Vorinostat (SAHA) 99.96%

Vorinostat, also known as SAHA, is a potent histone deacetylase (HDAC) inhibitor used in epigenetics, oncology, cell cycle, apoptosis, and chromatin regulation research. It inhibits HDAC activity with a reported IC50 of approximately 10 nM in a cell-free assay and has demonstrated inhibitory activity against HDAC1 and HDAC3.

Vorinostat promotes histone hyperacetylation, particularly acetylation of histone H4, and is widely used to study transcriptional regulation, tumour cell growth inhibition, cell differentiation, apoptosis, and HDAC-dependent signalling pathways. It has been investigated in several cancer research models, including prostate cancer, breast cancer, multiple myeloma, and viral DNA amplification studies.

Key Features

• Potent HDAC inhibitor
• Also known as SAHA
• Reported HDAC IC50 of approximately 10 nM
• Inhibits HDAC1 and HDAC3
• Promotes hyperacetylation of histone H4
• Used in epigenetics and chromatin regulation research
• Studied in prostate cancer, breast cancer, multiple myeloma, and viral replication models
• Induces cell cycle changes, differentiation, and apoptosis in selected cell models
• Reported to abrogate productive HPV-18 DNA amplification
• For research use only

Target Profile

Biological Activity

Vorinostat inhibits HDAC activity and promotes accumulation of acetylated histones, resulting in changes in chromatin structure and gene expression regulation. In cell-based studies, Vorinostat has been shown to inhibit cancer cell proliferation, induce cell cycle arrest, promote differentiation, and trigger apoptosis depending on the cell model and treatment conditions.

In prostate cancer cell lines including LNCaP, PC-3, and TSU-Pr1, Vorinostat inhibits cell growth at micromolar concentrations and induces dose-dependent cell death in LNCaP cells. In MCF-7 breast cancer cells, Vorinostat inhibits proliferation with a reported IC50 of 0.75 µM, causing accumulation of cells in the G1 and G2-M phases of the cell cycle.

In Vitro Research Applications

Cell-Based Research Data

HDAC Assay Summary

Vorinostat has been evaluated using immunoprecipitation-HDAC assays. In this method, HDAC1 or HDAC3 immune complexes are prepared from Jurkat cell lysates and incubated with a radiolabelled histone H4 peptide substrate. HDAC inhibition is assessed by measuring released radiolabelled acetic acid.

In Vivo Research Summary

Vorinostat has been studied in mouse xenograft and neurological disease models. In CWR22 human prostate cancer xenografts in nude mice, Vorinostat administration produced dose-dependent tumour growth inhibition. In an R6/2 mouse model of Huntington’s disease, oral administration was reported to cross the blood-brain barrier, increase histone acetylation in the brain, and improve motor impairment in the model.

Research Findings Summary

Technical Summary

Storage and Handling Notes

Vorinostat should be handled as a research compound by trained laboratory personnel using appropriate chemical safety procedures.

Recommended handling considerations include:

• Store according to supplier recommendations
• Prepare stock solutions using a suitable solvent such as DMSO
• Aliquot stock solutions where repeated use is expected
• Avoid repeated freeze-thaw cycles of prepared solutions
• Protect compound solutions from unnecessary exposure to light and moisture
• Use appropriate PPE, including gloves, lab coat, and eye protection
• Dispose of chemical waste according to institutional safety procedures

Vorinostat / SAHA is a potent HDAC inhibitor used extensively in epigenetics, oncology, chromatin regulation, apoptosis, and cell cycle research. With nanomolar HDAC inhibitory activity, demonstrated effects on histone acetylation, tumour cell growth, differentiation, and apoptosis, it is a valuable research compound for studying HDAC-dependent mechanisms across cancer biology and related biomedical research models.