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Dabcyl-KTSAVLQSGFRKM-Glu(Edans)-amide
Chemical name: Dabcyl-lysyl-threonyl-seryl-alanyl-valyl-leucyl-glutaminyl-seryl-glycyl-phenylalanyl-arginyl-lysyl-methionyl-glutamyl(Edans)-amide // Synonyms: Dabcyl-Lys-Thr-Ser-Ala-Val-Leu-Gln-Ser-Gly-Phe-Arg-Lys-Met-Glu(Edans); substrate of SARS-CoV-2 main protease Mpro
- Product code:LS-4180
- CAS No.:2642630-08-6
- Formula:C95H142N26O23S2
- Storage temperature:-20°C
- Molecular weight:2080.46 g/mol
- Purity :min. 95%
from €850.00
description
SARS-CoV-2 main protease Mpro (3CLpro) represents a major target in drug development against COVID-19. This compound can be used as fluorogenic FRET substrate for activity determination and inhibitor screening of Mpro protease.
The corresponding enzymatic assay was developed by the Hilgenfeld group. Before enzymatic cleavage, Edans fluorescence is quenched by Dabcyl. Upon cleavage, no more quenching occurs. Convenient read out of the fluorescent cleavage product: excitation at 340 nm leads to light emission at 490 nm.
Please also see our rhodamine-based Mpro substrate LS-4190.
Do not dissolve in DMSO, as this might cause oxidation of the methionine.
references
Á-Ketoamides as Broad-Spectrum Inhibitors of Coronavirus and Enterovirus Replication: Structure-Based Design, Synthesis, and Activity Assessment; L. Zhang, D. Lin, Y. Kusov, Y. Nian, Q. Ma, J. Wang, A. von Brunn, P. Leyssen, K. Lanko, J. Neyts, A. de Wilde, E. J. Snijder, H. Liu, and R. Hilgenfeld; J. Med. Chem. 2020; 63: 4562-4578; https://doi.org/10.1021/acs.jmedchem.9b01828
A structural view of the inactivation of the SARS coronavirus main proteinase by benzotriazole esters; K. H. G. Verschueren, K. Pumpor, S. Anemüller, S. Chen, J. R. Mesters, R. Hilgenfeld; Chem. Biol. 2008; 15: 597-606; https://doi.org/10.1016/j.chembiol.2008.04.011
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