2 mRNA with ribosomes and elevation of Nrf2 protein by selectively inhibitng HDAC6 activity and had no effect on other HDACs [2]. Using atomic force microscopy study, Ketene AN et al. revealed that Tubastatin A HCl increased cell elasticity by inhibiting HDAC6 [3].

参考文献:
[1].  Kyle V. Butler, Jay Kalin, Camille Brochier, et al. Rational Design and Simple Chemistry Yield a Superior, Neuroprotective HDAC6 Inhibitor, Tubastatin A [J]. J. Am. Chem. Soc., 2010, 132 (31), pp 10842–10846.
[2].  Kappeler KV, Zhang J, Dinh TN, et al. Histone deacetylase 6 associates with ribosomes and regulates de novo protein translation during arsenite stress [J]. Toxicol Sci. 2012 May;127(1):246-255.
[3].  Ketene AN, Roberts PC, Shea AA, et al. Actin filaments play a primary role for structural integrity and viscoelastic response in cells [J]. Integr Biol (Camb). 2012 May;4(5):540-549.