ligand
VH298
质量水平
检测方案
≥98% (HPLC)
形式
powder
反应适用性
reagent type: ligand
颜色
white to beige
溶解性
DMSO: 10 mg/mL, clear
储存温度
−20°C
生化/生理作用
VH298是一种细胞可透过性小分子，可破坏VHL与缺氧诱导因子HIF-α, 的相互作用，从而稳定HIF-α并诱导低氧反应。缺氧诱导因子 (HIFs) 是氧敏感的转录因子，可调节缺氧信号。它们受氧依赖性脯氨酰羟化酶结构域(PHD)酶调节，并由von Hippel-Lindau（VHL）Cullin RING E3泛素连接酶复合物进行多泛素化。与许多具有脱靶作用的PHD抑制剂不同，VH298在PHD酶的下游起作用，从而抑制VHL:HIF-α 互作。VH298的Kd为90 nM。VH298已表现出诱导HIF转录活性，可增加HIF-α在HeLa细胞中的积累，并刺激RCC4细胞中产生促红细胞生成素。
相关产品
产品编号
说明
价格
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Olena S Tokareva et al.
Nature communications, 14(1), 6992-6992 (2023-11-02)
Molecules that induce novel interactions between proteins hold great promise for the study of biological systems and the development of therapeutics, but their discovery has been limited by the complexities of rationally designing interactions between three components, and because known
Julianty Frost et al.
Nature communications, 7, 13312-13312 (2016-11-05)
Chemical strategies to using small molecules to stimulate hypoxia inducible factors (HIFs) activity and trigger a hypoxic response under normoxic conditions, such as iron chelators and inhibitors of prolyl hydroxylase domain (PHD) enzymes, have broad-spectrum activities and off-target effects. Here
Yong Hwan Kim et al.
Molecules (Basel, Switzerland), 29(2) (2024-01-23)
Autophagy is a pivotal biological process responsible for maintaining the homeostasis of intracellular organelles. Yet the molecular intricacies of peroxisomal autophagy (pexophagy) remain largely elusive. From a ubiquitin-related chemical library for screening, we identified several inhibitors of the Von Hippel-Lindau
Lauren M Meyers et al.
Toxicology and applied pharmacology, 445, 116041-116041 (2022-05-04)
Transcription factors HIF1 and HIF2 are central regulators of physiological responses to hypoxia and important for normal functioning of tissue stem cells and maintenance of healthy microvasculature. Even modest decreases in HIF activity exert detrimental effects in tissues although it
Misty Shuo Zhang et al.
Nature communications, 13(1), 954-954 (2022-02-19)
Hepatocellular carcinoma (HCC) invariably exhibits inadequate O2 (hypoxia) and nutrient supply. Hypoxia-inducible factor (HIF) mediates cascades of molecular events that enable cancer cells to adapt and propagate. Macropinocytosis is an endocytic process initiated by membrane ruffling, causing the engulfment of
我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.
联系技术服务部门