Photoreactive Histone Deacetylase (HDAC) Inhibitors
HDACs comprise a family of enzymes that regulate chromatin remodeling and gene transcription. They control critical cellular processes, including cell growth, cell cycle regulation, DNA repair, differentiation, proliferation, and apoptosis. Inhibitors of HDACs are powerful drug discovery tools, as they have been shown to inhibit tumor cell growth and induce differentiation and apoptosis. The HDAC inhibitors provided here utilize a novel approach through photoaffinity labeling to study HDAC activity and function.
Highlights
- Highly selective and specific compared to Trichostatin A (TSA) and suberoylanilide hydroxamic acid (SAHA)
- Highly pure (>95%, HPLC, LCMS)
- Photoreactive, suitable for photoaffinity labeling experiments
- Cell permeable and non-cytotoxic
Available Photoreactive HDAC Inhibitors
HDAC Inhibitor; V-91
V-91 is azole-based, and is selective for HDAC8. Selectivity of V-91 for the active site of HDAC8 was demonstrated by blocking it with SAHA.
HDAC3-Selective Inhibitor; HD-75
HD-75 is isoxazole-based, and specifically inhibits HDAC3. HD-75 is more selective for HDAC8 than SAHA, showing a 9-fold selectivity versus HDAC8.
HDAC8-Selective Inhibitor; HD-55
HD-55 is pyrazole-based, and specifically inhibits HDAC8 with superior selectivity compared to TSA and SAHA.
