90 CHF CHF 90.00
AG-CR1-3900-M01010 mgCHF 90.00
|Purity Chemicals||≥98% (HPLC)|
|Solubility||Soluble in DMSO.|
|Identity||Determined by 1H-NMR.|
|Shipping and Handling|
|Short Term Storage||+4°C|
|Long Term Storage||-20°C|
Keep cool and dry.
Protect from light.
|Use/Stability||Stable for at least 2 years after receipt when stored at -20°C.|
|Product Specification Sheet|
- 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.
- 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.
- 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)