PLpro inhibitor
Based on 5 publication(s) in Google Scholar
PLpro inhibitor is a potent inhibitor of papain-like protease (PLpro) with an IC50 of 2.6 µM. PLpro inhibitor inhibits SARS-CoV-2 PLpro with an IC50 of 5.0 µM and an EC50 of 21.0 µM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.88%
- No. CAS: 1093070-14-4
- Fòrmula: C22H22N2O2
- Peso molecular:346.42
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PLpro inhibitor
More
Actividad biológica
IC50 : 2.6 µM (Papain-like protease (PLpro))[1]; 5.0 µM (SARS-CoV-2 PLpro)[2]
EC50: 21.0 µM (SARS-CoV-2 PLpro)[2]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Vero | EC50 |
14.5 μM
Compound: 24
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Antiviral activity against SARS coronavirus in african green monkey Vero E6 cells assessed as inhibition of replication after 48 hrs
Antiviral activity against SARS coronavirus in african green monkey Vero E6 cells assessed as inhibition of replication after 48 hrs
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[PMID: 19645480] |
PLpro inhibitor is a potent inhibitor against the papain-like protease (PLpro) from the coronavirus that causes severe acute respiratory syndrome (SARS-CoV). PLpro inhibitor was found to have IC50 value of 2.6 μM. PLpro inhibitor display significant antiviral activity with EC50 values of 13.1 μM, without toxicity up to the highest concentration tested. Notably, the increasing antiviral potency correlates with the in vitro inhibition of PLpro, suggesting that the compounds work directly on the enzyme in cells[1][3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1093070-14-4
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Appearance Solid
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Peso molecular 346.42
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Fòrmula C22H22N2O2
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Color White to off-white
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SMILES
O=C(C1=CC(NC(C)=O)=CC=C1C)N[C@H](C)C2=C(C=CC=C3)C3=CC=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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 Rep
Hepatitis C virus drugs that inhibit SARS-CoV-2 papain-like protease synergize with remdesivir to suppress viral replication in cell culture. [Abstract]2021 May 18;35(7):109133. PMID: 33984267 -
Sci Rep
2021 Mar 8;11(1):5433. PMID: 33686143 -
ACS Infect Dis
Characterization and Noncovalent Inhibition of the Deubiquitinase and deISGylase Activity of SARS-CoV-2 Papain-Like Protease. [Abstract]2020 Aug 14;6(8):2099-2109. PMID: 32428392 -
Solvente y solubilidad
DMSO : 100 mg/mL (288.67 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, 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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 mg/mL (7.22 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
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.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Ratia, K., et al., A noncovalent class of papain-like protease/deubiquitinase inhibitors blocks SARS virus replication. Proc Natl Acad Sci U S A, 2008. 105(42): p. 16119-24. [Content Brief]
[2]. http://www.google.com/patents/WO2010022355A1cl=en
[3]. Brendan T Freitas, et al. Characterization and Noncovalent Inhibition of the Deubiquitinase and deISGylase Activity of SARS-CoV-2 Papain-Like Protease. ACS Infect Dis. 2020 May 19. [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 |
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| DMSO | 1 mM | 2.8867 mL | 14.4333 mL | 28.8667 mL | 72.1667 mL |
| 5 mM | 0.5773 mL | 2.8867 mL | 5.7733 mL | 14.4333 mL | |
| 10 mM | 0.2887 mL | 1.4433 mL | 2.8867 mL | 7.2167 mL | |
| 15 mM | 0.1924 mL | 0.9622 mL | 1.9244 mL | 4.8111 mL | |
| 20 mM | 0.1443 mL | 0.7217 mL | 1.4433 mL | 3.6083 mL | |
| 25 mM | 0.1155 mL | 0.5773 mL | 1.1547 mL | 2.8867 mL | |
| 30 mM | 0.0962 mL | 0.4811 mL | 0.9622 mL | 2.4056 mL | |
| 40 mM | 0.0722 mL | 0.3608 mL | 0.7217 mL | 1.8042 mL | |
| 50 mM | 0.0577 mL | 0.2887 mL | 0.5773 mL | 1.4433 mL | |
| 60 mM | 0.0481 mL | 0.2406 mL | 0.4811 mL | 1.2028 mL | |
| 80 mM | 0.0361 mL | 0.1804 mL | 0.3608 mL | 0.9021 mL | |
| 100 mM | 0.0289 mL | 0.1443 mL | 0.2887 mL | 0.7217 mL |
PLpro inhibitor Related Classifications
HY-17542 Related Classifications
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