#C1205N 3CLPro H172Y Expression Kit
Express 3CLpro with the H172Y 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) H172Y mutation Expression Kit
H172Y substitution results in reduced stability, and enzyme activity, with the IC50 of nirmatrelvir against the H172Y mutant being 24-fold greater, as measured by an enzymatic assay (de Oliveira et al. 2022). Huang et al. reported a 30.7-fold increase in the IC50 of nirmatrelvir using a FRET-based enzymatic assay (Huang et al. 2023). Additionally, the Ki increased by 146-fold, as measured by an enzymatic assay (Hu et al. 2023). In a biochemical assay using recombinant SARS-CoV-2 3CLpro containing amino acid substitution H172Y, Pfizer had reported a 250-fold increase in Ki (Pfizer Laboratories 2022).
- Identify protease inhibitors that maintain efficacy against the H172Y mutation
- Easy co-expression with our 3CLglow and 3CLglowUp sensors
- Cost effective screening with minimal safety requirements (BSL-1)
Materials in the Kit:
• 3CLpro H172Y in BacMam
• Sodium Butyrate, 500 mM in H2O
References:
de Oliveira, V., Ibrahim, M., Sun, X., Hilgenfeld, R., & Shen, J. (2022). H172Y Mutation Perturbs the S1 Pocket and Nirmatrelvir Binding of SARS-COV-2 Main Protease through a Nonnative Hydrogen Bond. https://doi.org/10.21203/rs.3.rs-1915291/v1
Hu, Y., Lewandowski, E. M., Tan, H., Zhang, X., Morgan, R. T., Zhang, X., Jacobs, L. M., Butler, S. G., Gongora, M. V., Choy, J., Deng, X., Chen, Y., & Wang, J. (2023). Naturally occurring mutations of SARS-COV-2 main protease confer drug resistance to Nirmatrelvir. ACS Central Science, 9(8), 1658–1669. https://doi.org/10.1021/acscentsci.3c00538
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
Pfizer Laboratories. (2022). (rep.). FACT SHEET FOR HEALTHCARE PROVIDERS: EMERGENCY USE AUTHORIZATION FOR PAXLOVID. Retrieved from https://labeling.pfizer.com/ShowLabeling.aspx?id=16474.
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 |
