R523062 is a potent small-molecule antiviral targeting enterovirus D68 (EV-D68), discovered via a CPE-based high-throughput screen at 15 µM in RD cells where it afforded ~92% protection. It exhibits low‑micromolar EC₅₀ values against multiple contemporaneous EV-D68 strains and notably reduced activity against EV-A71. Mechanistic studies—including serial viral passages, time-of-addition assays, protease activity tests, plaque assays with recombinant viruses, and thermal-shift binding—consistently identify the viral 2C ATPase/helicase protein as the direct target: R523062 binds to wild-type 2C (and Q322R mutant) but not to the I227L or I227L/Q322R mutants, with the I227L mutation alone conferring resistance. It also shows additive antiviral effects when combined with a 2A protease inhibitor (telaprevir) and with a VP1 capsid inhibitor (R856932). In summary, R523062 is a validated, direct-acting EV‑D68 2C inhibitor with confirmed in vitro potency, resistance mapping, and combination synergy.
MedKoo Cat#: 535252
Name: R523062
CAS#: 314768-41-7
Chemical Formula: C17H14N2OS
Exact Mass: 294.0827
Molecular Weight: 294.37
Elemental Analysis: C, 69.36; H, 4.79; N, 9.52; O, 5.43; S, 10.89
The following data is based on the product molecular weight 294.37 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |