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.
For research use only. We do not sell to patients.
- CAS No.: 3132184-09-6
- Formula: C37H45FN6O5S
- Molecular Weight:704.85
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
SARS-CoV-1 PLpro 42.4 nM (IC50) |
SARS-CoV-2 PLpro 50.5 nM (IC50) |
In Vitro
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. Further protocols information, click here.
Chemical Information
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CAS No. 3132184-09-6
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Molecular Weight 704.85
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GL-637 Related Classifications
HY-187197 Related Classifications
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