Tubastatin A hydrochloride
Synonym(s):N-Hydroxy-4-(2-methyl-1,2,3,4-tetrahydro-pyrido[4,3-b]indol-5-ylmethyl)benzamide hydrochloried; N-Hydroxy-4-((2-methyl-3,4-dihydro-1H-pyrido[4,3-b]-indol-5(2H)-yl)methyl)benzamide hydrochloride
- CAS NO.:1310693-92-5
- Empirical Formula: C20H22ClN3O2
- Molecular Weight: 371.87
- MDL number: MFCD20488052
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-04 13:44:46
What is Tubastatin A hydrochloride?
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
The Uses of Tubastatin A hydrochloride
Tubastatin A Hydrochloride is a neuroprotective HDAC6 inhibitor and is also known to induce hyperacetylation in primary cortical neuron cultures.
The Uses of Tubastatin A hydrochloride
Tubastatin A Hydrochloride is an LSD1 inhibitor, which targets SOX2-expressing cancer cells.
What are the applications of Application
Tubastatin A hydrochloride is an HDAC6 inhibitor
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.
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
Properties of Tubastatin A hydrochloride
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. |
Safety information for Tubastatin A hydrochloride
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation |
Precautionary Statement Codes |
P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. P332+P313:IF SKIN irritation occurs: Get medical advice/attention. P337+P313:IF eye irritation persists: Get medical advice/attention. |
Computed Descriptors for Tubastatin A hydrochloride
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