Triciferol acts as a multiple ligand with combined VDR agonist and HDAC antagonist activities. Triciferol binds directly to the VDR ( IC 50 =87 nM), and functions as an agonist with 1,25D-like potency on several 1,25D target genes. Triciferol induces marked tubulin hyperacetylation, and augments histone acetylation. Triciferol also exhibits efficacious antiproliferative and cytotoxic activities in cancer cell models in vitro [1].

Triciferol (0-10000 nM; 0-72 hours) significantly inhibits the growth of estrogen receptor-negative MDA-MB231 human breast cancer cells more effectively than 1,25D, with observable effects at concentrations as low as 1 nM. Additionally, treating MCF-7 cells with Triciferol (100-1000 nM) results in approximately 2.5 times more cell death compared to the same concentrations of 1,25D. [Cell Proliferation Assay; Cell Line: MDA-MB231; Concentration: 0-10000 nM; Incubation Time: 0-72 hours; Result: Marked growth reduction, significantly outperforming 1,25D from 1 nM concentration upwards.]