Ivaltinostat (CG-200745) formic is an orally active, potent pan-HDAC inhibitor. It features a hydroxamic acid moiety that binds zinc at the bottom of the catalytic pocket. This compound inhibits the deacetylation of histone H3 and tubulin. It also induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat formic enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine and 5-Fluorouracil, induces apoptosis, and exhibits anti-tumour effects.
- Inhibits deacetylation of histone H3 and tubulin
- Induces accumulation of p53 and promotes p53-dependent transactivation
- Enhances expression of MDM2 and p21 (Waf1/Cip1) proteins
- Increases sensitivity of Gemcitabine-resistant cells to Gemcitabine and 5-Fluorouracil
- Induces apoptosis and exhibits anti-tumour effects