2. JAK/STAT Signaling Stem Cell/Wnt Apoptosis Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. STAT Bcl-2 Family Ser/Thr Kinase Survivin c-Myc Apoptosis Necroptosis CDK
  4. Bruceantinol

Bruceantinol 可以从 Brucea javanica 中分离出来的一种类木素，能够抑制辣椒中的辣椒斑驳病毒 (PepMoV)。Bruceantinol 是一种 STAT3 抑制剂，在体外和体内人类结直肠癌 (CRC) 模型中表现出强效的抗肿瘤活性。Bruceantinol 还具有强效的抗白血病活性。Bruceantinol 能够强烈抑制 STAT3 的 DNA 结合能力 (IC50 = 2.4 pM)，阻断组成型和 IL-6 诱导的 STAT3 激活，并抑制 MCL-1、PTTG1、Survivin 和 c-Myc 的转录。Bruceantinol 与 CDK2/4/6 结合，通过蛋白酶体途径促进蛋白质降解。Bruceantinol 可以剂量和时间依赖性地降低细胞生长，阻碍细胞增殖，扰乱细胞周期，并诱导 MCF-7 细胞坏死 (necrosis) 和 MDA-MB-231 细胞凋亡 (apoptosis)。

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Bruceantinol

Bruceantinol Chemical Structure

CAS No. : 53729-52-5

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Bruceantinol 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Bruceantinol is a quassinoid that can be isolated from Brucea javanica, inhibits pepper mottle virus (PepMoV) in pepper. Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol has potent anti-leukemic activity. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC50 = 2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc. Bruceantinol binds with CDK2/4/6 to facilitate protein degradation through proteasome pathway. Bruceantinol can dose- and time-dependently reduces the cell growth, impede cell proliferation, disrupts the cell cycle, and induces necrosis in MCF-7 cells and apoptosis in MDA-MB-231 cells[1][2][3].

IC50 & Target

IC50: 2.4 pM (STAT3 DNA-binding ability)[2]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HCT-116 IC50
0.05 μM
Compound: 9e
Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by WST-1 assay
Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by WST-1 assay
[PMID: 33289552]
MCF7 IC50
0.063 μM
Compound: 9e
Cytotoxicity against human MCF-7 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human MCF-7 cells incubated for 72 hrs by MTT assay
[PMID: 33289552]
MDA-MB-231 IC50
0.088 μM
Compound: 9e
Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay
[PMID: 33289552]
体外研究
(In Vitro)

Bruceantinol (Compound 4) (5-40 μM) 对 PepMoV 表现出强烈的灭活作用，在 C. annuum 中的最低抑菌浓度为 10 μM[1]。
Bruceantinol (Compound BOL) (0-100 nM，24 小时) 以剂量依赖性方式显著降低人类 CRC 细胞系(HCT116、HCT116 p53-/-、HCA-7、H630 和 H630R1) 中的菌落形成[2]。
Bruceantinol (300 nM，24 小时) 可改变 HCT116 细胞中 25 种蛋白质 (p-STAT3、MCL-1、c-Myc 和裂解的 caspase-7) 的表达，其中 STAT3 介导的信号通路受到显著抑制[2]。
Bruceantinol (30 nM，0-24 小时) 可抑制 HCT116 细胞中的 STAT3 磷酸化[2]。
Bruceantinol (10-300 nM，24 小时) 可有效抑制 IL-6 诱导的 CRC 细胞中 STAT3 的激活[2]。
Bruceantinol (0-1000 nM，24 小时) 以剂量依赖性方式显著降低 MCL-1、c-Myc 和 survivin 的表达[2]。
Bruceantinol (0-1600 nM，24-48 小时) 可抑制乳腺癌细胞 (MCF-7 和 MDA-MB-231) 的生长[3]。
Bruceantinol (100-400 nM，24 小时) 可导致 MCF-7 和 MDA-MB-231 细胞中 G0/G1 期细胞数量逐渐减少，S 期和 G2/M 期细胞数量相应增加[3]。
Bruceantinol (100-400 nM，10 小时) 可通过蛋白酶体途径降低 MCF-7 和 MDA-MB-231 细胞中的 CDK2/4/6 蛋白水平[3]。

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

Bruceantinol 相关抗体:

Cell Proliferation Assay[2]

Cell Line: HCT116, HCT116 p53-/-, HCA-7, SW480, SW48, SW48G12D, RKO, H630 and H630R1
Concentration: 0, 10, 30, 100 nM
Incubation Time: 24 h
Result: Suppressed cell growth to the greatest extent across the human CRC cell line panel.
体内研究
(In Vivo)

Bruceantinol (Compound BOL) (2-4 mg/kg，腹腔注射，每周三次) 可抑制携带 HCT 116 异种移植瘤的小鼠的 p-STAT3 表达[2]。

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

Animal Model: Athymic nude female mice (6-7 w) bearing HCT 116 xenografts[2]
Dosage: 2 and 4 mg/kg
Administration: Intraperitoneal injection (i.p.) thrice a week
Result: Inhibited p-STAT3 expression 32% and 80% with 2 and 4 mg/kg, respectively.
Exhibited potent suppression of the STAT3-associated targets, c-Myc, and surviving.
Resulted in a significant reduction in Ki67 expression and increased TUNEL staining in a dose-dependdent manner.
分子量

606.61

Formula

C30H38O13
CAS 号
性状

固体

颜色

White to light yellow

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献

Bruceantinol 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.

Keywords:

Bruceantinol53729-52-5STATBcl-2 FamilySer/Thr KinaseSurvivinc-MycApoptosisNecroptosisCDKProtein Serine-Threonine KinaseMycCyclin dependent kinaseInhibitorinhibitorinhibit

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