4-O-Methyl honokiol

Name: 4-O-Methyl honokiol
Brand: MedChemExpress
SKU: HY-U00450
Rating: 4.5 (1 reviews)

Cat. No.: HY-U00450 Purity: 98.18%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

4-O-Methyl honokiol Chemical Structure

CAS No. : 68592-15-4

Size	Stock	Quantity
Solid or liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid or liquid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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•Related Screening Libraries:

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•Related Proteins:

View All PPAR Isoform Specific Products:

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PPARα PPARβ/δ PPARγ PPAR PPARδ

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

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]

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].

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

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 Aβ_1-42 accumulation, and activates astrocytes and microglia in LPS-injected mice brain^[2].

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

Molecular Weight

280.36

Formula

C₁₉H₂₀O₂

CAS No.

68592-15-4

Appearance

Viscous Liquid

Color

Orange to red

SMILES

OC1=CC=C(CC=C)C=C1C2=CC(CC=C)=C(OC)C=C2

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (356.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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
10 mM	0.3567 mL	1.7834 mL	3.5668 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.92 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (8.92 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.18%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (245 KB) LCMS (88 KB)

Handling Instructions (2659 KB)

References

[1]. Lee NJ, et al. 4-O-methylhonokiol, a PPARγ agonist, inhibits prostate tumour growth: p21-mediated suppression of NF-κB activity. Br J Pharmacol. 2013 Mar;168(5):1133-45. [Content Brief]

[2]. Lee YJ, et al. Inhibitory effect of 4-O-methylhonokiol on lipopolysaccharide-induced neuroinflammation, amyloidogenesis and memory impairment via inhibition of nuclear factor-kappaB in vitro and in vivo models. J Neuroinflammation. 2012 Feb 19;9:35. [Content Brief]

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.
References	[1]. Lee NJ, et al. 4-O-methylhonokiol, a PPARγ agonist, inhibits prostate tumour growth: p21-mediated suppression of NF-κB activity. Br J Pharmacol. 2013 Mar;168(5):1133-45. [Content Brief] [2]. Lee YJ, et al. Inhibitory effect of 4-O-methylhonokiol on lipopolysaccharide-induced neuroinflammation, amyloidogenesis and memory impairment via inhibition of nuclear factor-kappaB in vitro and in vivo models. J Neuroinflammation. 2012 Feb 19;9:35. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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