Description
2-
hexyl-
4-
Pentynoic acid is a derivative of valproic acid , an inhibitor of histone deacetylases (HDACs). It inhibits HDAC activity more potently (IC
50 = 13 μM) than valproic acid (IC
50 = 398 μM). 2-
hexyl-
4-
Pentynoic acid induces histone hyperacetylation in cerebellar granule cells significantly at 5 μM. It also induces the expression of heat shock proteins Hsp70-
1a and Hsp70-
1b and protects cerebellar granule cells from glutamate-
induced excitotoxicity when used at a concentration of 50 μM.
References
1) Eikel et al. (2006), Teratogenic effects mediated by inhibition of histone deacetylases: evidence from quantitative structure activity relationships of 20 valproic acid derivatives; Chem. Res. Toxicol., 19 272
2) Leng et al. (2010), Potent neuroprotective effects of novel structural derivatives of valproic acid: potential roles of HDAC inhibition and HSP70 induction; Neurosci. Lett., 476 127