Boceprevir
Antiviral, SARS-CoV-2 Mpro inhibitor / Boceprevir (394730-60-0) directly inhibits Hepatitis C virus (HCV) NS3 protease (overall binding constant for formation of covalent adduct, Ki* = 14 nM; initial inhibition constant Ki = 7.8 µM). This blocks NS3 autoactivation, and subsequent cleavage and maturation of other viral proteins necessary for replisome assembly. This reversible, slow-binding ketoamide also restores host interferon signaling obstructed by HCV, thus reactivating the immune response1. Recently, it was also found to inhibit the key SARS-CoV-2 protease, Mpro (3CLpro) in vitro (Ki = 1.18 µM) and in cells (EC50 = 1.9 µM, virus-induced cytopathic effects (CPE)
Biochemicals & reagents
394730-60-0
SCH 503034
1) Malcom et al. (2006), SCH 503034, a Mechanism-Based Inhibitor of Hepatitis C Virus NS3 Protease, Suppresses Polyprotein Maturation and Enhances the Antiviral Activity of Alpha Interferon in Replicon Cells; Antimicrob. Agents Chemother., 50 1013 2) Ma et al. (2020), Boceprevir, GC-376, and Calpain Inhibitors II, XII Inhibit SARS-CoV-2 Viral Replication by Targeting the Viral Main Protease; bioRxiv, Preprint May 8, DOI 1101/2020.04.20.051581
-20°C
TARGET: Protease; Cytochrome/MDR -- RESEARCH AREA: Immunology -- DISEASE AREA: Infectious disease