2. JAK/STAT Signaling Stem Cell/Wnt Protein Tyrosine Kinase/RTK Apoptosis NF-κB
  3. STAT VEGFR Bcl-2 Family Survivin IAP NF-κB Apoptosis Caspase
  4. Isolinderalactone

Isolinderalactone 是一种倍半萜，具有抗癌、抗炎和神经保护作用。Isolinderalactone抑制 的表达和 VEGFR2 的酪氨酸磷酸化。Isolinderalactone 降低 U-87 胶质母细胞瘤 (GBM) 细胞和结直肠癌 (CRC) 细胞的存活率并诱导其凋亡 (apoptosis)。Isolinderalactone 在结直肠癌 (CRC) 细胞中诱导 G2/M 期细胞周期停滞、活性氧 (ROS) 生成和 pJNK/p38 MAPK 激活。Isolinderalactone 在 RAW264.7 巨噬细胞中阻断 LPS 诱导的 NF-κB 活化，同时激活 Nrf2-HMOX1 信号通路。Isolinderalactone 改善 APP/PS1 小鼠的认知功能障碍。Isolinderalactone 可用于研究胶质母细胞瘤 (GBM)、结直肠癌、阿尔茨海默病和急性肺损伤。

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Isolinderalactone

Isolinderalactone Chemical Structure

CAS No. : 957-66-4

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Isolinderalactone 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

Isolinderalactone is a sesquiterpene that exhibits anti-cancer, anti-inflammatory, and neuroprotective effects. Isolinderalactone inhibits VEGF expression and tyrosine phosphorylation of VEGFR2. Isolinderalactone decreases viability and induces apoptosis in U-87 glioblastoma (GBM) cells and colorectal cancer (CRC) cells. Isolinderalactone induces G2/M phase cell cycle arrest, ROS generation, pJNK/p38 MAPK activation, in colorectal cancer (CRC) cells. Isolinderalactone blocks LPS (HY-D1056)-induced NF-κB activation while activating Nrf2-HMOX1 signaling in RAW264.7 macrophages. Isolinderalactone improves cognitive dysfunction in APP/PS1 mice. Isolinderalactone can be used for the study of Glioblastoma multiforme (GBM), colorectal cancer, Alzheimer’s disease and acute lung injury[1][2][3][4][5].

IC50 & Target

VEGFR2

 

Bcl-2

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
RAW264.7 IC50
0.3 μM
Compound: 7
Inhibition of iNOS-mediated NO production in LPS-stimulated mouse RAW264.7 cells after 24 hrs by Griess reagent method
Inhibition of iNOS-mediated NO production in LPS-stimulated mouse RAW264.7 cells after 24 hrs by Griess reagent method
[PMID: 22148193]
RAW264.7 CC50
66.41 μM
Compound: 7
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability after 3 hrs by alamar blue assay
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability after 3 hrs by alamar blue assay
[PMID: 22148193]
体外研究
(In Vitro)

Isolinderalactone (0.5-2.5 μg/mL, 24-72 h) 抑制 U-87 胶质母细胞瘤细胞生长[1]。
Isolinderalactone (0.5-2.5 μg/mL, 48 h) 通过降低 BCL-2、survivin 和 XIAP 表达，增加 cleaved caspase-3，并诱导 DNA 断裂，激活 U-87 GBM 细胞的凋亡途径，从而促进细胞凋亡[1]。
Isolinderalactone (0.5-2 μg/mL, 48 h) 抑制 U-87 GBM 细胞中 VEGF 表达，并抑制人脑微血管内皮细胞 (HBMECs) 的 VEGF 诱导血管生成[2]。
Isolinderalactone (2 μg/mL, 8 days) 在三维微流控芯片中抑制血管生成萌发[2]。
Isolinderalactone (2.5-5 μg/mL, 48 h) 降低 U-87 细胞中 HIF 表达和活性以及 HBMECs 中 VEGFR2 激活[2]。
Isolinderalactone (0-9 μM, 24-48 h) 抑制结直肠癌细胞 (HCT116, HCT116-OxR, HT29, HT29-OxR) 的增殖和集落形成[3]。
Isolinderalactone (0-9 μM, 48 h) 在结直肠癌细胞中诱导凋亡、G2/M 期细胞周期停滞、活性氧 (ROS) 生成和内质网应激[3]。
Isolinderalactone (0-9 μM, 48 h) 在结直肠癌细胞中诱导凋亡，通过线粒体和 caspase 依赖途径，可能通过调节 JNK/p38 MAPK 激活，其中 ROS 发挥关键作用[3]。
Isolinderalactone (10 μM, 2-27 h) 减轻 Aβ1-42 诱导的细胞损伤并降低 PC12 细胞中的神经毒性[4]。
Isolinderalactone (10 μM, 27 h) 通过抑制 JNK 减少 PC12 细胞中的神经元细胞损伤[4]。
Isolinderalactone (0.5-10 μM, 19 h) 在 RAW264.7 细胞、MH-S 细胞和骨髓源性巨噬细胞 (BMDMs) 中抑制 LPS 或 TNF-α 诱导的炎症反应[5]。
Isolinderalactone (1-10 μM, 13 h) 在 LPS 刺激的 RAW264.7 巨噬细胞中抑制促炎酶和细胞因子的 mRNA 表达[5]。
Isolinderalactone (1-10 μM, 2-9 h) 在 RAW264.7 巨噬细胞中阻断 LPS 诱导的 NF-κB 活化，同时激活 Nrf2-HMOX1 信号通路[5]。

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

Isolinderalactone 相关抗体:

Cell Viability Assay[1][2]

Cell Line: U-87 GBM cells and HBMECs
Concentration: 0.5, 1, 2, 2.5 μg/mL
Incubation Time: 24, 48, 72 h
Result: Inhibited cell viability in a dose-dependent manner.
Decreased VEGF-induced HBMEC proliferation in a dose-dependent manner.

Western Blot Analysis[1][2]

Cell Line: U-87 GBM cells and HBMECs
Concentration: 0.5, 1, 2.5,5 μg/mL
Incubation Time: 48 h
Result: Decreased BCL-2, survivin, and XIAP expression.
Increased the level of cleaved caspase-3 and cleaved PARP.
Decreased the expression of the potent angiogenic factor, VEGF.
Decreased HIF expression and activity in U-87 cells.
Reduced phosphorylation of VEGFR2 in HBMECs.

Immunofluorescence[1]

Cell Line: U-87 GBM cells
Concentration: 2.5 μg/mL
Incubation Time: 48 h
Result: Showed predominantly bright γ-H2AX nuclear staining.

Cell Viability Assay[3]

Cell Line: HCT116, HCT116-OxR, HT29, and HT29-OxR cells
Concentration: 3, 6, 9 μM
Incubation Time: 24, 48 h
Result: Suppressed colorectal cancer cells proliferation with IC50 values of 8.05 μM (HCT116), 5.13 μM (HCT116-OxR), 10.38 μM (HT29) and 9.46 μM (HT29-OxR).

Cell Cycle Analysis[3]

Cell Line: HCT116, HCT116-OxR, HT29, and HT29-OxR cells
Concentration: 3, 6, 9 μM
Incubation Time: 48 h
Result: Contributed to G2/M phase cell cycle arrest.

Western Blot Analysis[3]

Cell Line: HCT116, HCT116-OxR, HT29, and HT29-OxR cells
Concentration: 3, 6, 9 μM
Incubation Time: 48 h
Result: Increased the expression levels of ER stress related proteins (GRP78, CHOP, DR4, and DR5).
Activated JNK/p38 MAPK.
Increased the levels of pro-apoptotic proteins (Bim and Bax), apaf-1, and cleaved (c)-PARP.
Decreased expression levels of anti-apoptotic proteins (Mcl-1, Bid, Bcl-xL and Bcl-2), mitochondrial cyto c and caspase 3 in a dose-dependent manner.

Western Blot Analysis[4]

Cell Line: Aβ1-42-induced PC12 cells
Concentration: 10 μM
Incubation Time: 27 h
Result: Decreased Bax expression and intracellular levels of caspase-3 activation and increased Bcl2 levels.
Decreased the level of p-JNK, but had no significant effect on ERK and P38MAPK.

Real Time qPCR[5]

Cell Line: LPS-exposed RAW264.7 macrophages
Concentration: 1, 10 μM
Incubation Time: 13 h
Result: Decreased the mRNA levels of iNOS, COX2, IL-1β, IL-6, and TNF-α.

Western Blot Analysis[5]

Cell Line: LPS-exposed RAW264.7 macrophages
Concentration: 1, 5, 10 μM
Incubation Time: 2, 9 h
Result: Down-regulated LPS-induced phosphorylation of IKKα/β and the level of NF-κB p65.
Increased the protein level of Nrf2 protein in the cytoplasmic fraction and nuclear fraction.
体内研究
(In Vivo)

Isolinderalactone (1-5 mg/kg，腹腔注射，每隔一天一次，共 12 天) 抑制人 GBM 异种移植小鼠模型中的肿瘤生长[1]。
Isolinderalactone (2.5-5 mg/kg，腹腔注射，每隔一天一次，共 16 天) 减少人 GBM 异种移植模型中的肿瘤生长和血管生成[2]。
Isolinderalactone (5 mg/kg，腹腔注射，每天一次，共 6 天) 在小鼠体内 Matrigel 实验中抑制 VEGF 介导的血管生成[2]。
Isolinderalactone (1-10 mg/kg，腹腔注射，每天一次，共 30 天) 改善 APP/PS1 小鼠的学习和记忆缺陷[4]。
Isolinderalactone (2.5-10 mg/kg，腹腔注射，每日一次，持续 5 天) 可减轻 LPS 诱导的小鼠肺部炎症损伤[5]。

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

Animal Model: U-87 GBM cells (3 × 106 cells/100 μL of serum-free DMEM) were subcutaneously implanted into the right flank of the BALB/C nude mice[1]
Dosage: 1, 2.5, 5 mg/kg
Administration: i.p., every other day for 12 days
Result: Reduced tumor volume and weight Showed no differences on body weight.
Increased cleaved caspase-3 fluorescence.
Showed a significantly higher number of TUNEL-positive cells.
Animal Model: U-87 GBM cells (3 × 106 cells/100 μL of serum-free DMEM) were subcutaneously implanted into the right flank of the BALB/C nude mice[2]
Dosage: 2.5, 5 mg/kg
Administration: i.p., every other day for 16 days
Result: Decreased tumor volume and suppressed tumor progression.
Inhibited tumor angiogenesis.
Reduced VEGF immunoreactivity.
Animal Model: C57BL/6 mice (6-week-old, male)[2]
Dosage: 5 mg/kg
Administration: i.p. daily for 6 days
Result: Decreased hemoglobin concentration and CD31 staining.
Inhibited VEGF-induced new vessel formation in vivo.
Animal Model: 10-month-old APP/PS1 transgenic mice[4]
Dosage: 1, 10 mg/kg
Administration: i.p. daily for 30 days
Result: Enhanced the exploration of the novel object by the mice.
Ameliorated learning and memory deficits in APP/PS1mice.
Reduced the level of APP/β-amyloid.
Increased the levels of synapse-associated proteins, including PSD95 and Map2.
Reduced neuronal apoptosis in the cortex and hippocampus.
Increased the SOD content and decreased MDA levels in the hippocampus.
Increased Bcl2 levels, decreased Bax, p-JNK expression, and decreased caspase-3 activation.
Animal Model: Male Institute of Cancer Research (ICR) mice (SPF grade, 20-22 g, 6 weeks old) injected with LPS (15 mg/kg)[5]
Dosage: 2.5-10 mg/kg
Administration: i.p., daily for 5 days
Result: Improved the lung injury scores.
Reduced the MPO activity in LPS-exposed lung tissue.
Reduced the levels of PGE2, IL-1β, IL-6, and TNF-α.
分子量

244.29

Formula

C15H16O3
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, sealed storage, away from moisture and light

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

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 50 mg/mL (204.67 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 4.0935 mL 20.4675 mL 40.9350 mL
5 mM 0.8187 mL 4.0935 mL 8.1870 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 (sealed storage, away from moisture and 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% Corn Oil

    Solubility: ≥ 5 mg/mL (20.47 mM); 澄清溶液

    此方案可获得 ≥ 5 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。

    以 1 mL 工作液为例，取 100 μL 50.0 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

只
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 (sealed storage, away from moisture and 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
参考文献

Isolinderalactone 相关分类

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 (sealed storage, away from moisture and 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 4.0935 mL 20.4675 mL 40.9350 mL 102.3374 mL
5 mM 0.8187 mL 4.0935 mL 8.1870 mL 20.4675 mL
10 mM 0.4093 mL 2.0467 mL 4.0935 mL 10.2337 mL
15 mM 0.2729 mL 1.3645 mL 2.7290 mL 6.8225 mL
20 mM 0.2047 mL 1.0234 mL 2.0467 mL 5.1169 mL
25 mM 0.1637 mL 0.8187 mL 1.6374 mL 4.0935 mL
30 mM 0.1364 mL 0.6822 mL 1.3645 mL 3.4112 mL
40 mM 0.1023 mL 0.5117 mL 1.0234 mL 2.5584 mL
50 mM 0.0819 mL 0.4093 mL 0.8187 mL 2.0467 mL
60 mM 0.0682 mL 0.3411 mL 0.6822 mL 1.7056 mL
80 mM 0.0512 mL 0.2558 mL 0.5117 mL 1.2792 mL
100 mM 0.0409 mL 0.2047 mL 0.4093 mL 1.0234 mL
Help & FAQs
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    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:

Isolinderalactone957-66-4STATVEGFRBcl-2 FamilySurvivinIAPNF-κBApoptosisCaspaseVascular endothelial growth factor receptorNuclear factor-κBNuclear factor-kappaBBrain tumor3D microfluidic chiphypoxia-inducible factorvascular endothelialgrowth factorangiogenesis,Reactive oxygen speciesJNK/p38 MAPKColorectal cancerAlzheimer’s diseaseInhibitorinhibitorinhibit

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