GL-637
GL-637 is a covalent and selective inhibitor of SARS-CoV-1/2 papain-like protease (PLpro), with IC50 values of 42.4 nM and 50.5 nM against the two viruses, respectively. GL-637 covalently modifies the catalytic Cys111 of PLpro, binds to Glu167 and occupies the BL2 groove, thereby inhibiting the deubiquitinase and deISGylase activities of PLpro. GL-637 can be used in the research of coronaviruses.
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- CAS. Nr.: 3132184-09-6
- Formel: C37H45FN6O5S
- Molecular Weight:704.85
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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SARS-CoV-1 PLpro 42.4 nM (IC50) |
SARS-CoV-2 PLpro 50.5 nM (IC50) |
GL-637 (treated for 30 min) potently inhibits purified SARS-CoV-1 PLpro, with an IC50 value of 42.4 nM[1].
GL-637 (incubated for 30 min) potently inhibits purified SARS-CoV-2 PLpro, with an IC50 of 50.5 nM[1].
GL-637 is a time-dependent covalent inhibitor of purified SARS-CoV-2 PLpro, with a kinact/KI value of 18,317 M-1 s-1[1].
GL-637 inhibits SARS-CoV-2 PLpro-mediated hydrolysis of Ub-AMC and ISG15-AMC, with IC50 values of 318.4 nM and 438.4 nM, respectively[1].
GL-637 (1-30 μM) shows selectivity for SARS-CoV-1 and SARS-CoV-2 PLpro. It exerts no effect on MERS-CoV PLpro at a concentration of 1 μM, and has no impact on human deubiquitinases USP7 and USP14 even at the highest tested concentration of 30 μM[1].
GL-637 potently inhibits the replication of SARS-CoV-2 in A549-ACE2 cells, with an EC50 of 0.313 μM; this compound shows no detectable cytotoxicity (CC50 > 10 μM), and has a therapeutic index of 31.94[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 3132184-09-6
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Molecular Weight 704.85
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Formel C37H45FN6O5S
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SMILES
O=C(OC)/C=C/C(NNC(CCC1=CC=C(N2CCN(C)CC2)C=C1C(N[C@@H](C3=CC=CC(C4=CC=C(CN5C[C@@H](F)CC5)S4)=C3)C)=O)=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
GL-637 Related Classifications
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