Identification | Back Directory | [Name]
N-Hydroxy-4-[(1,2,3,4-tetrahydro-2-methyl-5H-pyrido[4,3-b]indol-5-yl)methyl]benzamide hydrochloride | [CAS]
1310693-92-5 | [Synonyms]
TSA HCl CS-1894 Tubastatin A HCl salt Tubastatin A HCl, >=98% Tubastatin A hydrochloride TUBASTATIN A HYDROCHLORIDE;TSA HCL Tubastatin A HCl (AG-CR-13900, TubA) Tubastatin A hydrochloride ISO 9001:2015 REACH Tubastatin A Hydrochloride (Also See: T897000) Tubastatin A HCl, 98%, a potent and selective HDAC6 inhibitor N-Hydroxy-4-(2-methyl-1,2,3,4-tetrahydro-pyrido[4,3-b]indol-5-ylmethyl)benzamide hydrochloried N-hydroxy-4-((2-methyl-1,2,3,4-tetrahydropyrido[4,3-b]indol-5-yl)methyl)benzamide hydrochloride N-Hydroxy-4-((2-methyl-3,4-dihydro-1H-pyrido[4,3-b]-indol-5(2H)-yl)methyl)benzamide hydrochloride N-Hydroxy-4-[(1,2,3,4-tetrahydro-2-methyl-5H-pyrido[4,3-b]indol-5-yl)methyl]benzamide hydrochloride N-Hydroxy-4-[(2-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-b]indol-5 -yl)methyl]benzamide hydrochloride (1:1) N-Hydroxy-4-[(1,2,3,4-tetrahydro-2-methyl-5H-pyrido[4,3-b]indol-5-yl)methyl]benzamide hydrochloride Tubastatin A HCl Tubastatin A hydrochloride N-Hydroxy-4-[(1,2,3,4-tetrahydro-2-methyl-5H-pyrido[4,3-b]indol-5-yl)methyl]benzamide hydrochloride | [Molecular Formula]
C20H21N3O2.HCl | [MDL Number]
MFCD20488052 | [MOL File]
1310693-92-5.mol | [Molecular Weight]
371.861 |
Chemical Properties | Back Directory | [Melting point ]
>221°C (subl.) | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO or Water. | [form ]
powder | [color ]
white to tan | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 3 months. |
Hazard Information | Back Directory | [Description]
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 macrophages.2?Tubastatin 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 | [Uses]
Tubastatin A Hydrochloride is a neuroprotective HDAC6 inhibitor and is also known to induce hyperacetylation in primary cortical neuron cultures. | [Biological Activity]
Tubastatin A hydrochloride is a potent and selective inhibitor of HDAC6. | [Biochem/physiol Actions]
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. | [target]
HDAC6 | [storage]
Store at -20°C | [References]
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 Alzheimer’s disease transgenic mice; J. Alzheimers Dis.,?41?1193 |
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