Triciferol functions 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. Antiproliferative and cytotoxic activities.
性状
Solid
体外研究(In Vitro)
Triciferol (0-10000 nM; 0-72 hours) is significantly more efficacious in suppressing the proliferation of estrogen receptor-negative human MDA-MB231 breast cancer cells.Treatment of MCF-7 cells with Triciferol (100-1000 nM) induces ≈2.5-fold higher rates of cell death than equimolar amounts of 1,25D. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
参考文献
[1]. Tavera-Mendoza LE, et al. Incorporation of histone deacetylase inhibition into the structure of a nuclear receptor agonist. Proc Natl Acad Sci U S A. 2008;105(24):8250-8255.
溶解度数据
In Vitro: DMSO : 100 mg/mL (232.78 mM; Need ultrasonic)配制储备液