4'-bromo-Resveratrol

4'-Bromo-resveratrol 是Sirtuin-1和Sirtuin-3的双重抑制剂。它通过线粒体代谢重编程,使黑色素瘤细胞的生长受到抑制。它通过代谢重编程、影响细胞周期以及细胞凋亡的信号传导,使其在黑色素瘤细胞中发挥抗增殖作用。

CAS号

1224713-90-9

分子式

C14H11BrO2

主要靶点

Sirtuin

仅限科研使用

Cat No : CM17582

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Synonyms



产品信息

4'-bromo-Resveratrolis a potent inhibitor of the deacetylases sirtuin 1 (SIRT1) and 3 (SIRT3)

CAS号 1224713-90-9
分子式 C14H11BrO2
主要靶点 Sirtuin
主要通路 表观遗传|DNA损伤和修复
分子量 291.14
纯度 99.40%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

体外活性

4'-BR treatment of melanoma cells resulted in (a) decrease in proliferation and clonogenic survival;?(b) induction of apoptosis accompanied by a decrease in procaspase-3, procaspase-8, and increase in the cleavage of caspase-3 and poly (ADP-ribose) polymerase (PARP);?(c) marked downregulation of proliferating cell nuclear antigen (PCNA);?and (d) inhibition of melanoma cell migration.?Further, 4'-BR caused a G0/G1 phase arrest of melanoma cells that was accompanied by an increase in WAF-1/P21 and decrease in Cyclin D1/Cyclin-dependent kinase 6 protein levels.?4'-BR causes a decrease in lactate production, glucose uptake, and NAD+ /NADH ratio.?These responses were accompanied by downregulation in lactate dehydrogenase A and glucose transporter 1 in melanoma cells.[1]

溶解度

DMSO:30 mg/mL (103.04 mM)

参考文献

1.George J ,  Nihal M ,  Singh C K , et al. 4′‐Bromo‐resveratrol, a dual Sirtuin‐1 and Sirtuin‐3 inhibitor, inhibits melanoma cell growth through mitochondrial metabolic reprogramming[J]. Molecular Carcinogenesis, 2019, 58.
2.Nguyen G ,  Gertz M ,  Steegborn C . Crystal Structures of Sirt3 Complexes with 4′-Bromo-Resveratrol Reveal Binding Sites and Inhibition Mechanism[J]. Chemistry & Biology, 2013, 20(11):1375-1385.

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