1093070-16-6

GRL-0617 (1093070-16-6) is a potent (IC50?= 600 nM) noncovalent inhibitor of severe acute respiratory syndrome-coronavirus papain-like protease (SARS-CoV PLpro). GRL-0617 inhibited SARS-CoV viral replication in Vero E6 cells with no cytotoxicity (EC50?= 15 μM).??Inactive against human DUB-like proteases HAUSP, USP18, UCH-L1, UCH-L3, and PLP2

Appearance: Solid, beige. Boiling point: 514.9 ± 50.0°C (predicted). Density: 1.168 ± 0.06 g/cm?? (predicted). Solubility: Soluble in DMSO (>30 mg/mL) and ethanol (15 mg/mL). Optical rotation: [α]/D -72.0 to -82.0°, c = 0.5 in chloroform-d.

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].

ChEBI: GRL-0617 is a benzamide resulting from the formal condensation of the carboxy group of 5-amino-2-methylbenzoic acid with the amino group of (1R)-1-(naphthalen-1-yl)ethan-1-amine. It is a potent noncovalent inhibitor (IC50 = 600 nM) of severe acute respiratory syndrome-coronavirus papain-like protease (SARS-CoV PLpro). It has a role as an anticoronaviral agent and a protease inhibitor. It is a member of naphthalenes, a substituted aniline, a member of benzamides and a secondary carboxamide.

Store at -20°C

1)????Ratia?et al. (2008),?A noncovalent class of papain-like protease/deubiquitinase inhibitors blocks SARS virus replication;?Proc. Natl. Acad. Sci. USA,?105?16119