Highly fluorescent and HDAC6 selective scriptaid analogues.

Affiliation

School of Life & Environmental Sciences, Deakin University, Waurn Ponds, Victoria, 3216, Australia. Electronic address: [Email]

Abstract

Fluorescent scriptaid analogues with excellent HDAC6 selectivity (HDAC1/6 > 500) and potency (HDAC6 IC50 < 5 nM) have been synthesised and evaluated. The highly fluorescent nature of the compounds (up to ΦF = 0.83 in DMSO and 0.38 in aqueous buffer) makes them ideally suited for cellular imaging and visualisation of their cytoplasmic localisation was readily accomplished. Whole organism imaging in zebrafish confirmed both the vascular localisation of the new inhibitors and the impact of HDAC6 inhibition on in vivo development.

Keywords

4MS,Fluorescence,HDAC,Imaging,Naphthalimide,Scriptaid,Zebrafish,