1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis
  2. HSP Apoptosis
  3. Cucurbitacin D

Cucurbitacin D  (Synonyms: 葫芦素 D)

目录号: HY-N1986 纯度: 98.41%
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Cucurbitacin D 是Trichosanthes kirilowii 中的活性成分,可破坏 Hsp90 与两种辅助分子伴侣 Cdc37 和 p23 的相互结合。Cucurbitacin D 是一种炎性体激活剂。Cucurbitacin D 诱导细胞周期阻滞和细胞凋亡,具有抗肿瘤和抗炎作用。

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Cucurbitacin D Chemical Structure

Cucurbitacin D Chemical Structure

CAS No. : 3877-86-9

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10 mM * 1 mL in DMSO ¥3069
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5 mg ¥2700
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10 mg ¥4600
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Other Forms of Cucurbitacin D:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Cucurbitacin D is the active ingredient in Trichosanthes kirilowii and can disrupt the interaction between Hsp90 and two co-chaperones, Cdc37 and p23. Cucurbitacin D is an inflammasome activator. Cucurbitacin D induces cell cycle arrest and cell apoptosis, exhibiting anti-tumor and anti-inflammatory effects[1][2][3][4].

IC50 & Target[1]

HSP90

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HeLa IC50
0.7 μM
Compound: 3
Cytotoxicity against human HeLa cells after 24 hrs by MTT assay
Cytotoxicity against human HeLa cells after 24 hrs by MTT assay
[PMID: 21459003]
HepG2 IC50
77.33 μM
Compound: 3
Cytotoxicity against human HepG2 cells after 24 hrs assessed as inhibition of cell viability by MTT assay
Cytotoxicity against human HepG2 cells after 24 hrs assessed as inhibition of cell viability by MTT assay
[PMID: 21459003]
HepG2 EC50
9 μM
Compound: 3
Hepatoprotective activity in human HepG2 cells assessed as inhibition of CCl4-induced toxicity after 24 hrs by MTT assay
Hepatoprotective activity in human HepG2 cells assessed as inhibition of CCl4-induced toxicity after 24 hrs by MTT assay
[PMID: 21459003]
HSC-T6 EC50
0.07 μM
Compound: 3
Antiproliferative activity against serum-stimulated rat HSC-T6 cells after 24 hrs by MTT assay
Antiproliferative activity against serum-stimulated rat HSC-T6 cells after 24 hrs by MTT assay
[PMID: 21459003]
HSC-T6 IC50
26 μM
Compound: 3
Cytotoxicity against rat HSC-T6 cell after 24 hrs by MTT assay
Cytotoxicity against rat HSC-T6 cell after 24 hrs by MTT assay
[PMID: 21459003]
HT-29 IC50
> 10 μM
Compound: 9
Cytotoxicity against human HT-29 cells after 3 days by mitochondrial transmembrane potential assay
Cytotoxicity against human HT-29 cells after 3 days by mitochondrial transmembrane potential assay
[PMID: 22239601]
HT-29 IC50
0.12 μM
Compound: 9
Cytotoxicity against human HT-29 cells after 3 days by sulforhodamine B assay
Cytotoxicity against human HT-29 cells after 3 days by sulforhodamine B assay
[PMID: 22239601]
JY IC50
1.36 μM
Compound: 4
Inhibition of LFA1 expressed in human JY cells interaction with ICAM1-IG expressed in human HeLa cell monolayer after 45 mins by cell adhesion assay
Inhibition of LFA1 expressed in human JY cells interaction with ICAM1-IG expressed in human HeLa cell monolayer after 45 mins by cell adhesion assay
[PMID: 7852999]
MCF7 IC50
0.598 μM
Compound: 4
Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay
Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay
[PMID: 25756299]
NCI-H460 IC50
0.12 μg/mL
Compound: 5
Antiproliferative activity against human NCI-H460 cells after 72 hrs
Antiproliferative activity against human NCI-H460 cells after 72 hrs
[PMID: 17190463]
体外研究
(In Vitro)

Cucurbitacin D (0.5 μg/mL,24 h) 和阿霉素联用可诱导 MCF7/ADR 细胞凋亡,G2/M 细胞周期阻滞[1]
Cucurbitacin D (0.125-16 μg/mL,24-72 h) 显著抑制 MCF7 和 MCF7/ADR 细胞生长,且呈剂量和时间依赖性[1]
Cucurbitacin D (0.5-2 μg/mL, 24 h) 抑制 MCF7/ADR 细胞中 STAT3 信号传导,抑制 NF-κB 信号通路[1]
Cucurbitacin D 增强了 LPS (HY-D1056) 诱导的 THP-1、PECs、BMDMs 和 RAW264 细胞中 IL-1β 的产生[2]

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

Western Blot Analysis[1]

Cell Line: MCF7/ADR induced by doxorubicin
Concentration: 0.5, 2 μg/mL
Incubation Time: 24 h
Result: Reduced p-STAT3 levels, increased the expression of IκB and NF-κB in the cytoplasm, and reduced the expression of pNF-κB in the nucleus.

Cell Viability Assay[1]

Cell Line: MCF7, MCF7/ADR
Concentration: 0.125, 0.5, 2, 4, 8, 16 μg/mL
Incubation Time: 24, 48, 72 h
Result: Inhibited cell proliferation.

Apoptosis Analysis[1]

Cell Line: MCF7/ADR
Concentration: 0.5 μg/mL
Incubation Time: 24 h
Result: Increased apoptosis by 114%.

Cell Cycle Analysis[1]

Cell Line: MCF7/ADR
Concentration: 0.5 μg/mL
Incubation Time: 24 h
Result: Induced G2/M cell cycle arrest.
体内研究
(In Vivo)

Cucurbitacin D (1 mg/kg,瘤内注射,每周三次,四周) 抑制小鼠肿瘤增殖[3]

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

Animal Model: Xenograft cervical cancer cell model in nude mice[3]
Dosage: 1 mg/kg; three times a week; four weeks
Administration: Intratumoral injection
Result: Reduced tumor volume and weight, and the expression of pAKT and pSTAT3 proteins was significantly reduced.
分子量

516.67

Formula

C30H44O7

CAS 号
性状

固体

颜色

White to off-white

中文名称

葫芦素 D

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)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 110 mg/mL (212.90 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9355 mL 9.6774 mL 19.3547 mL
5 mM 0.3871 mL 1.9355 mL 3.8709 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.75 mg/mL (5.32 mM); 悬浊液; 超声助溶

    此方案可获得 2.75 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    1 mL 工作液为例,取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.75 mg/mL (5.32 mM); 澄清溶液

    此方案可获得 ≥ 2.75 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

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

您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.91%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9355 mL 9.6774 mL 19.3547 mL 48.3868 mL
5 mM 0.3871 mL 1.9355 mL 3.8709 mL 9.6774 mL
10 mM 0.1935 mL 0.9677 mL 1.9355 mL 4.8387 mL
15 mM 0.1290 mL 0.6452 mL 1.2903 mL 3.2258 mL
20 mM 0.0968 mL 0.4839 mL 0.9677 mL 2.4193 mL
25 mM 0.0774 mL 0.3871 mL 0.7742 mL 1.9355 mL
30 mM 0.0645 mL 0.3226 mL 0.6452 mL 1.6129 mL
40 mM 0.0484 mL 0.2419 mL 0.4839 mL 1.2097 mL
50 mM 0.0387 mL 0.1935 mL 0.3871 mL 0.9677 mL
60 mM 0.0323 mL 0.1613 mL 0.3226 mL 0.8064 mL
80 mM 0.0242 mL 0.1210 mL 0.2419 mL 0.6048 mL
100 mM 0.0194 mL 0.0968 mL 0.1935 mL 0.4839 mL
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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产品名称:
Cucurbitacin D
目录号:
HY-N1986
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