Guanazole
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Guanazole is a ribonucleotide reductase (RNR) inhibitor that blocks replicative DNA synthesis by inhibiting deoxyribonucleotide biosynthesis. Guanazole selectively inhibits DNA synthesis in rapidly proliferating tissues, induces replication stress and G2/M phase arrest in Schizosaccharomyces pombe, and exhibits myelosuppressive, immunosuppressive, and anti-L1210 leukemia activities. Guanazole does not induce DNA repair and only shows slight mutagenicity towards Salmonella typhimurium TA102. Guanazole serves as an alternative tool to Hydroxyurea (HY-B0313) for replication checkpoint studies in Schizosaccharomyces pombe. Guanazole can be applied in research related to leukemia and solid tumors.
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- Pureté : 99.74%
- CAS No.: 1455-77-2
- Formule: C2H5N5
- Masse moléculaire:99.09
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
In Vitro
Guanazole (50-250 mM; 8 h) induces acute replication stress in rad3Δ Schizosaccharomyces pombe cells; due to the presence of additional stress responses, the cytotoxicity at high doses is unexpectedly reduced[3].
Guanazole (200 mM; 6 h) induces acute replication stress in Schizosaccharomyces pombe rad3Δ and cds1Δ cells, and both mutants exhibit comparable sensitivity due to additional G2/M checkpoint stress[3].
Guanazole (50-300 mM; 3 h) induces Rad3-dependent phosphorylation of Mrc1-Thr645 in wild-type Schizosaccharomyces pombe cells, and this site is a marker of replication stress[3].
Guanazole (200 mM; 6 h) induces G2/M phase cell cycle arrest accompanied by replication stress in both wild-type and rad3Δ Schizosaccharomyces pombe cells after 6 h [3].
Guanazole (200 mM; 3 h) inhibits the "cut" phenotype of premature mitosis in rad3Δ Schizosaccharomyces pombe cells, and does not induce elongation in wild-type, mrc1Δ, or erg11-1 cells. This result is consistent with G2/M cell cycle arrest[3].
Guanazole is an inhibitor of the ribonucleotide reductase M2 subunit, with a potency approximately one-quarter that of Hydroxyurea, and its inhibitory activity can be enhanced by iron chelators [5].
Guanazole exhibits cross-resistance in hydroxyurea-resistant Chinese hamster ovary cells and mouse L cells with upregulated or altered expression of ribonucleotide reductase[5].
Guanazole (15 mM; 18 h) inhibits replicative DNA synthesis in primary rat hepatocyte cultures[1].
Guanazole (15 mM; 18 h) supports the detection of DNA repair synthesis in primary cultured rat hepatocytes induced by a variety of genotoxic agents. Its detection sensitivity is comparable to that of Hydroxyurea (HY-B0313) for most agents, higher for MNNG, and lower for aflatoxin B1 and H2O2[1].
Guanazole (48 h) exhibits acute toxicity to Daphnia magna, with an EC50 of 4.13 mg/L[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:wild-type (TK48), rad3Δ, mrc1Δ, and erg11-1 Schizosaccharomyces pombe cells
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Concentration:50 mM, 100 mM, 150 mM, 200 mM, 250 mM, 300 mM
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Incubation Time:3 h
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Result:Increased Mrc1-Thr645 phosphorylation in a concentration-dependent manner in wild-type cells, with levels at 200 mM to 300 mM comparable to those in cells treated with 15 mM hydroxyurea.
Increased Mrc1 protein levels up to 150 mM, then decreased at concentrations above 150 mM.
Induced Rad3-dependent Mrc1 phosphorylation, with lower levels in erg11-1 cells compared to wild-type cells.
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Cell Line:wild-type (TK48) and rad3Δ Schizosaccharomyces pombe cells
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Concentration:200 mM
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Incubation Time:0, 1, 2, 3, 4, 5 and 6 h
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Result:Arrested wild-type and rad3Δ cells at the G2/M phase of the cell cycle throughout the 6-hour incubation period, unlike hydroxyurea treatment which caused S-phase arrest.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DBA/2J (female, 16-18 g)[2]
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Dosage:30 mg/mL
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Administration:i.v.; 0.3 mL/hr; 47 hr
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Result:Achieved tissue levels (μg/g wet weight, ~70% of steady-state levels) of 407.6 in spleen, 398.1 in thymus, 233.3 in heart, 145.1 in brain, 248.4 in kidney, 215.9 in liver; bone marrow levels were not measurable.
Reduced 14C-uridine incorporation into DNA to 16.4% of saline control in spleen, 33.6% in thymus, 58.4% in bone marrow, 74.5% in heart, 81.4% in brain, 103.8% in kidney, and increased it to 177.0% in liver.
Reduced 14C-uridine incorporation into RNA to 43.1% of saline control in spleen, 84.3% in thymus, 91.0% in bone marrow, 82.3% in heart, and increased it to 104.3% in brain, 102.1% in kidney, 131.8% in liver.
Left total DNA content per gram of tissue unchanged across all tissues.
Chemical Information
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CAS No. 1455-77-2
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Appearance Solid
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Masse moléculaire 99.09
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Formule C2H5N5
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SMILES
NC1=NN=C(N)N1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (1009.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 4 mg/mL (40.37 mM); Clear solution
This protocol yields a clear solution of ≥ 4 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (40.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 4 mg/mL (40.37 mM); Clear solution
This protocol yields a clear solution of ≥ 4 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (40.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (286 KB)
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SDS (623 KB)
- English - EN (623 KB)
- Français - FR (623 KB)
- Deutsch - DE (623 KB)
- Norwegian - NO (623 KB)
- Español - ES (623 KB)
- Swedish - SV (623 KB)
- Italian - IT (623 KB)
- Korean - KR (623 KB)
- Portuguese - PT (623 KB)
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Instruction de manipulation (2659 KB)
Références
[5]. HY-W015940-3.pdf
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 10.0918 mL | 50.4592 mL | 100.9184 mL | 252.2959 mL |
| 5 mM | 2.0184 mL | 10.0918 mL | 20.1837 mL | 50.4592 mL | |
| 10 mM | 1.0092 mL | 5.0459 mL | 10.0918 mL | 25.2296 mL | |
| 15 mM | 0.6728 mL | 3.3639 mL | 6.7279 mL | 16.8197 mL | |
| 20 mM | 0.5046 mL | 2.5230 mL | 5.0459 mL | 12.6148 mL | |
| 25 mM | 0.4037 mL | 2.0184 mL | 4.0367 mL | 10.0918 mL | |
| 30 mM | 0.3364 mL | 1.6820 mL | 3.3639 mL | 8.4099 mL | |
| 40 mM | 0.2523 mL | 1.2615 mL | 2.5230 mL | 6.3074 mL | |
| 50 mM | 0.2018 mL | 1.0092 mL | 2.0184 mL | 5.0459 mL | |
| 60 mM | 0.1682 mL | 0.8410 mL | 1.6820 mL | 4.2049 mL | |
| 80 mM | 0.1261 mL | 0.6307 mL | 1.2615 mL | 3.1537 mL | |
| 100 mM | 0.1009 mL | 0.5046 mL | 1.0092 mL | 2.5230 mL |
Guanazole Related Classifications
HY-W015940 Related Classifications
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