TDI-015051

TDI-015051 (dose-response format) potently inhibits SARS-CoV-2 NSP14 guanine-N7 methyltransferase activity in a biochemical assay with an IC₅₀ ≤ 0.15 nM^[1].
TDI-015051 inhibits SARS-CoV-2 infection in Huh-7.5 cells with an EC₅₀ of 11.4 nM, and this activity is potentiated to an EC₅₀ of 0.8 nM by co-treatment with 5 μM DZNeP, with no cytotoxicity at concentrations ≤ 3 μM^[1].
TDI-015051 (0.1-16 nM; 4 days post-infection) completely inhibits SARS-CoV-2 replication in human primary small airway epithelial cells at concentrations ≥ 4 nM^[1].
TDI-015051 (dose-response format; 1 h pre-treatment; 24 h, 48 h, 72 h post-infection evaluation) inhibits SARS-CoV-2 infection in Vero E6 cells with EC₅₀ values of 99.5 nM, 71.1 nM, and 52.4 nM at 24 h, 48 h, and 72 h post-infection, respectively, following 1 h pre-treatment^[1].
TDI-015051 (dose-response format) inhibits infection by multiple human coronaviruses in cell-based assays, with EC₅₀ values of 0.12 μM for α-hCoV-NL63, 3.7 μM for α-hCoV-229E, and 6.5 μM for β-hCoV-MERS, with no detectable cytotoxicity at the tested concentrations^[1].
TDI-015051 (dose-response format) does not inhibit SARS-CoV-2 NSP16-NSP10, human RNMT-RAM, or Zika virus NS5 methyltransferases, demonstrating selective activity against coronavirus NSP14^[1].
TDI-015051 (1 μM; 1 h pre-treatment, 24 h infection) treatment of SARS-CoV-2-infected A549-ACE2-TMPRSS2 cells induces a weak type I interferon-mediated immune response via increased interferon-stimulated gene expression^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.