#C1210N 3CLPro L50F + E166A + L167F Expression Kit
$395.00 – $795.00
Express 3CLpro with the L50F + E166A + L167F mutation in mammalian cells including HEK293, A549, and many more. Use alongside other 3CLpro mutant proteases and our 3CLglow biosensor assays to test 3CLpro inhibitor efficacy against a panel of mutations in the protease.
3CLpro (Mpro) L50F + E166A + L167F mutation Expression Kit
In biochemical analysis, nirmatrelvir’s IC50 value was found to be 72-fold greater in the presence of the L50F, E166A, L167F mutation (Jochmans et al. 2023). In a HEK293T cell-based 3CLpro fluorescent reporter assay nirmtrelvir EC50 increased from .96uM to 27uM with this mutation (Jochmans et al. 2023). These mutations occur independently in patients and have emerged collectively when passing the virus under nirmatrelvir selection (Jochmans et al. 2023; Shu and McCauley 2017). Furthermore, a FRET-based enzymatic assay demonstrated a 51.9-fold increase in IC50 values for nirmatrelvir in the presence of this mutation (Huang et al. 2023).
- Identify protease inhibitors that maintain efficacy against the L50F + E166A + L167F mutation
- Easy co-expression with our 3CLglow and 3CLglowUp sensors
- Cost effective screening with minimal safety requirements (BSL-1)
Materials in the Kit:
• 3CLpro L50F + E166A + L167F in BacMam
• Sodium Butyrate, 500 mM in H2O
References:
Huang, C., Shuai, H., Qiao, J., Hou, Y., Zeng, R., Xia, A., Xie, L., Fang, Z., Li, Y., Yoon, C., Huang, Q., Hu, B., You, J., Quan, B., Zhao, X., Guo, N., Zhang, S., Ma, R., Zhang, J., … Yang, S. (2023). A new generation mpro inhibitor with potent activity against SARS-COV-2 omicron variants. Signal Transduction and Targeted Therapy, 8(1). https://doi.org/10.1038/s41392-023-01392-w
Jochmans, D., Liu, C., Donckers, K., Stoycheva, A., Boland, S., Stevens, S. K., De Vita, C., Vanmechelen, B., Maes, P., Trüeb, B., Ebert, N., Thiel, V., De Jonghe, S., Vangeel, L., Bardiot, D., Jekle, A., Blatt, L. M., Beigelman, L., Symons, J. A., … Vandyck, K. (2023). The substitutions L50F, E166A, and L167F in SARS-COV-2 3clpro are selected by a protease inhibitor in vitro and confer resistance to Nirmatrelvir. mBio, 14(1). https://doi.org/10.1128/mbio.02815-22
Shu, Y., & McCauley, J. (2017). GISAID: Global initiative on sharing all influenza data – from vision to reality. Eurosurveillance, 22(13). https://doi.org/10.2807/1560-7917.es.2017.22.13.30494
Additional information
| Shipping | We strive for prompt delivery of each order, so we ship by FedEx 2-day service in lightweight, sturdy, and reusable/biodegradable packaging with an insulated cooler and moisture-resistant refrigerant gel packs. Shipping days are Mon-Wed so product does not sit in transit over the weekend. Web store ships to US & Canada only, contact sales for other locations. |
|---|---|
| Protocol for Use | https://montanamolecular.com/general-bacmam-transduction-protocol/ |
| MSDS | |
| Kit Volume | 5mL, 30mL |
| More Info | https://montanamolecular.com/detecting-inhibitors-of-mutant-3cl-proteases |
COVID-19 tools Publications
Pseudovirus and Host Factor Publications
- L. Monteonofrio. Molecular mechanisms of thalidomide effectiveness on COVID-19 patients explained: ACE2 is a new ΔNp63α target gene. Journal of Molecular Medicine. September 2024.
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- M. Farrag, et al. Structural requirements of Holothuria floridana fucosylated chondroitin sulfate oligosaccharides in anti-SARS-CoV-2 and anticoagulant activities. PLoS One. May 2023.
A. Maurya, et al. Structure, anti-SARS-CoV-2, and anticoagulant effects of two sulfated galactans from the red alga Botryocladia occidentalis. International Journal of Biological Macromolecules. March 2023. - X. Mei, et al. An inhaled bioadhesive hydrogel to shield non-human primates from SARS-CoV-2 infection. Nature Materials. February 2023.
- M. Spampinato, et al. Effects of Mangiferin on LPS-Induced Inflammation and SARS-CoV-2 Viral Adsorption in Human Lung Cells. Pharmaceutics. December 2022.
- S. Huang, et al. Long Chain N3-PUFA Decreases ACE2 Protein Levels and Prevents SARS-CoV-2 Cell Entry. International Journal of Molecular Sciences. November 2022.
- S. Shahbaz, et al. Differential effects of age, sex and dexamethasone therapy on ACE2/TMPRSS2 expression and susceptibility to SARS-CoV-2 infection. Frontiers in Immunology. November 2022.
- R. Dwivedi, et al. Anti-SARS-CoV-2 and anticoagulant properties of Pentacta Pygmaea fucosylated chondroitin sulfate depend on high molecular weight structures. Glycobiology. September 2022.
- A. Puhl, et al. Vandetanib Blocks the Cytokine Storm in SARS-CoV-2 Infected Mice. ACS Omega. August 2022.
- S.T. Chuang, P. Buchwald. Broad-Spectrum Small-Molecule Inhibitors of the SARS-CoV-2 Spike-ACE2 Protein-Protein Interaction from a Chemical Space of Privileged Protein Binders. Pharmaceuticals. August 2022.
- B.J. Travis, et al. Significance of chlorine-dioxide based oral rinses in preventing SARS-CoV-2 cell entry. Oral Diseases. July 2022.
- R. Dwivedi, et al. Inhibition of SARS-CoV-2 wild-type (Wuhan-Hu-1) and Delta (B.1.617.2) strains by marine sulfated glycans. Glycobiology. July 2022.
- Z. Wang, et al. Exosomes decorated with a recombinant SARS-CoV-2 receptor-binding domain as an inhalable COVID-19 vaccine. Nature Biomedical Engineering. July 2022.
- BR Jo, et al. A Novel Antiviral Protein Derived from Oenanthe javanica: Type I Interferon-Dependent Antiviral Signaling and Its Pharmacological Potential. biomolecules. June 2022.
- S. Chuang, et al. Methylene Blue Is a Non-Specific Protein-Protein Interaction Inhibitor with Potential for Repurposing as Antiviral for COVID-19. Pharmaceuticals. May 2022.
- L. Souza-Moreira, et al. Poly(I:C) Enhances Mesenchymal Stem Cell Control of Myeloid Cells from COVID-19 Patients. iScience. April 2022.
- A. Puhl, et al. Vandetanib Reduces Inflammatory Cytokines and Ameliorates COVID-19 in Infected Mice. bioRxiv. December 2021.
- R. Dwivedi, et al. Structural and kinetic analyses of holothurian sulfated glycans suggest potential treatment for SARS-CoV-2 infection. Journal of Biological Chemistry. September 2021.
- Q. Zhang, et al. ACE2 interaction with cytoplasmic PDZ protein enhances SARS-CoV-2 invasion. iScience. July 2021.
- D. Bojadzic, et al. Small-Molecule Inhibitors of the Coronavirus Spike: ACE2 Protein-Protein Interaction as Blockers of Viral Attachment and Entry for SARS-CoV-2. ACS Infectious Diseases. May 2021.
- A. Riad, et al. Differential gene expression by RNA-Seq in Sigma-2 Receptor/TMEM97 knockout cells reveals its role in complement activation and SARS-CoV-2 viral uptake. bioRxiv. March 2021.
- D. Bojadzic, et al. Methylene Blue Inhibits the SARS-CoV-2 Spike-ACE2 Protein-Protein Interaction-a Mechanism that can Contribute to its Antiviral Activity Against COVID-19. Frontiers in Pharmacology. January 2021.
- Pramanik, et al. The rapid diagnosis and effective inhibition of coronavirus using spike antibody attached gold nanoparticles. Nanoscale Advances. January 2021.
3CLglow Publications
- J. Pérez-Vargas, et al. A novel class of broad-spectrum active-site-directed 3C-like protease inhibitors with nanomolar antiviral activity against highly immune-evasive SARS-CoV-2 Omicron subvariants. Emerging Microbes & Infections. August 2023.
- A. Citarella, et al. SARS-CoV-2 Mpro: A Potential Target for Peptidomimetics and Small-Molecule Inhibitors. biomolecules. September 2021.
