PLpro inhibitor Chemical Properties

Boiling point:

584.7±50.0 °C(Predicted)

Density 

1.189±0.06 g/cm3(Predicted)

storage temp. 

Sealed in dry,Room Temperature

solubility 

DMF: 30 mg/ml; DMSO: 30 mg/ml

form 

Powder

pka

14.13±0.46(Predicted)

color 

White to off-white

PLpro inhibitor Usage And Synthesis

Uses

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].

Definition

ChEBI: KOM70144 is a benzamide that is GRL-0617 in which one of the hydrogen's of the primary amino group is replaced by an acetyl group. It an inhibitor of SARS-CoV and SARS-CoV-2 papain-like protease (PLpro) with an IC50 of 2.6 muM and 5.0 muM, respectively. It also inhibits SARS-CoV and SARS-CoV-2 infection of Vero E6 cells in vitro (EC50 values are 13.1 and 21 muM, respectively). It has a role as a protease inhibitor and an anticoronaviral agent. It is a member of naphthalenes, a member of benzamides, a secondary carboxamide and a member of acetamides. It is functionally related to a GRL-0617.

storage

Store at -20°C

References

[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. DOI:10.1073/pnas.0805240105
[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. DOI:10.1021/acsinfecdis.0c00168