1. Anti-infection Apoptosis
  2. HIV Apoptosis
  3. Mitoguazone

Mitoguazone  (Synonyms: Methylglyoxal-bis(guanylhydrazone); MGBG; Methyl-GAG)

Cat. No.: HY-106634 Purity: 99.33%
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Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment.

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

Mitoguazone Chemical Structure

Mitoguazone Chemical Structure

CAS No. : 459-86-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
USD 165 In-stock
Solution
10 mM * 1 mL in Water USD 165 In-stock
Solid
5 mg USD 150 In-stock
10 mg USD 220 In-stock
50 mg USD 610 In-stock
100 mg   Get quote  
200 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Mitoguazone:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Mitoguazone

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment[1][2][3][4].

Cellular Effect
Cell Line Type Value Description References
CHO IC50
3.3 μM
Compound: MGBG
Cytotoxicity against CHO cells expressing MGBG polyamine transporter after 48 hrs by MTT assay
Cytotoxicity against CHO cells expressing MGBG polyamine transporter after 48 hrs by MTT assay
[PMID: 20064676]
CHO-MG IC50
> 100 μM
Compound: MGBG
Cytotoxicity against MGBG polyamine transporter deficient CHO-MG cells after 48 hrs by MTT assay
Cytotoxicity against MGBG polyamine transporter deficient CHO-MG cells after 48 hrs by MTT assay
[PMID: 20064676]
In Vitro

Mitoguazone competitively inhibits spermidine synthesis in lymphocytes at concentrations as low as 0.5 μg/mL. Levels of 30 μg/mL or more inhibit protein synthesis and mitochondrial respiration[1].
The ability of Mitoguazone to induce apoptosis by inhibiting the polyamine pathway is assessed in three Burkitt's lymphoma cell lines (Raji, Ramos and Daudi) and one prostate carcinoma cell line (MPC 3). Mitoguazone induces apoptosis in all the different human cancer cell lines tested in a concentration- and time-dependent way, and triggers a p53-independent programmed cell death in the human breast cancer MCF7 cell line[2].

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

In Vivo

The influence of different stages of leukemia P388 on the pharmacokinetics of the antineoplastic agent Mitoguazone in mice is investigated. Independent of the tumor stage investigated, the total clearance of mitoguazone is slightly reduced reflecting a moderate increase of AUC in the serum of leukemia-bearing animals. Furthermore, in an advanced tumor stage the drug levels in kidneys, liver, spleen and serum are found to be elevated to some extent in comparison to tumor-free controls in contrast to an earlier stage of leukemia[5].

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

Clinical Trial
Molecular Weight

184.20

Formula

C5H12N8

CAS No.
Appearance

Solid

Color

Light brown to brown

SMILES

CC(/C=N/NC(N)=N)=N\NC(N)=N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (271.44 mM; ultrasonic and adjust pH to 9 with HCl)

DMSO : 8.33 mg/mL (45.22 mM; ultrasonic and warming and heat to 60°C; 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 5.4289 mL 27.1444 mL 54.2888 mL
5 mM 1.0858 mL 5.4289 mL 10.8578 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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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)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

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:  PBS

    Solubility: 4 mg/mL (21.72 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.33%

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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 5.4289 mL 27.1444 mL 54.2888 mL 135.7220 mL
5 mM 1.0858 mL 5.4289 mL 10.8578 mL 27.1444 mL
10 mM 0.5429 mL 2.7144 mL 5.4289 mL 13.5722 mL
15 mM 0.3619 mL 1.8096 mL 3.6193 mL 9.0481 mL
20 mM 0.2714 mL 1.3572 mL 2.7144 mL 6.7861 mL
25 mM 0.2172 mL 1.0858 mL 2.1716 mL 5.4289 mL
30 mM 0.1810 mL 0.9048 mL 1.8096 mL 4.5241 mL
40 mM 0.1357 mL 0.6786 mL 1.3572 mL 3.3931 mL
H2O 50 mM 0.1086 mL 0.5429 mL 1.0858 mL 2.7144 mL
60 mM 0.0905 mL 0.4524 mL 0.9048 mL 2.2620 mL
80 mM 0.0679 mL 0.3393 mL 0.6786 mL 1.6965 mL
100 mM 0.0543 mL 0.2714 mL 0.5429 mL 1.3572 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Help & FAQs
  • 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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Mitoguazone
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