Tubastatin A hydrochloride

Tubastatin A (1310693-92-5) is a potent and highly selective inhibitor of HDAC6 (IC50= 15 nM, >1000-fold selectivity against other HDAC isoforms, approx. 60-fold versus HDAC8).1It displayed anti-inflammatory and anti-rheumatic effects in Freund’s competitive adjuvant induced animal model of inflammation.2Tubastatin A inhibited TNF-α (IC50= 272 nM) and IL-6 (IC50 = 712 nM) in LPS stimulated human THP-1 macrophages.2Tubastatin A has also been shown to have therapeutic potential for treatment of Alzheimer’s disease via altered amyloid-β load and reduced tau hyperphosphorylation.3-5

Tubastatin A Hydrochloride is a neuroprotective HDAC6 inhibitor and is also known to induce hyperacetylation in primary cortical neuron cultures.

Tubastatin A Hydrochloride is an LSD1 inhibitor, which targets SOX2-expressing cancer cells.

Tubastatin A increases the total numbers of mitochondria and restores the number of moving mitochondria in DRG neurons. It reverses the axonal loss in peripheral neurons in mouse model of Charcot-Marie-Tooth disease. Tubastatin A inhibits the deacetylation of α-tubulin in murine myoblasts.

HDAC6

Store at -20°C

[1] KYLE V. BUTLER. Rational Design and Simple Chemistry Yield a Superior, Neuroprotective HDAC6 Inhibitor, Tubastatin A[J]. Journal of the American Chemical Society, 2010, 132 31: 10842-10846. DOI:10.1021/ja102758v
[2] SANTOSH VISHWAKARMA . Tubastatin, a selective histone deacetylase 6 inhibitor shows anti-inflammatory and anti-rheumatic effects[J]. International immunopharmacology, 2013, 16 1: Pages 72-78. DOI:10.1016/j.intimp.2013.03.016
[3] MONIKA NOACK  Christiane R L  Janina Leyk. HDAC6 inhibition results in tau acetylation and modulates tau phosphorylation and degradation in oligodendrocytes[J]. Glia, 2014, 62 4: 535-547. DOI:10.1002/glia.22624
[4] MAJ-LINDA SELENICA. Histone deacetylase 6 inhibition improves memory and reduces total tau levels in a mouse model of tau deposition.[J]. Alzheimer’s Research & Therapy, 2014, 6 1: 12. DOI:10.1186/alzrt241
[5] LING ZHANG. Tubastatin A/ACY-1215 improves cognition in Alzheimer’s disease transgenic mice.[J]. ACS Applied Electronic Materials, 2014: 1193-1205. DOI:10.3233/jad-140066