2. Metabolic Enzyme/Protease Epigenetics Cell Cycle/DNA Damage
  3. Endogenous Metabolite PARP
  4. 7-Methylguanine

7-Methylguanine is an orally active and competitive PARP-1 inhibitor with a Ki value of 61 μM. 7-Methylguanine is a metabolite of nucleic acids. 7-Methylguanine has anticancer activity against uterine sarcoma and colon adenocarcinoma. 7-Methylguanine is used as a probe for protein-DNA interactions.

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7-Methylguanine Chemical Structure

7-Methylguanine Chemical Structure

CAS No. : 578-76-7

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Based on 1 publication(s) in Google Scholar

Other Forms of 7-Methylguanine:

7-Methylguanine Related Antibodies

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Description

7-Methylguanine is an orally active and competitive PARP-1 inhibitor with a Ki value of 61 μM. 7-Methylguanine is a metabolite of nucleic acids. 7-Methylguanine has anticancer activity against uterine sarcoma and colon adenocarcinoma. 7-Methylguanine is used as a probe for protein-DNA interactions[1][2][3][4][5][6].

IC50 & Target[1][2][3][4][5][6]

Human Endogenous Metabolite

 

PARP-1

61 μM (Ki)

In Vitro

7-Methylguanine (0-200 μM) inhibits PARP1 enzymatic activity in a dose-dependent manner[1].
7-Methylguanine is a competitive PARP-1 inhibitor with a Ki value of 61 μM[2].
7-Methylguanine (0-450 μM) inhibits the dissociation of the PARP-1-DNA complex due to suppression of PARP-1 catalytic activity[2].
7-Methylguanine (0.02-0.2 mg/mL; 24 h) does not produce DNA damage in immortalized human kidney epithelial cells (NKE-hTERT)[3].

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

7-Methylguanine Related Antibodies
In Vivo

7-Methylguanine (50 mg/kg; p.o..; 3 times per week; 4 weeks for toxicology study) exerts no adverse effects or changes in morphology in CBA, BALB/c, and C57BL/6 mice as well as inhibits tumor growth in CBA mice with uterine sarcoma US-322[3].
7-Methylguanine (50 mg/kg; i.g.; 3 times per week) effectively penetrates tumor tissue and suppresses colon adenocarcinoma growth in BALB/c mice with transplanted Akatol tumor[5].

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

Animal Model: CBA, BALB/c, C57BL/6 mice (6-week-old); toxicology study and carcinogenicity study[3]
Dosage: 50 mg/kg, 200 mg/kg, 600 mg/kg
Administration: Intragastric administration, 3 times per week for 4 weeks (for 50 mg/kg group), 3 times per week for 1 week (for 200 mg/kg group), single dose (for 600 mg/kg group)
Result: Exerted no adverse effects or changes in morphology (at 50 mg/kg for 3 times per week up to 4 weeks).
Caused some lymphoid infiltrates in lungs, liver and spleen, and focal lymphoid hyperplasia in intestines in CBA mice (at 600 mg/kg single dose).
Did not induce mutations or structural chromosomal abnormalities, and had no blastomogenic activity.
Significantly inhibited tumor growth in CBA mice with uterine sarcoma US-322 (at 50 mg/kg 3 times per week).
Had an antitumor effect in CBA mice with cervical squamous cell carcinoma RShM-5 (alone for 1 week).
Inhibited tumor growth in combination with Cisplatin (HY-17394) within a week after inoculation.
Molecular Weight

165.15

Formula

C6H7N5O
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C1NC(N)=NC2=C1N(C)C=N2
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

1M NaOH : 100 mg/mL (605.51 mM; Need ultrasonic)

H2O : 4.72 mg/mL (28.58 mM; ultrasonic and adjust pH to 11 with 1 M NaOH)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 6.0551 mL 30.2755 mL 60.5510 mL
5 mM 1.2110 mL 6.0551 mL 12.1102 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 (protect from light). 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
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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

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C1

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V1

=
Concentration (final)

C2

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V2

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

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g

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working 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).
Purity & Documentation
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 (protect from light). 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
H2O / 1M NaOH 1 mM 6.0551 mL 30.2755 mL 60.5510 mL 151.3775 mL
5 mM 1.2110 mL 6.0551 mL 12.1102 mL 30.2755 mL
10 mM 0.6055 mL 3.0276 mL 6.0551 mL 15.1378 mL
15 mM 0.4037 mL 2.0184 mL 4.0367 mL 10.0918 mL
20 mM 0.3028 mL 1.5138 mL 3.0276 mL 7.5689 mL
25 mM 0.2422 mL 1.2110 mL 2.4220 mL 6.0551 mL
1M NaOH 30 mM 0.2018 mL 1.0092 mL 2.0184 mL 5.0459 mL
40 mM 0.1514 mL 0.7569 mL 1.5138 mL 3.7844 mL
50 mM 0.1211 mL 0.6055 mL 1.2110 mL 3.0276 mL
60 mM 0.1009 mL 0.5046 mL 1.0092 mL 2.5230 mL
80 mM 0.0757 mL 0.3784 mL 0.7569 mL 1.8922 mL
100 mM 0.0606 mL 0.3028 mL 0.6055 mL 1.5138 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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7-Methylguanine Related Classifications

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.

Keywords:

7-Methylguanine578-76-7Endogenous MetabolitePARPpoly ADP ribose polymeraseCBABALB/c C57BL/6colon adenocarcinomaUS-322Inhibitorinhibitorinhibit

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