1. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease NF-κB
  2. PPAR NF-κB
  3. 4-O-Methyl honokiol

4-O-Methyl honokiol  (Synonyms: 4--O-甲基和厚朴酚)

目录号: HY-U00450 纯度: 98.18%
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4-O-Methyl honokiol 是从厚朴中分离到的木脂素类化合物,为 PPARγ 的激动剂,可抑制 NF-κB 的活性,用于癌症,炎症等研究。

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4-O-Methyl honokiol Chemical Structure

4-O-Methyl honokiol Chemical Structure

CAS No. : 68592-15-4

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10 mM * 1 mL in DMSO ¥1650
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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

4-O-Methyl honokiol is a natural neolignan isolated from Magnolia officinalis, acts as a PPARγ agonist, and inhibtis NF-κB activity, used for cancer and inflammation research.

IC50 & Target[1]

PPARγ

 

NF-κB

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A2780 IC50
14.67 μM
Compound: 2b
Antiproliferative activity against human A2780 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Antiproliferative activity against human A2780 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 32996316]
A549 IC50
> 5 μg/mL
Compound: 4
Cytotoxicity against human A549 cells by MTT assay
Cytotoxicity against human A549 cells by MTT assay
[PMID: 17918910]
A549 IC50
1.24 μM
Compound: 1
Cytotoxicity against human A549 cells after 72 hrs by MTS assay
Cytotoxicity against human A549 cells after 72 hrs by MTS assay
[PMID: 22533983]
A549 IC50
1.56 μM
Compound: 1
Cytotoxicity against human A549 cells after 24 hrs by MTS assay
Cytotoxicity against human A549 cells after 24 hrs by MTS assay
[PMID: 22533983]
A549 IC50
21.97 μM
Compound: 2b
Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 32996316]
BV-2 IC50
52.3 μM
Compound: 2
Anti-inflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by griess assay
Anti-inflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by griess assay
[PMID: 30472026]
CNE2Z IC50
25.53 μM
Compound: 1a
Antiproliferative activity against human CNE2Z cells assessed as growth inhibition after 72 hrs by MTT assay
Antiproliferative activity against human CNE2Z cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 31831382]
HeLa IC50
> 5 μg/mL
Compound: 4
Cytotoxicity against human HeLa cells by MTT assay
Cytotoxicity against human HeLa cells by MTT assay
[PMID: 17918910]
HepG2 IC50
17.47 μM
Compound: 2b
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 32996316]
HepG2 IC50
55.3 μM
Compound: 9a
Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay
[PMID: 21853991]
HT-29 IC50
14.13 μM
Compound: 1
Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay
Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay
[PMID: 22533983]
HT-29 IC50
21.07 μM
Compound: 2b
Antiproliferative activity against human HT29 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Antiproliferative activity against human HT29 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 32996316]
HT-29 IC50
22.45 μM
Compound: 1
Cytotoxicity against human HT-29 cells after 24 hrs by MTS assay
Cytotoxicity against human HT-29 cells after 24 hrs by MTS assay
[PMID: 22533983]
HUVEC IC50
55.8 μM
Compound: 9a
Antiproliferative activity against human HUVEC cells after 24 hrs by MTT assay
Antiproliferative activity against human HUVEC cells after 24 hrs by MTT assay
[PMID: 21853991]
I10 IC50
26.54 μM
Compound: 1a
Antiproliferative activity against mouse I10 cells assessed as growth inhibition after 72 hrs by MTT assay
Antiproliferative activity against mouse I10 cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 31831382]
K562 IC50
> 5 μg/mL
Compound: 4
Cytotoxicity against human K562 cells by MTT assay
Cytotoxicity against human K562 cells by MTT assay
[PMID: 17918910]
L02 IC50
23.94 μM
Compound: 2b
Antiproliferative activity against human L02 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Antiproliferative activity against human L02 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 32996316]
Lewis lung carcinoma cell line IC50
68.8 μM
Compound: 9a
Antiproliferative activity against mouse LL/2 cells after 24 hrs by MTT assay
Antiproliferative activity against mouse LL/2 cells after 24 hrs by MTT assay
[PMID: 21853991]
MCF7 IC50
24.71 μM
Compound: 1a
Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 31831382]
Neutrophil IC50
14.32 μM
Compound: 17
Antiinflammatory activity in human neutrophils assessed as inhibition of FMLP/CB-induced superoxide anion generation by measuring superoxide dismutase-inhibitable reduction of ferricytochrome c by spectrophotometric analysis
Antiinflammatory activity in human neutrophils assessed as inhibition of FMLP/CB-induced superoxide anion generation by measuring superoxide dismutase-inhibitable reduction of ferricytochrome c by spectrophotometric analysis
[PMID: 26928286]
Neutrophil IC50
8.18 μM
Compound: 17
Antiinflammatory activity in human neutrophils assessed as inhibition of FMLP/CB-induced elastase release using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as substrate incubated for 5 mins by spectrophotometric analysis
Antiinflammatory activity in human neutrophils assessed as inhibition of FMLP/CB-induced elastase release using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as substrate incubated for 5 mins by spectrophotometric analysis
[PMID: 26928286]
Oocyte EC50
27.2 μM
Compound: 1
Modulation of GABA Aalpha1beta2 receptor expressed in Xenopus laevis oocytes assessed as potentiation of GABA-induced chloride current at holding potential -70 mV by two-microelectrode voltage clamp technique
Modulation of GABA Aalpha1beta2 receptor expressed in Xenopus laevis oocytes assessed as potentiation of GABA-induced chloride current at holding potential -70 mV by two-microelectrode voltage clamp technique
[PMID: 21699169]
PANC-1 IC50
16.73 μM
Compound: 2b
Antiproliferative activity against human PANC1 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Antiproliferative activity against human PANC1 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 32996316]
PC-3 IC50
17.87 μM
Compound: 2b
Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 32996316]
RAW264.7 IC50
18 μM
Compound: 3
Inhibition of LPS-induced NO production in mouse RAW264.7 cells after 24 hrs by Griess assay
Inhibition of LPS-induced NO production in mouse RAW264.7 cells after 24 hrs by Griess assay
[PMID: 22494844]
RAW264.7 IC50
27 μM
Compound: 3
Cytotoxicity against mouse RAW264.7 cells assessed as cell viability by propidium iodide staining based FACS-flow cytometry
Cytotoxicity against mouse RAW264.7 cells assessed as cell viability by propidium iodide staining based FACS-flow cytometry
[PMID: 22494844]
UACC-903 IC50
24.13 μM
Compound: 1
Cytotoxicity against human UACC-903 cells after 72 hrs by MTS assay
Cytotoxicity against human UACC-903 cells after 72 hrs by MTS assay
[PMID: 22533983]
UACC-903 IC50
37.68 μM
Compound: 1
Cytotoxicity against human UACC-903 cells after 24 hrs by MTS assay
Cytotoxicity against human UACC-903 cells after 24 hrs by MTS assay
[PMID: 22533983]
体外研究
(In Vitro)

4-O-Methyl honokiol is a natural neolignan isolated from Magnolia officinalis, acts as a PPARγ agonist, and inhibtis NF-κB activity. 4-O-Methyl honokiol (20 μM) increases the expression, transcription and DNA binding activities, and nuclear translocation of PPARγ in both in prostate PC-3 and LNCap cells. 4-O-Methyl honokiol (0-30 μM) inhibits LNCaP and PC-3 cancer cells growth, causes G0/G1 phase arrest and induces apoptotic cell death, and such effects can be reversed by PPARγ antagonist. 4-O-Methyl honokiol inhibits NF-κB activity and cancer cell growth, but such effects as well as its activation of PPARγ can be abolished by knock-down of p21[1]. 4-O-methylhonokiol (0.5, 1 and 2 μM) reduces LPS-induced release of NO, PGE2, ROS, TNF-α and IL-1β in cultured astrocytes, and amyloidogenesis in cultured astrocytes and microglial BV-2 cells[2].

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

体内研究
(In Vivo)

4-O-Methyl honokiol (40 or 80 mg/kg, i.p. everyday for 4 weeks) inhibits the growth of SW620 and PC3 tumours in SW620 and PC3 xenograft model. 4-O-Methyl honokiol significantly increases the expression of p21 and PPARγ in the tumour tissues[1]. 4-O-Methyl honokiol (0.5 or 1 mg/kg/day daily for 3 weeks) significantly ameliorates LPS-induced memory impairment, and inhibits LPS-induced iNOS and COX-2 expression in mice. 4-O-Methyl honokiol also shows inhibitory activities against the Aβ1-42 accumulation, and activates astrocytes and microglia in LPS-injected mice brain[2].

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

分子量

280.36

Formula

C19H20O2

CAS 号
性状

粘稠液体

颜色

Orange to red

中文名称

4--O-甲基和厚朴酚

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (356.68 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 3.5668 mL 17.8342 mL 35.6684 mL
5 mM 0.7134 mL 3.5668 mL 7.1337 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。-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: ≥ 2.5 mg/mL (8.92 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 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: ≥ 2.5 mg/mL (8.92 mM); 澄清溶液

    此方案可获得 ≥ 2.5 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。

    1 mL 工作液为例,取 100 μL 25.0 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

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)。
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: 98.18%

参考文献
Cell Assay
[1]

Cells (5 × 104 cells per well) are plated onto 24-well plates. The cell growth inhibitory effect of 4-O-Methyl honokiol is evaluated in cells treated with 4-O-Methyl honokiol (0-30 μM) for 0-72 h, using an excluded trypan blue assay[1].

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

Animal Administration
[1]

Six-week-old male BALB/c athymic nude mice are used in the assay. SW620 and PC3 cells are injected s.c. (1 × 107 cells in 0.1 mL PBS per animal) into the lower right flanks of mice. After 20 days, when the tumours have reached an average volume of 300-400 mm3 or about 50 mm3, the tumour-bearing nude mice are i.p. injected with 4-O-Methyl honokiol (40 and 80 mg/kg dissolved in 0.1% DMSO) twice per week for 3 weeks. Cisplatin (10 mg/kg) is also i.p. injected once a week as a positive control. The group treated with 0.1% DMSO is designated as the control. The tumour volumes are measured with vernier calipers and calculated by the following formula: (A × B2)/2, where A is the larger and B is the smaller of the two dimensions[1].

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

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。-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 3.5668 mL 17.8342 mL 35.6684 mL 89.1711 mL
5 mM 0.7134 mL 3.5668 mL 7.1337 mL 17.8342 mL
10 mM 0.3567 mL 1.7834 mL 3.5668 mL 8.9171 mL
15 mM 0.2378 mL 1.1889 mL 2.3779 mL 5.9447 mL
20 mM 0.1783 mL 0.8917 mL 1.7834 mL 4.4586 mL
25 mM 0.1427 mL 0.7134 mL 1.4267 mL 3.5668 mL
30 mM 0.1189 mL 0.5945 mL 1.1889 mL 2.9724 mL
40 mM 0.0892 mL 0.4459 mL 0.8917 mL 2.2293 mL
50 mM 0.0713 mL 0.3567 mL 0.7134 mL 1.7834 mL
60 mM 0.0594 mL 0.2972 mL 0.5945 mL 1.4862 mL
80 mM 0.0446 mL 0.2229 mL 0.4459 mL 1.1146 mL
100 mM 0.0357 mL 0.1783 mL 0.3567 mL 0.8917 mL
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产品名称:
4-O-Methyl honokiol
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HY-U00450
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