1. PI3K/Akt/mTOR MAPK/ERK Pathway Stem Cell/Wnt JAK/STAT Signaling Apoptosis
  2. PI3K Akt p38 MAPK STAT Apoptosis
  3. Isocucurbitacin B

Isocucurbitacin B 是一种被发现存在于甜瓜 (Pedicellus melo) 中的天然萜类化合物。Isocucurbitacin B 能够抑制 PI3K/AKTMAPKSTAT3 信号通路并下调 CAV1 表达。Isocucurbitacin B 能够抑制癌细胞的增殖、迁移和侵袭。Isocucurbitacin B 能够诱导细胞凋亡 (apoptosis) 并导致 G2/M 期阻滞。Isocucurbitacin B 能够降低细胞内胆固醇和 pH 值,并升高细胞内钙离子水平。Isocucurbitacin B 可用于癌症的研究,如胶质瘤。

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Isocucurbitacin B

Isocucurbitacin B Chemical Structure

CAS No. : 17278-28-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Isocucurbitacin B is a natural terpenoid compound found in Pedicellus Melo. Isocucurbitacin B can inhibit the PI3K/AKT, MAPK, and STAT3 signaling pathways and downregulate CAV1 expression. Isocucurbitacin B can inhbit cancer cell proliferation, migration and invision. Isocucurbitacin B can induce apoptosis and cause G2/M phase arrest. Isocucurbitacin B can decrease intracellular cholesterol and PH levels and increase intracellular calcium levels. Isocucurbitacin B can be used for the research of cancer, such as glioma[1][2].

IC50 & Target[1]

STAT3

 

体外研究
(In Vitro)

Isocucurbitacin B (0.001-25 μmol/L;12-24 小时) 抑制 U251 和 U87 细胞增殖[1][2]
Isocucurbitacin B (0-1 μmol/L;24 小时) 诱导 U251 和 GL261 细胞凋亡[1][2]
IsoCuB (0-1 μmol/L;24 小时) 在 U251 细胞中阻滞 G2/M 周期,减少 cyclin A2 和 CDK1 的表达[2]
Isocucurbitacin B (0-0.1 μmol/L;12-36 小时) 抑制 U251 和 GL261 细胞迁移和侵袭,降低 MMP2、N-cadherin 和 vimentin 的水平[1][2]
Isocucurbitacin B (0-0.1 μmol/L;24 小时) 抑制 U251 和 GL261 细胞侵袭[1][2]
Isocucurbitacin B (0-1 μmol/L;24 h) 抑制 U251 细胞中 PI3K/AKT,MAPK 和 STAT3 信号通路的激活[1]
Isocucurbitacin B (0-1 μmol/L;24 h) 下调 U251 细胞中的 pdk1,RXRα,PPAα 和 Bcl-2 mRNA 表达[1]
Isocucurbitacin B (0-1 μmol/L;24 小时) 降低 U251 细胞内胆固醇和 pH 水平,并提高细胞内钙离子水平[2]

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

Cell Proliferation Assay[12]

Cell Line: U251 and U87 cells
Concentration: 0.001, 0.01, 0.1, 0.5, 1, 5, 25 μmol/L
Incubation Time: 12 h, 24 h
Result: Inhibited U251 and U87 cell proliferation in a concentration- and time-dependent manner.

Apoptosis Analysis[12]

Cell Line: U251 and GL261 cells
Concentration: 0, 0.1, 0.5, 1 μmol/L
Incubation Time: 24 h
Result: Promoted the apoptosis of U251 and GL261 cells in a concentration-dependent manner. Increaseed BCL-2 amd BAX levels.

Cell Migration Assay [12]

Cell Line: U251 and GL261
Concentration: 0, 0.001, 0.01, 0.005, 0.1 μmol/L
Incubation Time: 12 h, 24 h, 36 h
Result: Inhibited the migration of U251 and GL 261 cells in a concentration- and time-dependent manner.

Cell Invasion Assay[12]

Cell Line: U251 and GL261
Concentration: 0, 0.001, 0.01, 0.05, 0.1 μmol/L
Incubation Time: 24 h
Result: Inhibited the invasion of U251 and GL261 cells in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: U251
Concentration: 0, 0.1, 0.5, 1 μmol/L
Incubation Time: 24 h
Result: Inhibited the activation of the PI3K/AKT, MAPK, and STAT3 signaling pathways by decreasing the levels of p-MAPK1/3, total PI3K, t-AKT, PDK1, and p-STAT3 proteins.

Real Time qPCR[1]

Cell Line: U251
Concentration: 0, 0.1, 0.5, 1 μmol/L
Incubation Time: 24 h
Result: Downregulated the mRNA expressions of PDK1, RXRα, PPARα, and Bcl-2 in U251 cells.

Cell Cycle Analysis[2]

Cell Line: U251 cells
Concentration: 0, 0.1, 0.5, 1 μmol/L
Incubation Time: 24 hours
Result: Blocked the cell cycle of U251 cells at the G2/M phase in a concentration-dependent manner and reduced expression levels of cyclin A2 and CDK1.
体内研究
(In Vivo)

Isocucurbitacin B (2 mg/kg;腹腔注射;每日;从第 6 天起连续 18 天) 抑制 U251 细胞移植的 BALB/c 裸鼠的肿瘤生长[1]
Isocucurbitacin B (0.025-0.05 mg/L;72 小时) 减少胶质瘤细胞诱导斑马鱼的肿瘤负荷[2]
Isocucurbitacin B (1 mg/kg;腹腔注射;每日;从第 7 天起连续 21 天) 抑制 GL261 细胞诱导的 C57BL/6 鼠胶质瘤的生长[2]

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

Animal Model: Six-week-old specific pathogen-free (SPF) BALB/c nude mice transplanted with U251 cells [1]
Dosage: 2 mg/kg
Administration: Intraperitoneally injection; daily; 18 days from day 6
Result: Tumor growth was significantly inhibited. No significant effect on body weight was observed.
Animal Model: C57BL/6 (Male, 5 weeks old)[2]
Dosage: 1 mg/kg
Administration: intraperitoneal; daily; 27 days
Result: Tumor volume was significantly reduced, and cell proliferation and glial fibrillary acidic protein expression were decreased.
Animal Model: Glioma cell-induced Zebrafish[2]
Dosage: 0.025 mg/L, 0.05 mg/L
Administration: In water; 72 hours
Result: Fluorescence intensity was significantly reduced, indicating a reduction in tumor burden.
分子量

558.70

Formula

C32H46O8

CAS 号
性状

固体

颜色

White to off-white

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

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

纯度 & 产品资料
参考文献
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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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