Tubastatin A · HCl

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