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Cucurbitacin I

Cucurbitacin I

产品编号 TQ0196   CAS 2222-07-3
别名: NSC-521777, JSI-124, Elatericin B, 葫芦素 I

Cucurbitacin I (JSI-124) 是从曲莲中提取的一种天然产物,是 JAK2/STAT3选择性抑制剂,有抗肿瘤活性。

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Cucurbitacin I Chemical Structure
Cucurbitacin I, CAS 2222-07-3
规格 价格/CNY 货期 数量
1 mg ¥ 760 现货
5 mg ¥ 3,610 现货
1 mL * 10 mM (in DMSO) ¥ 4,120 现货
产品目录号及名称: Cucurbitacin I (TQ0196)
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选择批次  
纯度: 98.2%
纯度: 96.69%
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天然产物信息
生物活性
化学信息
存储 & 溶解度
参考文献
植物来源
结构类型
产品描述 Cucurbitacin I (JSI-124), a natural compound, is a selective inhibitor of JAK2/STAT3 with anti-cancer activity.
体外活性 The anticancer activity of Cucurbitacin I is accomplished by downregulating p-STAT3 and MMP-9 expression [1]. Incubation of the Seax cell line with the Jak/Stat3 inhibitor Cucurbitacin I result in a time- and concentration-dependent decrease of P-Stat3 and Stat3. Incubation of freshly isolated Sz cells with 30 μM Cucurbitacin I for 6 hours induces apoptosis in the large majority (73-91%) of tumor cells [2]. PE-induced cell enlargement and upregulation of ANF and β-MHC are significantly suppressed by pretreatment of the cardiomyocytes with Cucurbitacin I. Cucurbitacin I also impaired connective tissue growth factor (CTGF) and MAPK signaling, pro-hypertrophic factors, as well as TGF-β/Smad signaling, the important contributing factors to fibrosis [3].
体内活性 The differences in tumor volume between the Cucurbitacin I and control, combination and control, and combination and Cucurbitacin I arms are significant. Furthermore, combination-treated tumors exhibit a significantly lower average tumor weight at study termination than control. Moreover, there was no effect on the body weights of mice [4].
动物实验 BALB/c nude (nu/nu) female mice are used. U251 cells (5×10^6 cells in 50 μL of serum-free DMEM) are inoculated subcutaneously into the right flank of 5-week-old female mice after acclimatization for a week. Tumor growth is measured daily with calipers. When the tumors reach a mean volume of 90-120 mm3, animals are randomized into groups. In the first experiment, 16 mice are randomly assigned to Cucurbitacin I (1 mg/kg/day in 20% DMSO in PBS) or drug vehicle control (20% DMSO in PBS) and dosed intraperitoneally with 100 μL of vehicle or drug once daily for 18 days, whereas, in the second, 20 mice are assigned to four groups. Control animals receive 20% DMSO in PBS vehicle, whereas treated animals are injected with Cucurbitacin I (1 mg/kg/day) in 20% DMSO in PBS, CQ (25 mg/kg/day) in 20% DMSO in PBS, and Cucurbitacin I (1 mg/kg/day) plus CQ (25 mg/kg/day) in 20% DMSO in PBS and dosed intraperitoneally with 100 μL of vehicle or drug once daily for 15 days [4].
别名 NSC-521777, JSI-124, Elatericin B, 葫芦素 I
分子量 514.65
分子式 C30H42O7
CAS No. 2222-07-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 95 mg/mL (184.59 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9431 mL 9.7153 mL 19.4307 mL 48.5767 mL
5 mM 0.3886 mL 1.9431 mL 3.8861 mL 9.7153 mL
10 mM 0.1943 mL 0.9715 mL 1.9431 mL 4.8577 mL
20 mM 0.0972 mL 0.4858 mL 0.9715 mL 2.4288 mL
50 mM 0.0389 mL 0.1943 mL 0.3886 mL 0.9715 mL
100 mM 0.0194 mL 0.0972 mL 0.1943 mL 0.4858 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Song J, et al. Cucurbitacin I inhibits cell migration and invasion and enhances chemosensitivity in colon cancer. Oncol Rep. 2015 Apr;33(4):1867-71. 2. Jeong MH, et al. Cucurbitacin I Attenuates Cardiomyocyte Hypertrophy via Inhibition of Connective Tissue Growth Factor (CCN2) and TGF- β/Smads Signalings. PLoS One. 2015 Aug 21;10(8):e0136236. 3. van Kester MS, et al. Cucurbitacin I inhibits Stat3 and induces apoptosis in Sézary cells. J Invest Dermatol. 2008 Jul;128(7):1691-5. 4. Yuan G, et al. Cucurbitacin I induces protective autophagy in glioblastoma in vitro and in vivo. J Biol Chem. 2014 Apr 11;289(15):10607-19.

文献引用

1. Gong X, Liu Y, Liang K, et al.Cucurbitacin I Reverses Tumor-Associated Macrophage Polarization to Affect Cancer Cell Metastasis.International Journal of Molecular Sciences.2023, 24(21): 15920.
W1131 TFA MNK8  ENMD-1198 Cryptotanshinone Homoharringtonine Saikosaponin D Niclosamide STAT3-IN-11

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 NO PAINS 化合物库 抗胰腺癌化合物库 经典已知活性库 萜类天然产物库 转录因子库 癌细胞分化化合物库 人代谢物化合物库 植物来源化合物库 表观遗传库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Cucurbitacin I 2222-07-3 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells JAK STAT NSC-521777 Janus kinase NSC521777 Inhibitor JSI-124 Elatericin B JSI124 JSI 124 葫芦素 I NSC 521777 inhibit inhibitor

 

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