hdacs

Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that suppresses HDAC1 activity and induces HDAC2 degradation, exhibiting oral bioavailability. Valproic Acid activates Notch1 signalling and inhibits the proliferation of small cell lung carcinoma cells, making it applicable for research into epilepsy and bipolar disorder.

Parthenolide ((-)-Parthenolide) is a natural sesquiterpene lactone that is an NF-κB inhibitor and also specifically inhibits HDAC1 protein, but is inactive against other class I/II HDACs. Parthenolide has anti-inflammatory, anti-tumor, and anti-viral activities.

1-Alaninechalmydocin is a fungal metabolite originally isolated from a Great Lakes-derived Tolypocladium sp. and an inhibitor of histone deacetylases (HDACs). It reduces total HDAC activity in HeLa cell lysates in a concentration-dependent manner. 1-Alaninechlamydocin reduces proliferation of MIA PaCa-2, PANC-1, and hTERT-HPNE cells (GI50s = 5.3, 14, and 2.0 nM, respectively).

OKI-006, a potent and orally active histone deacetylase (HDAC) inhibitor, stands as a distinctive derivative of the natural product HDAC inhibitor, largazole. By targeting HDACs—key players in epigenomic regulation whose dysfunction often occurs in numerous human cancers—OKI-006 holds promise for cancer research applications [1].

Homobutein (3-O-Methylbutein) is a dual inhibitor of HDACs and NF-κB with IC50s of 190 and 38 μM. Homobutein is an iron chelator with anticancer, anti-inflammatory, antiparasite, and antioxidation activities.