1. NF-κB Apoptosis
  2. NF-κB Apoptosis Caspase
  3. Berubicin hydrochloride

Berubicin hydrochloride  (Synonyms: RTA 744; WP 744; WP 769 hydrochloride)

目录号: HY-14942A 纯度: 95.08%
COA 产品使用指南 技术支持

Berubicin (RTA 744) hydrochloride 是一种可穿过血脑屏障的 Doxorubicin (HY-15142A) 的类似物。Berubicin hydrochloride 可抑制 P-gp 和 MRP1 介导的外排,并抑制多形性胶质母细胞瘤 (GBM) 生长。Berubicin hydrochloride 通过激活核因子 κB (NF-κB) 对白血病细胞产生细胞毒性作用,并诱导了神经母细胞瘤细胞凋亡 (apoptosis)。Berubicin hydrochloride 可用于神经系统相关的肿瘤研究。

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Berubicin hydrochloride

Berubicin hydrochloride Chemical Structure

CAS No. : 293736-67-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Berubicin (RTA 744) hydrochloride is a Doxorubicin (HY-15142A) analog that can cross the blood-brain barrier. Berubicin hydrochloride inhibits P-gp and MRP1-mediated efflux and suppresses glioblastoma multiforme (GBM). Berubicin hydrochloride exerts toxic effects on leukemia cells by activating nuclear factor κB (NF-κB) and induces apoptosis in neuroblastoma cells. Berubicin hydrochloride can be used in the study of tumors related to the nervous system[1][2][3][4][5].

体外研究
(In Vitro)

Berubicin (0.1-10 μM, 0-5 d) hydrochloride 在抑制 SH-SY5Y 细胞生长方面比 Doxorubicin (Dox) 更有效[2]
Berubicin (0-10 μM, 0-48 h) hydrochloride 在较低药物浓度下通过 caspase-9 和-3 依赖性途径诱导细胞凋亡并激活 NF-κB,而在 SH-SY5Y 细胞中,较高浓度下其他细胞死亡机制可能占主导地位[2]
Berubicin (0-100 μM, 24 h) hydrochloride 抑制三种 AML 细胞系 K562、KBM-3、OCIM2 和 KBM-5细胞,IC50 分别为 0.18、< 0.05、< 0.05 μg/mL 和 0.5 μM[3][4]
Berubicin (0-10 μM, 0-8 h) hydrochloride 在抑制 DNA 合成 (IC50 = 0.2 μM)、激活 NF-κB 和降解 KBM-5 细胞的 IkBα 方面比 Dox 更有效[4]

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

Apoptosis Analysis[2]

Cell Line: SH-SY5Y cells
Concentration: 0.05, 0.5 and 5 μM
Incubation Time: 48 h
Result: \Induced significantly higher apoptosis at 500 nM than Dox, but higher concentrations of the drug reduced the apoptosis-inducing effect.

Western Blot Analysis[2]

Cell Line: SH-SY5Y cells
Concentration: 0, 0.1, 1.0 or 10 µM
Incubation Time: 0, 0.5, 1, 2, 4, 6, 8, 12 or 24 h
Result: Observed a caspase-9 cleavage band as early as 0.5 h after drug treatment and accumulated to highest levels after 12 h, and caspase-3 cleavage was seen as early as 8 h.
Did not express caspase 8, and there was no increase or decrease in caspase 7 expression.
Significantly increased p53 levels, whereas Dox had no such effect and p21 expression increased with increased p53.
Significantly reduced mitochondrial AIF and nuclear AIF accumulation increases over time.
Showed 50 times more potent than Dox in activating NF-κB.
Downregulated the expression of IκBα, Bcl-w, Bcl-XL and cyclin D1.

Western Blot Analysis[4]

Cell Line: KBM-5 cells
Concentration: 0, 0.1, 1 and 10 µM
Incubation Time: 0, 5, 10, 15, 30, 60, 120, 240, 480 min
Result: Was most active, reaching maximum activation in activating NF-kβ and degradation of IkBαat a 1 μM concentration, and Doxorubicin least active, reaching maximum at 50 μM.
体内研究
(In Vivo)

Berubicin hydrochloride 与 Temozolomide (HY-17364) 相比延长了小鼠颅内原位胶质瘤模型的生存时间[5]

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

Clinical Trial
分子量

670.10

Formula

C34H36ClNO11

CAS 号
性状

固体

颜色

Brown to red

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

纯度 & 产品资料
参考文献
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Help & FAQs
  • 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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Berubicin hydrochloride
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HY-14942A
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