4'-bromo-Resveratrol (Synonyms:4'-溴-白藜芦醇;4′‐BR)
目录号 : KCM10736 CAS No. : 1224713-90-9 纯度 : ≥98%
4’-bromo-Resveratrol is a potent inhibitor of the deacetylases sirtuin 1 (SIRT1) and 3 (SIRT3). It is a brominated derivative of resveratrol, a polyphenol found in red wine, which activates SIRT1 and inhibits SIRT3. The use of 4’-bromo-resveratrol in an SIRT3 crystal binding study revealed two compound binding sites which, combined with homology modeling, suggested that the second site may account for the paradoxical activation of SIRT1 by unmodified resveratrol.
规格 价格 是否有货 数量
10mg
In-stock
50mg
In-stock
100mg
In-stock
10 mM * 1 mL in DMSO
In-stock

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生物活性

4'-Bromo-resveratrol is a dual SIRT1/SIRT3 inhibitor with an IC50 of 0.2 mM for both targets. 4'-Bromo-resveratrol induces caspase-dependent apoptosis, induces G0/G1 cell cycle arrest, and inhiibits proliferation. 4'-Bromo-resveratrol reduces lactate production, glucose uptake, and NAD+/NADH ratio, and downregulates lactate dehydrogenase A and glucose transporter 1 (GLUT1). 4'-Bromo-resveratrol can be used for the research of melanoma.

IC50&Target

SIRT1                               SIRT3                               Caspase 3            Caspase 8          GLUT1       LDHA

0.2 mM (IC50)                 0.2 mM (IC50)

体外研究

4 '- Bromo resveratrol (0.0125-0.2 mM; 24-72 h) can dose - and time-dependent inhibit the proliferation and survival of G361, SK-MEL-28, and SK-MEL-2 human melanoma cells.
4 '- Bromo resperatrol (0.0125-0.2 mM; 48 h) can dose dependently damage the clonal survival ability of G361, SK-MEL-28, and SK-MEL-2 human melanoma cells.
4 '- Bromo resveratrol (0.0125-0.05 mM; 24-72 h) can induce apoptosis in G361, SK-MEL-28, and SK-MEL-2 human tumor cells in a dose - and time-dependent manner, resulting in morphological changes of apoptosis, including nuclear condensation and fragmentation.
4 '- Bromo resparatrol (0.05 mM; 48 h) was used to induce Cyclin D1 and CDK6 inhibition through P21, mediating G0/G1 phase arrest in G361, SK-MEL-28, and SK-MEL-2 human melanoma cells.
4 '- Bromo resveratrol (0.05 mM; 48 h) can reduce the expression of glycolysis related proteins LDHA and GLUT1 in G361, SK-MEL-28, and SK-MEL-2 human melanoma cells.
4 '- Bromo resveratrol (0.05 mM; 48 h) significantly inhibited the migration of G361, SK-MEL-28, and SK-MEL-2 human melanoma cells.
4 '- Bromo resveratrol (0.025-0.05 mM; 48 h) can dose dependently inhibit aerobic glycolysis in G361, SK-MEL-28, and SK-MEL-2 human melanoma cells, reducing lactate production, glucose uptake, and NAD+/NADH ratio.

 

Cell Proliferation Assay

Cell Line: G361, SK-MEL-28, SK-MEL-2 cells
Concentration: 0.0125, 0.025, 0.05, 0.1, 0.2 mM
Incubation Time: 24,48,72 hours
Result: Inhibited melanoma cell proliferation and viability in a dose- and time-dependent manner. Caused massive reduction in proliferation at 0.1 mM and 0.2 mM. Induced appreciable growth inhibition at 0.025 mM, with statistically significant differences compared to vehicle control.

Apoptosis Analysis

Cell Line: G361, SK-MEL-28, SK-MEL-2
Concentration: 0.0125, 0.025, 0.05 mM
Incubation Time: 24,48,72 hours
Result:

Increased the percentage of apoptotic cells across all three melanoma cell lines in a doseand time-dependent manner. Showed statistically significant differences compared to vehicle control.

Cell Cycle Analysis

Cell Line: G361, SK-MEL-28, SK-MEL-2
Concentration: 0.05 mM
Incubation Time: 48 hours
Result: Caused a significant increase in the percentage of cells in the G0/G1 phase across all three melanoma cell lines. Induced a concomitant decrease in the G2/M phase population across all three melanoma cell lines. Showed statistically significant differences compared to vehicle control.

Western Blot Analysis

Cell Line: G361, SK-MEL-28, SK-MEL-2
Concentration: 0.05 mM
Incubation Time: 48 hours
Result: Decreased protein levels of procaspase-3 and procaspase-8. Increased levels of cleaved caspase-3. Induced cleavage of full-length PARP (116 kDa) to its 89 kDa cleaved product. Significantly diminished expression of PCNA across all three melanoma cell lines.\nAttenuated protein levels of Cyclin D1 and CDK6 across all three melanoma cell lines. Induced expression of the CDK inhibitor P21 across all three melanoma cell lines.\nSignificantly decreased protein levels of lactate dehydrogenase A (LDHA) across all three melanoma cell lines. Reduced expression of glucose transporter 1 (GLUT1) across all three melanoma cell lines.
分子式
C14H11BrO2
分子量
291.1
CAS号
1224713-90-9
中文名称
5-[(E)-2-(4-溴苯基)乙烯基]间苯二酚;5-[(1E)-2-(4-溴苯基)乙烯基]-1,3-苯二酚
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO: 250 mg/mL (858.69 mM; Need ultrasonic)

配制储备液
                                           
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
                                                                                                                    
1 mM 3.4348 mL 17.1739 mL 34.3477 mL
5 mM 0.6870 mL 3.4348 mL 6.8695 mL
10 mM 0.3435 mL 1.7174 mL 3.4348 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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