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Submit ReviewGRL 0617
Description: Coronavirus PLpro inhibitor
Chemical Name: 5-Amino-2-methyl-N-[(1R)-1-(1-naphthalenyl)ethyl]benzamide
Purity: ≥98% (HPLC)
Biological Activity for GRL 0617
GRL 0617 is a coronavirus papain-like protease (Plpro) inhibitor (IC50 values are 0.6 and 0.8 μM for SARS-COV and SARS-CoV-2 PLpro, respectively). Inhibits deubiquitination activity of SARS-CoV PLpro. Displays no inhibition of human deubiquitinating enzymes. Improves cell viability following SARS-CoV infection. Inhibits SARS-CoV-2 viral replication and induces antiviral immune signaling pathways following SARS-CoV-2 infection in CaCo-2 cells.
Compound Libraries for GRL 0617
GRL 0617 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for GRL 0617
| M. Wt | 304.39 |
| Formula | C20H20N2O |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1093070-16-6 |
| PubChem ID | 24941262 |
| InChI Key | UVERBUNNCOKGNZ-CQSZACIVSA-N |
| Smiles | C[C@H](C1=CC=CC2=C1C=CC=C2)NC(C3=C(C=CC(N)=C3)C)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for GRL 0617
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 30.44 | 100 | |
| ethanol | 30.44 | 100 |
Preparing Stock Solutions for GRL 0617
The following data is based on the product molecular weight 304.39. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.29 mL | 16.43 mL | 32.85 mL |
| 5 mM | 0.66 mL | 3.29 mL | 6.57 mL |
| 10 mM | 0.33 mL | 1.64 mL | 3.29 mL |
| 50 mM | 0.07 mL | 0.33 mL | 0.66 mL |
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Product Datasheets for GRL 0617
References for GRL 0617
References are publications that support the biological activity of the product.
Ratia et al (2008) A noncovalent class of papain-like protease/deubiquitinase inhibitors blocks SARS virus replication. Proc.Natl.Acad.Sci.USA. 105 16119 PMID: 18852458
Freitas et al (2020) Characterization and noncovalent inhibition of the deubiquitinase and deISGylase activity of SARS-CoV-2 papain-Like protease. ACS Infect.Dis. 6 2099 PMID: 32428392
Shin et al (2020) Papain-like protease regulates SARS-CoV-2 viral spread and innate immunity. Nature 587 657 PMID: 32726803
If you know of a relevant reference for GRL 0617, please let us know.
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Citations for GRL 0617
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