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Tubastatin A HCl | HDAC inhibitor

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).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 macrophages2. Tubastatin A has also been shown to have therapeutic potential for treatment of Alzheimer's disease via altered amloid-β load and reduced tau hyperphosphorylation.3,4,5

References/Citations
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

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Catalog#  10-4530

$29.00
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CAS:
1310693-92-5
Catalog Number:
10-4530
Activity:
HDAC inhibitor
Chemical Name:
N-Hydroxy-4-[(2-methyl-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl)methyl]benzamide hydrochloride
Molecular Weight:
371.86
Molecular Formula:
C20H22N3O2 HCl
Solubility:
Soluble in DMSO or Water.
Physical Properties:
Solid
Purity:
99% by HPLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 2 years as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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