所有图片(1)
别名:
5-Amino-2-methyl-N-[(1R)-1-(1-naphthalenyl)ethyl]benzamide, GRL 0617, GRL0617
经验公式（希尔记法）:
C20H20N2O
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质量水平
检测方案
≥98% (HPLC)
形式
powder
旋光性
[α]/D -72.0 to -82.0°, c = 0.5 in chloroform-d
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
InChI
1S/C20H20N2O/c1-14-9-10-17(21)13-19(14)20(23)22-12-11-16-7-4-6-15-5-2-3-8-18(15)16/h2-10,13H,11-12,21H2,1H3,(H,22,23)
InChI key
SVHZQKLXYGYSMU-UHFFFAOYSA-N
生化/生理作用
GRL-0617 is a cell penetrant non-cytotoxic and potent inhibitor of the SARS-CoV -2 papain-like protease (SCoV2-PLpro) and SCoV-PLpro. GRL-0617 reversibly binds to SCoV2-PLpro and disrupts its interaction with Interferon-stimulated gene 15 (ISG15). GRL-0617 poorly affects (> 100 μM) the activities of MERS PLpro, a series of cysteine proteases, including the human deubiquitinating enzymes HAUSP, USP18, UCH-L1, UCH-L3, and a papain-like protease (PLP2) from the human coronavirus NL63. GRL-0617 suppress SARS-CoV-2 infection and promote anti-viral immunity.
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
A noncovalent class of papain-like protease/deubiquitinase inhibitors blocks SARS virus replication.
Kiira Ratia et al.
Proceedings of the National Academy of Sciences of the United States of America, 105(42), 16119-16124 (2008-10-15)
We report the discovery and optimization of a potent inhibitor against the papain-like protease (PLpro) from the coronavirus that causes severe acute respiratory syndrome (SARS-CoV). This unique protease is not only responsible for processing the viral polyprotein into its functional
Donghyuk Shin et al.
Nature, 587(7835), 657-662 (2020-07-30)
The papain-like protease PLpro is an essential coronavirus enzyme that is required for processing viral polyproteins to generate a functional replicase complex and enable viral spread1,2. PLpro is also implicated in cleaving proteinaceous post-translational modifications on host proteins as an
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