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  5. 4-Methylumbelliferone

4-Methylumbelliferone  (Synonyms: Hymecromone; 4-MU)

Cat. No.: HY-N0187 Purity: 99.79%
SDS COA Handling Instructions

4-Methylumbelliferone is a hyaluronic acid biosynthesis inhibitor with antitumoral and antimetastatic effects.

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

4-Methylumbelliferone Chemical Structure

4-Methylumbelliferone Chemical Structure

CAS No. : 90-33-5

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10 mM * 1 mL in DMSO
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of 4-Methylumbelliferone:

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

4-Methylumbelliferone is a hyaluronic acid biosynthesis inhibitor with antitumoral and antimetastatic effects.

IC50 & Target

hyaluronic acid[1]

Cellular Effect
Cell Line Type Value Description References
A2780 IC50
> 2 μM
Compound: 7-hydroxy-4-methylcoumarin
Antiproliferative activity against human A2780 cells after 48 hrs by MTT assay
Antiproliferative activity against human A2780 cells after 48 hrs by MTT assay
[PMID: 25350923]
A549 IC50
> 100 μM
Compound: Hymecromone
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 24 hrs
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 24 hrs
[PMID: 37252094]
HEK293 IC50
100 μM
Compound: 4-Methylumbelliferone
Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method
Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method
[PMID: 21030469]
HEK293 IC50
100 μM
Compound: 4-Methylumbelliferone
Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method
Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method
[PMID: 21030469]
HepG2 IC50
> 100 μM
Compound: Hymecromone
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 24 hrs
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 24 hrs
[PMID: 37252094]
J774.A1 IC50
> 100 μM
Compound: Hymecromone
Cytotoxicity against mouse J774.A1 cells assessed as reduction in cell viability measured after 24 hrs
Cytotoxicity against mouse J774.A1 cells assessed as reduction in cell viability measured after 24 hrs
[PMID: 37252094]
MCF7 IC50
54.77 μM
Compound: Hymecromone
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs
[PMID: 37252094]
NIH3T3 IC50
23.99 μM
Compound: Hymecromone
Cytotoxicity against mouse 3T3 cells assessed as reduction in cell viability measured after 24 hrs
Cytotoxicity against mouse 3T3 cells assessed as reduction in cell viability measured after 24 hrs
[PMID: 37252094]
SiHa IC50
> 100 μM
Compound: Hymecromone
Cytotoxicity against human SiHa cells assessed as reduction in cell viability measured after 24 hrs
Cytotoxicity against human SiHa cells assessed as reduction in cell viability measured after 24 hrs
[PMID: 37252094]
SK-MEL-28 IC50
0.58 μM
Compound: 6
Anticancer activity against human SK-MEL-28 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Anticancer activity against human SK-MEL-28 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
[PMID: 37197457]
SK-MEL3 IC50
1.6 μM
Compound: 6
Anticancer activity against human SK-MEL3 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Anticancer activity against human SK-MEL3 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
[PMID: 37197457]
U-937 IC50
> 2000 μM
Compound: 12
Growth inhibition of human U937 cells by [3H]thymidine incorporation assay
Growth inhibition of human U937 cells by [3H]thymidine incorporation assay
[PMID: 18060791]
U-937 CC50
> 2000 μM
Compound: 10
Cytotoxicity against human U937 cells after 48 hrs by trypan blue assay
Cytotoxicity against human U937 cells after 48 hrs by trypan blue assay
[PMID: 22925447]
U-937 CC50
> 2000 μM
Compound: 12
Cytotoxicity against human U937 cells by trypan blue assay after 48 hrs
Cytotoxicity against human U937 cells by trypan blue assay after 48 hrs
[PMID: 18060791]
U-937 CC50
> 2000 μM
Compound: 7
Cytotoxicity against human U937 cells by trypan blue assay after 48 hrs
Cytotoxicity against human U937 cells by trypan blue assay after 48 hrs
[PMID: 18060791]
U-937 IC50
710.9 μM
Compound: 7
Growth inhibition of human U937 cells by [3H]thymidine incorporation assay
Growth inhibition of human U937 cells by [3H]thymidine incorporation assay
[PMID: 18060791]
U-937 IC50
710.9 μM
Compound: 10
Antiproliferative activity against human U937 cells assessed as incorporation of [3H]-methyl-thymidine after 12 hrs by scintillation counting
Antiproliferative activity against human U937 cells assessed as incorporation of [3H]-methyl-thymidine after 12 hrs by scintillation counting
[PMID: 22925447]
In Vitro

4-Methylumbelliferone (4-MU) affects several key steps of angiogenesis, including endothelial cell proliferation, adhesion, tube formation, and extracellular matrix remodeling. Half-maximal inhibitory concentrations (IC50) values in the proliferation assay are 0.65±0.04 and 0.37±0.03 mM for human microvascular endothelial cells (HMEC) and RF-24 endothelial cells, respectively. 4-Methylumbelliferone (2 mM) treatment for 24 h induces apoptosis in 13% of HMEC and 5% of RF-24 cells. The number of adherent endothelial cells decreases by >20% after 24 h of treatment with 1 mM 4-Methylumbelliferone. Minimal inhibitory concentrations in the tube formation assay are 2 and 0.5 mM 4-Methylumbelliferone for HMEC and RF-24, respectively. Matrix metalloproteinase-2 expression is differentially altered upon 4-Methylumbelliferone treatment in both tested endothelial cell lines[1].

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

Clinical Trial
Molecular Weight

176.17

Formula

C10H8O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C=C(C)C2=CC=C(O)C=C2O1

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (567.63 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 5.6763 mL 28.3817 mL 56.7634 mL
5 mM 1.1353 mL 5.6763 mL 11.3527 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (14.19 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 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (14.19 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  50% PEG300    50% Saline

    Solubility: 50 mg/mL (283.82 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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
References
Cell Assay
[1]

The MTT dye reduction assay in 96-well microplates is used. The assay is dependent on the reduction of MTT by mitochondrial dehydrogenases of viable cells to a blue formazan product, which can be measured spectrophotometrically. Endothelial cells (2.5×103 cells in a total volume of 100 μL of complete medium) are incubated in each well with serial dilutions of 4-Methylumbelliferone (4-MU) (0, 0.5, 1, 1.5 and 2 mM). After 3 days of incubation in the dark (37°C, 5% CO2 in a humid atmosphere), 10 μL of MTT (5 mg/mL in PBS) is added to each well, and the plate is incubated for further a 4 h (37°C). The formazan is dissolved in 150 μL of 0.04 N HCl-2 propanol, and samples are spectrophotometrically measured at 550 nm. All determinations are carried out in quadruplicate, and at least three independent experiments are carried out. IC50 values are calculated as those concentrations of compound yielding 50% cell survival, taking the values obtained for control as 100%[1].

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

References

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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 5.6763 mL 28.3817 mL 56.7634 mL 141.9084 mL
5 mM 1.1353 mL 5.6763 mL 11.3527 mL 28.3817 mL
10 mM 0.5676 mL 2.8382 mL 5.6763 mL 14.1908 mL
15 mM 0.3784 mL 1.8921 mL 3.7842 mL 9.4606 mL
20 mM 0.2838 mL 1.4191 mL 2.8382 mL 7.0954 mL
25 mM 0.2271 mL 1.1353 mL 2.2705 mL 5.6763 mL
30 mM 0.1892 mL 0.9461 mL 1.8921 mL 4.7303 mL
40 mM 0.1419 mL 0.7095 mL 1.4191 mL 3.5477 mL
50 mM 0.1135 mL 0.5676 mL 1.1353 mL 2.8382 mL
60 mM 0.0946 mL 0.4730 mL 0.9461 mL 2.3651 mL
80 mM 0.0710 mL 0.3548 mL 0.7095 mL 1.7739 mL
100 mM 0.0568 mL 0.2838 mL 0.5676 mL 1.4191 mL
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  • Do most proteins show cross-species activity?

    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.

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