Name: Menadione (Vitamin K3)
Brand: Selleck Chemicals
SKU: S1949
Rating: 5 (9 reviews)

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Quality Control

Batch: Purity: 99.88%

99.88

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite
Other phosphatase Inhibitors	Osunprotafib (ABBV-CLS-484) SHP099 Hydrochloride RMC-4550 SHP099 GSK2830371 β-Glycerophosphate sodium salt hydrate Batoprotafib (TNO155) NSC87877 TPI-1 Sanguinarine chloride

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description
HT22 cells	Function assay			Neuroprotective activity in mouse HT22 cells assessed as prevention from glutamate-induced oxidative cell death by MTS assay, PD50=0.797 μM
HeLa cell	Cytotoxicity assay			Cytotoxicity against HeLa cell lines, EC50=3.7 μM
PaCa2 cell	Proliferation assay			Antiproliferative activity against human pancreatic carcinoma Mia PaCa2 cell line by colorimetric assay, IC50=6.2 μM
HT-29 cells	Cytotoxicity assay		72 h	Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by MTS assay, IC50=9.69 μM
DU145 cells	Cytotoxicity assay		72 h	Cytotoxicity against human DU145 cells assessed as growth inhibition after 72 hrs by MTS assay, IC50=9.86 μM
MDA-MB-231 cells	Cytotoxicity assay		72 h	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTS assay, IC50=12.68 μM
human A2058 cells	Cytotoxicity assay			Cytotoxicity against human A2058 cells assessed as inhibition of formazan formation at day 5 by measuring absorbance at 430 nm, IC50=13.4 μM
SAS cells	Cytotoxicity assay		48 h	Cytotoxicity against human SAS cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=14 μM
HaCaT cells	Function assay		48 h	Antihyperproliferative activity against human HaCaT cells assessed as inhibition of cell growth after 48 hrs by phase contrast microscopy, IC50=15.8 μM
HeLa cells	Cytotoxicity assay		48 h	Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=18 μM
CRL2796 cells	Cytotoxicity assay			Cytotoxicity against human CRL2796 cells assessed as inhibition of formazan formation at day 4 by measuring absorbance at 430 nm, IC50=21 μM
HL60 cells	Function assay	50 μM		Induction of necrosis in intact human HL60 cells assessed as cytosolic LDH release at 50 uM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	172.18	Formula	C₁₁H₈O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	58-27-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC 4170			Smiles	CC1=CC(=O)C2=CC=CC=C2C1=O

Solubility

In vitro
Batch:

DMSO : 34 mg/mL (197.46 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 34 mg/mL

Water : 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	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.	1.700mg/ml (9.87mM)	Taking the 1 mL working solution as an example, add 50 μL of 34 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.	1.700mg/ml (9.87mM)	Taking the 1 mL working solution as an example, add 50 μL of 34 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.

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	Cdc25 phosphatase DNA polymerase γ
In vitro	Menadione (Vitamin K3) prevents mitochondrial Ca(2+) uptake in normal pancreatic acinar cells, which permits rapid spread of Ca(2+) throughout the cell. Its-induced mitochondrial depolarisation is due to induction of the permeability transition pore. At nontoxic concentration, this compound results in a brief activation of extracellular signal-regulated kinase (ERK) and c-Jun N-terminal kinase (JNK) in the RALA255-10G rat hepatocyte cell line. It is equipotent against multidrug-resistant and parental leukemia cell lines with IC50 values of 13.5 mM and 18 mM, respectively. The compound inhibits the incorporation of radioactive thymidine, uridine and amino acids into DNA, RNA and protein, respectively, in three humancancer cell lines. At 1-20 mM, it dose- and time-dependently inhibits cell proliferation of AR4-2J cells. A concentration of 100 mM causes rapid cell death. This level (100 mM) induces DNA smear in electrophoresis indicative of necrosis, while lower concentrations (10-20 mM) induces a DNA ladder indicative of apoptosis. Concentrations of 1-20 mM induce wild-type P53, whereas 100 mM has a minor effect on wild-type P53. Treatment with it clearly affects the mitochondrial function of Jurkat T cells by inducing a collapse of the inner transmembrane potential (DeltaPsi(m)) and a decrease in inner membrane mass, which could be completely reversed by N-acetylcysteine.
References	[1] https://pubmed.ncbi.nlm.nih.gov/11861756/ [2] https://pubmed.ncbi.nlm.nih.gov/12774020/ [3] https://pubmed.ncbi.nlm.nih.gov/2018560/ [4] https://pubmed.ncbi.nlm.nih.gov/9378363/ [5] https://pubmed.ncbi.nlm.nih.gov/11726226/ [6] http://www.sciencedirect.com/science/article/pii/S0045206896910524 [7] https://pubmed.ncbi.nlm.nih.gov/24520419/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-JNK / JNK / p-c-Jun / c-Jun / p-ERK / ERK Cyclin B1 / CDK1 / CDC25C c-Fos / HO-1		20578144

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01094444	Completed	Folliculitis	Per Pfeiffer\|Odense University Hospital	May 2010	Phase 2
NCT00656786	Completed	EGFR Inhibitor-associated Rash	Spectrum Pharmaceuticals Inc	April 3 2008	Phase 1

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Handling Instructions

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Menadione (Vitamin K3) phosphatase inhibitor

Chemical Structure

Molecular Weight: 172.18