Mizoribine
Based on 5 publication(s) in Google Scholar
Mizoribine (NSC 289637), an imidazole nucleoside, inhibits HCV RNA replication with IC50 of approximately 100 μM for anti-HCV activity. Immunosuppressant. Mizoribine, an IMPDH inhibitor, inhibits replication of SARS-CoV with IC50s of 3.5 μg/mL and 16 μg/mL for SARS-CoV Frankfurt-1 and SARS-CoV HKU39849, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.99%
- CAS. Nr.: 50924-49-7
- Formel: C9H13N3O6
- Molecular Weight:259.22
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) Mizoribine
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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Bio/Physico-chemical Assay
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Apoptosis Analysis
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WB
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WB
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Biologische Aktivität
Beschreibung
IC50 & Target
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-1080 | IC50 |
>100 μg/mL
Compound: bredinin
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In vitro inhibitory activity against growth of Human fibrosarcoma (HT1080) cells
In vitro inhibitory activity against growth of Human fibrosarcoma (HT1080) cells
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[PMID: 1995901] |
| KB | IC50 |
>100 μg/mL
Compound: bredinin
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In vitro inhibitory activity against growth of Human oral epidermoid carcinoma (KB) cells
In vitro inhibitory activity against growth of Human oral epidermoid carcinoma (KB) cells
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[PMID: 1995901] |
| Lu-65 | IC50 |
>100 μg/mL
Compound: bredinin
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In vitro inhibitory activity against growth of Human gaint cell carcinoma (Lu-65) cells
In vitro inhibitory activity against growth of Human gaint cell carcinoma (Lu-65) cells
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[PMID: 1995901] |
| OST | IC50 |
>100 μg/mL
Compound: bredinin
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In vitro inhibitory activity against growth of Human osteosarcoma (OST) cells
In vitro inhibitory activity against growth of Human osteosarcoma (OST) cells
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[PMID: 1995901] |
| PC-13 | IC50 |
>100 μg/mL
Compound: bredinin
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In vitro inhibitory activity against growth of Human large-cell carcinoma (PC-13) cells
In vitro inhibitory activity against growth of Human large-cell carcinoma (PC-13) cells
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[PMID: 1995901] |
| PC-3 | IC50 |
>100 μg/mL
Compound: bredinin
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In vitro inhibitory activity against growth of Human lung adenocarcinoma (PC-3) cells.
In vitro inhibitory activity against growth of Human lung adenocarcinoma (PC-3) cells.
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[PMID: 1995901] |
| PC-6 | IC50 |
49 μg/mL
Compound: bredinin
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In vitro inhibitory activity against growth of Human lung small-cell carcinoma (PC-6) cells
In vitro inhibitory activity against growth of Human lung small-cell carcinoma (PC-6) cells
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[PMID: 1995901] |
| SW480 | IC50 |
42 μg/mL
Compound: bredinin
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In vitro inhibitory activity against growth of Human colon adenocarcinoma (SW-480) cells
In vitro inhibitory activity against growth of Human colon adenocarcinoma (SW-480) cells
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[PMID: 1995901] |
| T-24 | IC50 |
>100 μg/mL
Compound: bredinin
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In vitro inhibitory activity against growth of Human bladder transitional-cell carcinoma (T-24) cells
In vitro inhibitory activity against growth of Human bladder transitional-cell carcinoma (T-24) cells
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[PMID: 1995901] |
| Vero | CC50 |
>700 μM
Compound: mizoribin
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Cytotoxicity against Vero E6 cells
Cytotoxicity against Vero E6 cells
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[PMID: 17336519] |
| Vero | IC50 |
13.5 μM
Compound: mizoribin
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Antiviral activity against SARS-CoV Frankfurt1 in Vero E6 cells by plaque reduction assay
Antiviral activity against SARS-CoV Frankfurt1 in Vero E6 cells by plaque reduction assay
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[PMID: 17336519] |
In Vitro
Mizoribine, isolated from culture medium of the mold Eupenicillium brefeldianum M-2166, acts as an immunosuppressant which exerts its effects without severe side effects[1].
Mizoribine is an inosine-5′-monophosphate dehydrogenase (IMPDH) inhibitorused for renal transplantation, autoimmune diseases and steroid-resistant nephrotic syndrome [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male DBA/1 J mice with collagen-induced arthritis[3]
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Dosage:10, 20 and 50 mg/kg
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Administration:Administered orally 5 days a week for 12 weeks
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Result:Showed dose-dependency of the suppressive effect.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 50924-49-7
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Appearance Solid
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Molecular Weight 259.22
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Formel C9H13N3O6
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Color White to off-white
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SMILES
OC[C@@H]1[C@@H](O)[C@@H](O)[C@H](N2C(O)=C(C(N)=O)N=C2)O1
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Synonyms
NSC 289637; HE 69
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Structure Classification
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Initial Source
Eupenicillium brefeldianum M-2166
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Nucleic Acids Res
COVID19 Drug Repository: text-mining the literature in search of putative COVID19 therapeutics. [Abstract]2021 Jan 8;49(D1):D1113-D1121. PMID: 33166390 -
Cell Death Differ
AF9 targets acetyl-modified STAT6 to diminish purine metabolism and accelerate cell apoptosis during metastasis. [Abstract]2023 Jul;30(7):1695-1709. PMID: 37308587
Mizoribine purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2023 Jul;30(7):1695-1709. [Abstract]
Mizoribine (0, 5, 10, 20, 40, 80 μM; 36 h) inhibited cell viability in 786-0 cells with restored expression of WT- or K284R-STAT6.
Mizoribine purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2023 Jul;30(7):1695-1709. [Abstract]
Mizoribine (10, 20 μM; 12 h) inhibited the biosynthesis of guanine and adenine in 786-0 cells stably expressing shSTAT6, with restored expression of WT- or K284R-STAT6.
Mizoribine purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2023 Jul;30(7):1695-1709. [Abstract]
Mizoribine (10, 20 μM; 24 h) upregulated the percentage of apoptotic cells in cells expressing K284R-STAT6 to the same degree as the cells expressing WT-STAT6.
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mBio
Heat Shock Protein 60 Is Involved in Viral Replication Complex Formation and Facilitates Foot and Mouth Virus Replication by Stabilizing Viral Nonstructural Proteins 3A and 2C. [Abstract]2022 Oct 26;13(5):e0143422. PMID: 36106732
Mizoribine purchased from MedChemExpress. Usage Cited in: mBio. 2022 Oct 26;13(5):e0143422. [Abstract]
Mizoribine (100 mM; 2 h) treated PK-15 cells were then infected with FMDV type O at an MOI of 1. Mizoribine showed that the inhibition of HSP60 significantly reduced viral protein level and virus production at 4, 6, and 8 h postinfection (hpi).
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Molecules
In Vitro and in Vivo Antiviral Activity of Mizoribine Against Foot-And-Mouth Disease Virus. [Abstract]2019 May 3;24(9):1723. PMID: 31058822
Mizoribine purchased from MedChemExpress. Usage Cited in: Molecules. 2019 May 3;24(9):1723. [Abstract]
Guanosine supplementation attenuated the anti-FMDV effect of mizoribine. Serial dilutions of guanosine (from 100 to 25 μM) are added to FMDV (100 TCID50 O/MY98/BY/2010)-infected IBRS-2 cells, when treated with 75 μM mizoribine for 48 h. (A) The cell viability of cells and (B) FMDV VP1 levels are analyzed.
Mizoribine purchased from MedChemExpress. Usage Cited in: Molecules. 2019 May 3;24(9):1723. [Abstract]
Mizoribine (6, 12, 25, 50, 75, 100 μM; 72 h) showed no cytotoxicity in IBRS-2 cells.
Mizoribine purchased from MedChemExpress. Usage Cited in: Molecules. 2019 May 3;24(9):1723. [Abstract]
Mizoribine (6, 12, 25, 50, 75, 100 μM; 48 h) inhibited FMDV infection in IBRS-2 cells viability with inhibition rates of approximately 63.01%, 82.03%, 90.89%, and 90.41% in cells treated with 25, 50, 75, and 100 µM, respectively.
Mizoribine purchased from MedChemExpress. Usage Cited in: Molecules. 2019 May 3;24(9):1723. [Abstract]
Mizoribine (12, 25, 50, 75, 100 μM; 12 h) inhibited the expression of FMDV protein in a dose-dependent manner in IBRS-2 cells were infected by 100 TCID50 O/MY98/BY/2010.
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bioRxiv
Systemic inhibition of de novo purine biosynthesis prevents weight gain and improves metabolic health by increasing thermogenesis and decreasing food intake. [Abstract]2024 Nov 1:2024.10.28.620705. PMID: 39553975
Lösungsmittel & Löslichkeit
In Vitro:
H2O : ≥ 100 mg/mL (385.78 mM)
DMSO : 62.5 mg/mL (241.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
* 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.
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.
* 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.08 mg/mL (8.02 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (8.02 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.
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.
Add each solvent one by one: PBS
Solubility: ≥ 100 mg/mL (385.78 mM); Clear solution
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (421 KB)
- English - EN (421 KB)
- Français - FR (421 KB)
- Deutsch - DE (421 KB)
- Norwegian - NO (421 KB)
- Español - ES (421 KB)
- Swedish - SV (421 KB)
- Italian - IT (421 KB)
- Korean - KR (421 KB)
- Portuguese - PT (421 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Naka K, et al. Mizoribine inhibits hepatitis C virus RNA replication: effect of combination with interferon-alpha. Biochem Biophys Res Commun. 2005 May 13;330(3):871-9. [Content Brief]
[2]. Saijo M, et al. Inhibitory effect of Mizoribine and ribavirin on the replication of severe acute respiratory syndrome (SARS)-associated coronavirus. Antiviral Res. 2005 Jun;66(2-3):159-63. [Content Brief]
[3]. Kamada H, et al. Effect of Mizoribine on collagen-induced arthritis in mice. Jpn J Pharmacol. 1996 Feb;70(2):169-75. [Content Brief]
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 / H2O | 1 mM | 3.8578 mL | 19.2888 mL | 38.5776 mL | 96.4439 mL |
| 5 mM | 0.7716 mL | 3.8578 mL | 7.7155 mL | 19.2888 mL | |
| 10 mM | 0.3858 mL | 1.9289 mL | 3.8578 mL | 9.6444 mL | |
| 15 mM | 0.2572 mL | 1.2859 mL | 2.5718 mL | 6.4296 mL | |
| 20 mM | 0.1929 mL | 0.9644 mL | 1.9289 mL | 4.8222 mL | |
| 25 mM | 0.1543 mL | 0.7716 mL | 1.5431 mL | 3.8578 mL | |
| 30 mM | 0.1286 mL | 0.6430 mL | 1.2859 mL | 3.2148 mL | |
| 40 mM | 0.0964 mL | 0.4822 mL | 0.9644 mL | 2.4111 mL | |
| 50 mM | 0.0772 mL | 0.3858 mL | 0.7716 mL | 1.9289 mL | |
| 60 mM | 0.0643 mL | 0.3215 mL | 0.6430 mL | 1.6074 mL | |
| 80 mM | 0.0482 mL | 0.2411 mL | 0.4822 mL | 1.2055 mL | |
| 100 mM | 0.0386 mL | 0.1929 mL | 0.3858 mL | 0.9644 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.
Mizoribine Related Classifications
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