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Honokiol Antineoplastic and Immunosuppressive Antibiotics inhibitor

Name: Honokiol
Brand: Selleck Chemicals
SKU: S2310
Availability: InStock
Rating: 5 (35 reviews)

Cat.No.S2310

Honokiol is the active principle of magnolia extract that inhibits Akt-phosphorylation and promotes ERK1/2 phosphorylation. This compound causes G0/G1 phase arrest, induces apoptosis, and autophagy via the ROS/ERK1/2 signaling pathway. It inhibits hepatitis C virus (HCV) infection. Phase 3.

Chemical Structure

Molecular Weight: 266.334

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability

Quality Control

Batch: Purity: 99.96%

99.96

Related Targets	PI3K Akt mTOR AMPK GSK-3 ATM/ATR DNA-PK PDPK1 PTEN PP2A PDK PI4K PIKfyve MELK
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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description
human UACC-903 cells	Cytotoxicity assay			Cytotoxicity against human UACC-903 cells after 72 hrs by MTS assay, IC50=5.1 μM
Vero E6 cells	Function assay			Antiviral activity against SARS coronavirus in Vero E6 cells assessed as inhibition of viral replication by ELISA, EC50=6.5 μM
human UACC-903 cells	Cytotoxicity assay			Cytotoxicity against human UACC-903 cells after 24 hrs by MTS assay, IC50=7.45 μM
human A549 cells	Cytotoxicity assay			Cytotoxicity against human A549 cells after 72 hrs by MTS assay, IC50=7.75 μM
human CEM cells	Cytotoxicity assay			Cytotoxicity against human CEM cells, IC50=10.9 μM
HEK293 cells	Function assay			Agonist activity at RXRalpha in HEK293 cells assessed as transcriptional activation after 48 hrs by luciferase reporter gene assay, EC50=11.8 μM
human A549 cell	Cytotoxicity assay		24 h	Cytotoxicity against human A549 cells after 24 hrs by MTS assay, IC50=12.51 μM
human HT-29 cells	Cytotoxicity assay		72 h	Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay, IC50=13.24 μM
human PBM cells	Cytotoxicity assay			Cytotoxicity against human PBM cells, IC50=16.1 μM
Hep-G2 cells	Cytotoxicity assay			Cytotoxicity of compound against human liver tumor cell line (Hep-G2) was determined, IC50=16.5 μM
human HepG2 cells	Proliferation assay		24 h	Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay, IC50=16.5 μM
human K562 cells	Proliferation assay			Antiproliferative activity against human K562 cells by MTT assay, IC50=21.1 μM
Vero cells	Cytotoxicity assay			Cytotoxicity against Vero cells, IC50=22.5 μM
human A2780 cells	Proliferation assay			Antiproliferative activity against cisplatin-sensitive human A2780 cells by MTT assay, IC50=30.5 μM
human SPC-A1 cells	Proliferation assay			Antiproliferative activity against human SPC-A1 cells by MTT assay, IC50=36.1 μM
HUVEC cells	Function assay	20 μM	24 h	Antimigratory activity against human HUVEC cells at 20 uM after 24 hrs by wound-healing assay
HEK293 cells	Function assay		24-48 h	Agonist activity at human RXR-alpha expressed in HEK293 cells coexpressing with pCMX-beta-gal after 24 to 48 hrs by luciferase reporter gene assay
human SH-SY5Y cells	Function assay	10 μM	30 mins	Neuroprotective activity in human SH-SY5Y cells assessed as inhibition of CHP and TBHP-induced cell death at 10 uM incubated for 30 mins prior to challenge measured after 3 hrs by MTT assay
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	266.334	Formula	C₁₈H₁₈O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	35354-74-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC 293100			Smiles	C=CCC1=CC(=C(C=C1)O)C2=CC(=C(C=C2)O)CC=C

Solubility

In vitro
Batch:

DMSO : 53 mg/mL ( (198.99 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2%DMSO 1 40%PEG300 2 2%Tween80 3 56%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.000mg/ml (7.51mM)	Taking the 1 mL working solution as an example, add 20 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 560 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.000mg/ml (7.51mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (1.88mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Akt-phosphorylation ^[1] MEK ^[8]
In vitro	Honokiol shows pro-apoptotic effects in melanoma, sarcoma, myeloma, leukemia, bladder, lung, prostate, oral squamous cell carcinoma and colon cancer cell lines. This compound is effective on inducing apoptosis in SVR angiosarcoma cells. Treatment of SVR cells with this chemical causes decreased phosphorylation of MAP kinase, akt, and c-src. In addition, it potentiates TRAIL-mediated apoptosis, and its cytotoxicity is partially abrogated by neutralizing antibodies to TRAIL. This compound also has direct antiangiogenic activity, in that it blocks the phosphorylation and rac activation due to VEGF-VEGFR2 interactions. ^[1] It causes apoptosis in CLL cells through activation of caspase 8, followed by caspase 9 and 3 activation. This chemical prevents interleukin-4-mediated survival of CLL cells, and potentiats the cytotoxicity of CB-1348, FaraA, and 2-CdA. ^[3] It kills myeloma cells from relapsed patients at doses that does not kill PBMCs. Caspase 3, 7, 8, and 9 are induced by this compound treatment, as well as PARP cleavage. ^[2] It is found to induce apoptosis in the colon cancer cell lines RKO. ^[4] This chemical potentiates apoptosis, suppresses osteoclastogenesis, and inhibits invasion through modulation of nuclear factor-kappaB activation pathway. ^[5] It may act as a potent anti-inflammatory agent with multipotential activities due to an inhibitory effect on the PI3K/Akt pathway. ^[6]
In vivo	Honokiol is highly effective against SVR angiosarcoma in nude mice. ^[1] This compound inhibits the growth of RKO cells in murine xenografts. ^[4] It prevents the growth of MDA-MD-231 breast cancer cells in murine xenografts. ^[7]
References	https://pubmed.ncbi.nlm.nih.gov/12816951/ https://pubmed.ncbi.nlm.nih.gov/15870175/ https://pubmed.ncbi.nlm.nih.gov/15802533/ https://pubmed.ncbi.nlm.nih.gov/15259066/ https://pubmed.ncbi.nlm.nih.gov/16966432/ https://pubmed.ncbi.nlm.nih.gov/18158873/ https://pubmed.ncbi.nlm.nih.gov/17487375/ https://pubmed.ncbi.nlm.nih.gov/15922325/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-EGFR / p-AKT / p-STAT3 / p-ERK / p-GSK3α/β / Bax / p-pRb / p-BAD / IκBα / CDK2 / CDK4 / Cyclin D1 p-Lyn / Lyn / p-PI3K		27458163
Immunofluorescence	Vimentin / Occludin IκBα / NF-κB p65		24508063

Tech Support

Handling Instructions

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