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  3. Monobenzone

Monobenzone is a potent skin depigmenting agent. Monobenzone induces depigmentation and exhibits good potential for vitiligo research. Monobenzone is a potent inhibitor of RNR (Ribonucleotide reductase) enzyme activity by targeting RRM2 (a regulatory small subunit M2 of RNR) protein, and thus has significant anti-leukemia efficacy in vitro and in vivo. Monobenzone inhibits acute myeloid leukemia (AML) cells proliferation and DNA synthesis, induces cell cycle arrest, and Apoptosis .

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Monobenzone Chemical Structure

Monobenzone Chemical Structure

CAS No. : 103-16-2

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Monobenzone:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Monobenzone

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Monobenzone is a potent skin depigmenting agent. Monobenzone induces depigmentation and exhibits good potential for vitiligo research. Monobenzone is a potent inhibitor of RNR (Ribonucleotide reductase) enzyme activity by targeting RRM2 (a regulatory small subunit M2 of RNR) protein, and thus has significant anti-leukemia efficacy in vitro and in vivo. Monobenzone inhibits acute myeloid leukemia (AML) cells proliferation and DNA synthesis, induces cell cycle arrest, and Apoptosis [1][2].

In Vitro

Monobenzone (2.5- 40 μM, 24-48 h) inhibits AML cells proliferation with IC50s of 6-18 μM and causes dose dependent DNA synthesis inhibition, induces cell cycle arrest and apoptosis in KG-1A, MOLM13, NB4 cells[2].
Monobenzone (0-10 μM, 24-48 h) blocks DNA damage repair in KG-1A, MOLM13, NB4 cells[2].
Monobenzone (0-100 μM, 72 h) overcomes the drug resistance to Ara-C (Cytarabine (HY-13605)), DOX (Doxorubicin(HY-15142)) and HU (Hydroxyurea(HY-B0313)) in KG-1A-ARAC, KG-1A-DOX, and KG-1A-HU cells[2].
Monobenzone (0-100 μM, 72 h) with the Bcl-2 inhibitor ABT-737 (HY-50907) synergistically inhibits cell the growth with an IC50 of 2.52 μM in MOLM13 cells and an IC50 of 9.69 μM in KG-1A cells compared with monobenzone alone[2].

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

Cell Viability Assay [2]

Cell Line: Ara-C-, DOX-, and HU-resistant KG-1A cell lines (KG-1A-ARAC, KG-1A-DOX, and KG-1A-HU)
Concentration: 3, 10, 30, 100 μM
Incubation Time: 72 h
Result: Inhibited the growth of KG-1A, KG-1A-ARAC, KG-1A-DOX, and KG-1A-HU cells in a dose-dependent manner with IC50 values of 13, 16, 24, 37 μM.

Cell Proliferation Assay [2]

Cell Line: KG-1A, MOLM13, NB4 cells (AML cells)
Concentration: 0.25, 1, 4, 16, 64, 256, 1024 μM
Incubation Time: 72 h
Result: Exerted a strong, dose-dependent inhibitory effect on the proliferation of treated AML cells, with IC50 values of approximately 6-18 μM.

Cell Cycle Analysis [2]

Cell Line: KG-1A, MOLM13, NB4 cells
Concentration: 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Induced cell cycle arrest at the S phase.
dNTP precursors significantly reversed the cell cycle arrest in S phase, suggesting that RNR (Ribonucleotide reductase) is the active target in the treated cells, resulting in the inhibition of DNA synthesis and cell proliferation.

Western Blot Analysis [2]

Cell Line: KG-1A, MOLM13, NB4 cells
Concentration: 0, 1.25, 2.5, 5, 10μM
Incubation Time: 24, 48 h
Result: Increased r-H2Ax dose-dependently, blocking DNA damage repair in the treated cells
In Vivo

Monobenzone (40%, 60% cream, daily, 30-50 days) induces skin depigmentation on the non exposed sites and that the severity of lesions depends on drug dosage in C57BL/6 mice [1].
Monobenzone (100 - 200 mg/kg, i.p., daily, 2 weeks) effectively inhibits AML cell (MOLM13 cells) xenograft growth in nude mice [2].

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

Animal Model: Rag1 knockout and healthy C57BL/6 mice [1].
Dosage: 40%, 60% Monobenzone cream
Administration: daily, 30-50 days
Result: Developed depigmentation on exposed site and non-exposed site.
Developed depigmentation restricted only in the drug exposure area in Rag1 KO mice.
Induced depigmentation in the mice also indicated loss of melanocytes in the lesional skin and CD8+ T infiltration in the perilesional skin.
Animal Model: Two hundred microlitres of PBS containing 2 *105 MOLM13 cells were injected subcutaneously into 4-week-old male nude mice[2].
Dosage: 100, 200 mg/kg
Administration: i.p., daily, 2 weeks
Result: Significantly reduced AML cell growth in nude mice compared with the solvent control.
Inhibited AML cell growth in vivo with relatively low toxicity.
Molecular Weight

200.24

Formula

C13H12O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC1=CC=C(C=C1)OCC2=CC=CC=C2

Shipping

Room temperature in continental US; may vary elsewhere.

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

Methanol : 400 mg/mL (1997.63 mM; Need ultrasonic)

DMSO : ≥ 100 mg/mL (499.41 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.9941 mL 24.9704 mL 49.9408 mL
5 mM 0.9988 mL 4.9941 mL 9.9882 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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Volume (final)

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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: ≥ 2.08 mg/mL (10.39 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (10.39 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(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: 99.93%

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / Methanol 1 mM 4.9941 mL 24.9704 mL 49.9408 mL 124.8521 mL
5 mM 0.9988 mL 4.9941 mL 9.9882 mL 24.9704 mL
10 mM 0.4994 mL 2.4970 mL 4.9941 mL 12.4852 mL
15 mM 0.3329 mL 1.6647 mL 3.3294 mL 8.3235 mL
20 mM 0.2497 mL 1.2485 mL 2.4970 mL 6.2426 mL
25 mM 0.1998 mL 0.9988 mL 1.9976 mL 4.9941 mL
30 mM 0.1665 mL 0.8323 mL 1.6647 mL 4.1617 mL
40 mM 0.1249 mL 0.6243 mL 1.2485 mL 3.1213 mL
50 mM 0.0999 mL 0.4994 mL 0.9988 mL 2.4970 mL
60 mM 0.0832 mL 0.4162 mL 0.8323 mL 2.0809 mL
80 mM 0.0624 mL 0.3121 mL 0.6243 mL 1.5607 mL
100 mM 0.0499 mL 0.2497 mL 0.4994 mL 1.2485 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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Product Name:
Monobenzone
Cat. No.:
HY-30272
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