Triciferol |
Catalog No.GC61947 |
트리시페롤은 결합된 VDR 작용제 및 HDAC 길항제 활성과 함께 다중 리간드로 기능합니다. 트리시페롤은 VDR(IC50=87nM)에 직접 결합하고 여러 1,25D 표적 유전자에 대해 1,25D 유사 효능을 갖는 작용제로 기능합니다. 트리시페롤은 현저한 튜불린 과아세틸화를 유도하고 히스톤 아세틸화를 증가시킵니다. 항증식 및 세포독성 활동.
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Cas No.: 957214-00-5
Sample solution is provided at 25 µL, 10mM.
Triciferol functions as a multiple ligand with combined VDR agonist and HDAC antagonist activities. Triciferol binds directly to the VDR (IC50=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[1].
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[1].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[1].
References:
[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.
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