1. Epigenetics
  2. MicroRNA
  3. Rubone

Rubone 是一种查耳酮类似物,是 miR-34a 的调节剂。Rubone 以 p53 依赖性方式上调 miR-34a 表达,下调下游靶标 Bcl-2 和细胞周期蛋白 D1 表达,并抑制体内肝细胞癌 (HCC) 的生长。Rubone 通过逆转 miR-34a 下游靶标的表达来增强紫杉醇 (PTX; HY-B0015) 在 PTX 耐药的前列腺癌细胞系中的抗癌作用。

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Rubone Chemical Structure

Rubone Chemical Structure

CAS No. : 73694-15-2

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规格 价格 是否有货 数量
5 mg ¥1601
3 - 4 周
10 mg   询价  
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Rubone, a chalcone analog, is a modulator of miR-34a. Rubone upregulates miR-34a expression in a p53 dependent manner, downregulates the downstream target Bcl-2 and Cyclin D1 expression, and suppresses hepatocellular carcinoma (HCC) growth in vivo. Rubone enhances the anticancer effect of Paclitaxel (PTX; HY-B0015) in PTX-resistant prostate cancer cell lines by reversing the expression of miR-34a downstream targets[1][2][3].

体外研究
(In Vitro)

Rubone (0-60 μM) 在 DU145-TXR 和 PC3-TXR 细胞中表现出显着的细胞毒性,表明 Rubone 在晚期前列腺癌细胞中具有更强的抗癌作用,这些细胞具有较低的 miR-34a 表达[3]
Rubone (5, 10 uM; 48 小时) 显着逆转 DU145-TXR 和 PC3-TXR 细胞系的 miR-34a 下游基因靶标的表达。Rubone 以剂量依赖性方式上调 PTX 抗性 DU145-TXR 和 PC3-TXR 细胞系中的 miR-34a
[3]。
Rubone (5 μM; 持续 2 周) 和 PTX (持续 2 周) 联合疗法抑制 3D 模型中的 PC3-TXR 细胞生长和球体形成,包括顶部 3D 和悬滴模型。Rubone 和 PTX 联合疗法抑制 p53 独立途径中的细胞侵袭、迁移和癌症干细胞样细胞 (CSC) 种群。Rubone 单一疗法或 Rubone 与 PTX 组合可显着增强 TAp73 和 Elk-1 的表达
[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[3]

Cell Line: DU145, PC3, PTX resistant DU145-TXR, PC3-TXR, LNCaP, LNCaP developed C4-2 cells
Concentration: 0-60 μM
Incubation Time:
Result: Exhibited significantly higher cytotoxicity in DU145-TXR and PC3-TXR cells.

Western Blot Analysis[3]

Cell Line: DU145-TXR and PC3-TXR cell lines
Concentration: 5, 10 uM
Incubation Time: 48 h
Result: Significantly reversed the expression of miR-34a downstream gene targets of DU145-TXR and PC3-TXR cell lines, including E-cadherin, SIRT1, and Cyclin D1, whereas E-cadherin expression was not reversed in DU145-TXR cell line.

Real Time qPCR[3]

Cell Line: DU145-TXR and PC3-TXR cell lines
Concentration: 5, 10 uM
Incubation Time: 48 h
Result: Upregulated miR-34a in PTX-resistant DU145-TXR and PC3-TXR cell lines in a dose dependent manner.
体内研究
(In Vivo)

Rubone 单一疗法 (装载 20 mg/kg 的 PEG-PCD 胶束; 每隔一天静脉注射; 共五剂) 或与 PTX 联合治疗 (PEG-PCD 胶束装载每种药物 10 mg/kg) 显着上调肿瘤中的 miR-34a 表达。联合疗法抑制肿瘤生长。Rubone 单一疗法未能抑制肿瘤细胞增殖[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 8 weeks old male nude mice transfected prostate cancer cells[3]
Dosage: 20 mg/kg or 10 mg/kg for each drug (PTX and Rubone) loaded PEG-PCD micelles
Administration: Intravenously for five doses every other day
Result: Had little effect on body weight loss and inhibited tumor growth.
Monotherapy or combination therapy with PTX significantly upregulated miR-34a expression in tumor.
Alone or with PTX significantly reversed E-cadherin, Cyclin D1, and SIRT1 expression.
分子量

374.38

Formula

C20H22O7

CAS 号
结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

Rubone 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HY-119833
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