PeptideDB

PLpro inhibitor

CAS: 1093070-14-4 F: C22H22N2O2 W: 346.42

PLpro inhibitor is a potent inhibitor of papain-like protease (PLpro) with an IC50 of 2.6 µM. PLpro inhibitor inhibits
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Bioactivity PLpro inhibitor is a potent inhibitor of papain-like protease (PLpro) with an IC50 of 2.6 µM[1]. PLpro inhibitor inhibits SARS-CoV-2 PLpro with an IC50 of 5.0 µM and an EC50 of 21.0 µM[2].
Target IC50 : 2.6 µM (Papain-like protease (PLpro)); 5.0 µM (SARS-CoV-2 PLpro)EC50: 21.0 µM (SARS-CoV-2 PLpro)
Invitro 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].
Name PLpro inhibitor
CAS 1093070-14-4
Formula C22H22N2O2
Molar Mass 346.42
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Reference [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. [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.