GRL0617 is a potent, selective and competitive noncovalent inhibitor of SARS PLPro. GRL0617, inhibited SARS-CoV viral replication in Vero E6 cells with an EC(50) of 15 microM and had no associated cytotoxicity. The X-ray structure of PLpro in complex with GRL0617 indicates that the compound has a unique mode of inhibition whereby it binds within the S4-S3 subsites of the enzyme and induces a loop closure that shuts down catalysis at the active site.
CAS Number: 1093070-16-6
Molecular Weight: 304.39
Chemical Name: 5-Amino-2-methyl-N-[(1R)-1-(1-naphthalenyl)ethyl]benzamide
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
- Chaudhuri R, Tang S, Zhao G, Lu H, Case DA, Johnson ME. Comparison of SARS and NL63 papain-like protease binding sites and binding site dynamics: inhibitor design implications. J Mol Biol. 2011 Nov 25;414(2):272-88. doi: 10.1016/j.jmb.2011.09.030. Epub 2011 Sep 29. PubMed PMID: 22004941; PubMed Central PMCID: PMC3397151.
- Nathan J. SchauerRobert S. MaginXiaoxi LiuLaura M. DohertySara J. Buhrlage* Advances in Discovering Deubiquitinating Enzyme (DUB) Inhibitors. Journal of Medicinal Chemistry, Articles ASAP (Perspective). Publication Date (Web):November 4, 2019DOI: 10.1021/acs.jmedchem.9b01138.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.