|
| | Tubastatin A hydrochloride Basic information |
| Product Name: | Tubastatin A hydrochloride | | Synonyms: | N-Hydroxy-4-[(1,2,3,4-tetrahydro-2-methyl-5H-pyrido[4,3-b]indol-5-yl)methyl]benzamide hydrochloride;Tubastatin A hydrochloride;TSA HCl;Tubastatin A Hydrochloride (Also See: T897000);Tubastatin A HCl salt;N-hydroxy-4-((2-methyl-1,2,3,4-tetrahydropyrido[4,3-b]indol-5-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 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 | | CAS: | 1310693-92-5 | | MF: | C20H22ClN3O2 | | MW: | 371.87 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 1310693-92-5.mol |  |
| | Tubastatin A hydrochloride Chemical Properties |
| 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. |
| WGK Germany | 3 | | HS Code | 29339900 |
| | Tubastatin A hydrochloride Usage And Synthesis |
| 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. | | Uses | Tubastatin A Hydrochloride is an LSD1 inhibitor, which targets SOX2-expressing cancer cells. | | 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 |
| | Tubastatin A hydrochloride Preparation Products And Raw materials |
|
