200 CHF CHF 200.00
AG-CR1-3904-M0011 mgCHF 200.00
AG-CR1-3904-M0055 mgCHF 800.00
|Synonyms||4-(Dimethylamino)-N-(5-(2-mercaptoacetamido)pentyl)benzamide; Mercaptoacetamide BC-4-55|
|Purity Chemicals||≥95% (HPLC)|
|Solubility||Soluble in DMSO, ethanol or methanol.|
|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 HDAC6 inhibitor (IC50 =114nM). Displays selectivity over other HDACs (IC50=1-8µM).
- Neuroprotective and anti-neuroinflammatory agent. Reduced neuronal degeneration after traumatic brain injury (TBI).
- Shown to increase histone H3 acetylation.
- 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.
- Chemistry and biology of mercaptoacetamides as novel histone deacetylase inhibitors: B. Chen, et al.; Bioorg. Med. Chem. Lett. 15, 1389 (2005)
- Functional differences in epigenetic modulators - Superiority of mercaptoacetamide-based histone deacetylase inhibitors relative to hydroxamates in cortical neuron neuroprotection studies: A. Kozikowski, et al.; J. Med. Chem. 50, 3054 (2007)
- In vitro plasma stability, permeability and solubility of mercaptoacetamide histone deacetylase inhibitors: R. Konsoula & M. Jung; Int. J. Pharm. 361, 19 (2008)
- HDAC inhibitor increases histone H3 acetylation and reduces microglia inflammatory response following traumatic brain injury in rats: B. Zhang, et al.; Brain Res. 1226, 181 (2008)
- Novel inhibitors of human histone deacetylase (HDAC) identified by QSAR modeling of known inhibitors, virtual screening, and experimental validation: H. Tang, et al.; J. Chem. Inf. Model 49, 461 (2009)