| Bioactivity | GSK5852 (GSK2485852) is an HCV NS5B polymerase inhibitor, with an IC50 value of 50 nM. GSK5852 displays antiviral activity and inhibits HCV with EC50s of 3.0 nM (genotype 1a, GT1a) and 1.7 nM (GT1b), respectively[1][2][3]. |
| Target | Target: 50 nM (NS5B, HCV) |
| Invitro | Nonstructural protein 5B (NS5B) RNA-dependent RNA polymerase (RdRp) is a component of HCV, for researching HCV infection-related diseases[1].GSK5852 (compound 87) inhibits aggregation by two mechanisms: 1) stabilizing β-flap in a closed inactive state to inhibit the initiation step of the RdRp RNA replication cycle; 2) disruption of RNA processing channels through direct spatial contact[1].GSK5852 is a non-nucleoside NS5B inhibitor and exhibits inhibitory effect on HCV mutant variants with EC50s of 3.2 nM (GT1a C316Y), 1.9 nM (GT1b C316N), respectively[1].GSK5852 displays an excellent resistance profile and shows a 40 hours[3].GSK5852 (0.6, 10 μM; 15 min) inhibits NS5B∆21 1b 316N with an IC50 value of 130 nM[3]. Western Blot Analysis[3] Cell Line: |
| Name | GSK5852 |
| CAS | 1331942-30-3 |
| Formula | C27H25BF2N2O6S |
| Molar Mass | 554.37 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Zhou Z, et al. Small molecule NS5B RdRp non-nucleoside inhibitors for the treatment of HCV infection: A medicinal chemistry perspective. Eur J Med Chem. 2022 Jul 8. 240:114595. [2]. Voitenleitner C, et al. In vitro characterization of GSK2485852, a novel hepatitis C virus polymerase inhibitor. Antimicrob Agents Chemother. 2013 Nov;57(11):5216-24. [3]. Maynard A, et al. Discovery of a potent boronic acid derived inhibitor of the HCV RNA-dependent RNA polymerase. J Med Chem. 2014 Mar 13;57(5):1902-13. |