Coronavirus papain-like protease (Plpro) inhibitor (IC50values 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 ce
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Product Description
Product description
GRL0617 is a selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLpro), with an IC50 of 0.6 μM and a Ki value of 0.49 μM. GRL0617 also inhibits SARS-CoV with an EC50 of 14.5 μM. GRL0617 can be used for the research of severe acute respiratory syndrome.
1.Ratia K, Pegan S, Takayama J, Sleeman K, Coughlin M, Baliji S, Chaudhuri R, Fu W, Prabhakar BS, Johnson ME et al.. (2008) A noncovalent class of papain-like protease/deubiquitinase inhibitors blocks SARS virus replication.. Proc Natl Acad Sci USA, 105 (42):(16119-24). [PMID:18852458][10.1021/op500134e]
2.Ghosh AK, Takayama J, Aubin Y, Ratia K, Chaudhuri R, Baez Y, Sleeman K, Coughlin M, Nichols DB, Mulhearn DC et al.. (2009) Structure-based design, synthesis, and biological evaluation of a series of novel and reversible inhibitors for the severe acute respiratory syndrome-coronavirus papain-like protease.. J Med Chem, 52 (16):(5228-40). [PMID:19645480][10.1021/op500134e]
3.Freitas BT, Durie IA, Murray J, Longo JE, Miller HC, Crich D, Hogan RJ, Tripp RA, Pegan SD. (2020) Characterization and Noncovalent Inhibition of the Deubiquitinase and deISGylase Activity of SARS-CoV-2 Papain-Like Protease.. ACS Infect Dis, 6 (8):(2099-2109). [PMID:32428392][10.1021/op500134e]
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D23061593