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AdipoGen Life Sciences
Tubastatin A
90
CHF
CHF 90.00
In stock
AG-CR1-3900-M01010 mgCHF 90.00
| Product Details | |
|---|---|
| Synonyms | N-hydroxy-4-[(1,2,3,4-tetrahydro-2-methyl-5H-pyrido[4,3-b]indol-5-yl)methyl] benzamide |
| Product Type | Chemical |
| Properties | |
| Formula |
C20H21N3O2 |
| MW | 335.4 |
| CAS | 1252003-15-8 |
| Purity Chemicals | ≥98% (HPLC) |
| Appearance | Off-white solid. |
| Solubility | Soluble in DMSO. |
| Identity | Determined by 1H-NMR. |
| InChi Key | GOVYBPLHWIEHEJ-UHFFFAOYSA-N |
| Smiles | CN1CCC2=C(C1)C1=CC=CC=C1N2CC1=CC=C(C=C1)C(=O)NO |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice |
Keep cool and dry. Protect from light. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- Cell permeable potent and selective class IIb histone deacetylase 6 (HDAC6) inhibitor (IC50=15nM, >1000-fold selective against other HDACs and 60-fold for HDAC8).
- Neuroprotective. Effectively prevents neuronal cell death (by ≥95% at 10µM) upon oxidative stress induction by HCA and selectively induces cellular α-tubulin, but not histone H4, hyperacetylation (2.5 to 5µM) in primary rat cortical neuron cultures.
- Improves cognition in Alzheimer's disease transgenic mice.
- Exhibits cardioprotective and anticancer chemotherapeutic activities. Reduces tumor growth and cell proliferation and induces cell cycle arrest in G1.
- Inhibits TNFα (IC50=272nM) and IL-6 (IC50=712nM) in LPS-stimulated human THP-1 macrophages and displays anti-inflammatory activity in animal models.
- Antileishmanial.
- HDAC6 deacetylates tubulin, HSP90 and the core histones (H2A, H2B, H3, H4). Histone deacetylases act via the formation of large multiprotein complexes. HDAC6 plays an important role in microtubule-dependent cell motility, transcriptional regulation, degradation of misfolded proteins and cell cycle and is involved in autophagy, inflammation, cancer and neurodegeneration.
Product References
- Rational design and simple chemistry yield a superior, neuroprotective HDAC6 inhibitor, tubastatin A: K.V. Butler, et al.; JACS 132, 10842 (2010)
- Histone deacetylase 6 and heat shock protein 90 control the functions of Foxp3(+) T-regulatory cells: E.F. de Zoeten, et al.; Mol. Cell Biol. 31, 2066 (2011)
- Second-generation histone deacetylase 6 inhibitors enhance the immunosuppressive effects of Foxp3+ T-regulatory cells: J.H. Kalin, et al.; J. Med. Chem. 55, 639 (2012)
- Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth: J.A. Bergman, et al.; J. Med. Chem. 55, 9891 (2012)
- HDAC6 inhibition restores ciliary expression and decreases tumor growth: S.A. Gradilone, et al.; Cancer Res. 73, 2259 (2013)
- Tubastatin, a selective histone deacetylase 6 inhibitor shows anti-inflammatory and anti-rheumatic effects: S. Vishwakarma, et al.; Int. Immunopharmacol. 16, 72 (2013)
- HDAC6 inhibition results in tau acetylation and modulates tau phosphorylation and degradation in oligodendrocytes: M. Noack, et al.; Glia 62, 535 (2014)
- Histone deacetylase 6 inhibition improves memory and reduces total tau levels in a mouse model of tau deposition: M.L. Selenica, et al.; Alzheimers Res. Ther. 6, 12 (2014)
- Tubastatin A/ACY-1215 improves cognition in Alzheimer's disease transgenic mice: L. Zhang, et al.; J. Alzheimers Dis. 41, 1193 (2014)
- Selective inhibitor of histone deacetylase 6 (tubastatin A) suppresses proliferation of hepatitis C virus replicon in culture of human hepatocytes: M.V. Kozlov, et al.; Biochem. 79, 637 (2014)
- The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors: Q. Sodji, et al.; Bioorg. Med. Chem. Lett. 24, 4826 (2014)
- Targeting histone deacetylase 6 mediates a dual anti-melanoma effect: Enhanced antitumor immunity and impaired cell proliferation: K.V. Woan, et al.; Mol. Oncol. 9, 1447 (2015)
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