Tubastatin A · HCl
HDAC-6 inhibitor / Tubastatin A is a potent and highly selective inhibitor of HDAC6 (IC50 = 15 nM, >1000-fold selectivity against other HDAC isoforms, approx. 60-fold versus HDAC8).1 It displayed anti-inflammatory and anti-rheumatic effects in Freund’s competitive adjuvant induced animal model of inflammation.2 Tubastatin A inhibited TNF-α (IC50 = 272 nM) and IL-6 (IC50 = 712 nM) in LPS stimulated human THP-1 macrophages.2 Tubastatin A has also been shown to have therapeutic potential for treatment of Alzheimers disease via altered amloid-β load and reduced tau hyperphosphorylation.3,4,5
Biochemicals & reagents
1310693-92-5
1) Butler et al. (2010), Rational design and simple chemistry yield a superior, neuroprotective HDAC6 inhibitor, tubastatin A; J.Am.Chem.Soc. 132 10842 2) Vishwakarma et al. (2013), Tubastatin, a selective histone deacetylase 6 inhibitor shows anti-inflammatory and anti-rheumatic effects; Int.Immunopharmacol, 16 72 3) Noack and Richter-Landsberg (2014), HDAC6 inhibition results in tau acetylation and modulates tau phosphorylation and degradation in oligodendrocytes; Glia, 62 535 4) Selenica et al. (2014), Histone deacetylase 6 inhibition improves memory and reduces total tau levels in a mouse model of tau deposition; Alzheimers Res.Ther. 6 12 5) Zhang et al. (2014) Tubastatin A/ACY-1215 improves cognition in Alzheimers disease transgenic mice; J.Alzheimers Dis. 41 1193
-20°C
TARGET: Protein deacetylase -- PATHWAY: Chromatin; Posttranslational modification -- RESEARCH AREA: Epigenetics; Neuroscience -- DISEASE AREA: Inflammation; Neurodegeneration