rdrp inhibitor nitd008 Search Results


rdrp inhibitor nitd008  (Tocris)
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Tocris rdrp inhibitor nitd008
a Chemical structure of IRBM-Z-2 along with biological data and in vitro and in vivo ADME profiles. Two-dimensional (2D) interaction patterns of IRBM-Z-2 and NS2B-NS3 protease depicted by dashed lines. b Representative BLI (biolayer interferometry) sensorgrams (blue curves) with 1:1 fitting (red curves) of the IRBM-Z-2 and ZIKV NS2B-NS3 protease interaction. Binding parameters represent the mean ± SD of six independent experiments. c Close-up view of the allosteric binding mode of IRBM-Z-2 (cyan sticks) co-crystallized in complex with the ZIKV NS2B-NS3 protease (PDB ID 9IBY). The ligand is depicted in cyan sticks; the H-bonds are depicted as dashed yellow lines and the π-stacking interactions as dashed purple lines. The second monomer is depicted as transparent sticks and cartoons. Electron density difference map 2F O -F C , at +1σ carved at 1.5 Å from the ligand is shown as grey isomesh. d Dose–response curves and IC 50 and EC₅₀ values of IRBM-Z-1 in the NS2B-NS3 protease enzymatic assay (red curve) and ZIKV replicon assay (blue curve), and Vero cell proliferation assay (black curve). All data represent the mean ± SD from at least three independent experiments . e Dose-response curves showing antiviral activity and cytotoxicity of IRBM-Z-2 and Ribavirin against ZIKV (PRVABC59 strain) infected BHK-21 cells. Antiviral activity is measured as a % reduction of cytopathic effect (CPE); cytotoxicity was assessed in parallel. f Dose-response curves showing antiviral activity and cytotoxicity of IRBM-Z-2 and <t>NITD008</t> against WNV infected Vero cells. The analysis is presented as % luminescence signal (indicative of viral replication). Cytotoxicity was evaluated using the XTT assay. All graphs represent the mean ± SD. from three biological replicates ( n = 3).
Rdrp Inhibitor Nitd008, supplied by Tocris, used in various techniques. Bioz Stars score: 94/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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rdrp inhibitor nitd008 - by Bioz Stars, 2026-07
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a Chemical structure of IRBM-Z-2 along with biological data and in vitro and in vivo ADME profiles. Two-dimensional (2D) interaction patterns of IRBM-Z-2 and NS2B-NS3 protease depicted by dashed lines. b Representative BLI (biolayer interferometry) sensorgrams (blue curves) with 1:1 fitting (red curves) of the IRBM-Z-2 and ZIKV NS2B-NS3 protease interaction. Binding parameters represent the mean ± SD of six independent experiments. c Close-up view of the allosteric binding mode of IRBM-Z-2 (cyan sticks) co-crystallized in complex with the ZIKV NS2B-NS3 protease (PDB ID 9IBY). The ligand is depicted in cyan sticks; the H-bonds are depicted as dashed yellow lines and the π-stacking interactions as dashed purple lines. The second monomer is depicted as transparent sticks and cartoons. Electron density difference map 2F O -F C , at +1σ carved at 1.5 Å from the ligand is shown as grey isomesh. d Dose–response curves and IC 50 and EC₅₀ values of IRBM-Z-1 in the NS2B-NS3 protease enzymatic assay (red curve) and ZIKV replicon assay (blue curve), and Vero cell proliferation assay (black curve). All data represent the mean ± SD from at least three independent experiments . e Dose-response curves showing antiviral activity and cytotoxicity of IRBM-Z-2 and Ribavirin against ZIKV (PRVABC59 strain) infected BHK-21 cells. Antiviral activity is measured as a % reduction of cytopathic effect (CPE); cytotoxicity was assessed in parallel. f Dose-response curves showing antiviral activity and cytotoxicity of IRBM-Z-2 and NITD008 against WNV infected Vero cells. The analysis is presented as % luminescence signal (indicative of viral replication). Cytotoxicity was evaluated using the XTT assay. All graphs represent the mean ± SD. from three biological replicates ( n = 3).

Journal: Nature Communications

Article Title: An allosteric inhibitor of the Zika virus NS2B-NS3 protease with oral efficacy in mouse models

doi: 10.1038/s41467-026-68943-x

Figure Lengend Snippet: a Chemical structure of IRBM-Z-2 along with biological data and in vitro and in vivo ADME profiles. Two-dimensional (2D) interaction patterns of IRBM-Z-2 and NS2B-NS3 protease depicted by dashed lines. b Representative BLI (biolayer interferometry) sensorgrams (blue curves) with 1:1 fitting (red curves) of the IRBM-Z-2 and ZIKV NS2B-NS3 protease interaction. Binding parameters represent the mean ± SD of six independent experiments. c Close-up view of the allosteric binding mode of IRBM-Z-2 (cyan sticks) co-crystallized in complex with the ZIKV NS2B-NS3 protease (PDB ID 9IBY). The ligand is depicted in cyan sticks; the H-bonds are depicted as dashed yellow lines and the π-stacking interactions as dashed purple lines. The second monomer is depicted as transparent sticks and cartoons. Electron density difference map 2F O -F C , at +1σ carved at 1.5 Å from the ligand is shown as grey isomesh. d Dose–response curves and IC 50 and EC₅₀ values of IRBM-Z-1 in the NS2B-NS3 protease enzymatic assay (red curve) and ZIKV replicon assay (blue curve), and Vero cell proliferation assay (black curve). All data represent the mean ± SD from at least three independent experiments . e Dose-response curves showing antiviral activity and cytotoxicity of IRBM-Z-2 and Ribavirin against ZIKV (PRVABC59 strain) infected BHK-21 cells. Antiviral activity is measured as a % reduction of cytopathic effect (CPE); cytotoxicity was assessed in parallel. f Dose-response curves showing antiviral activity and cytotoxicity of IRBM-Z-2 and NITD008 against WNV infected Vero cells. The analysis is presented as % luminescence signal (indicative of viral replication). Cytotoxicity was evaluated using the XTT assay. All graphs represent the mean ± SD. from three biological replicates ( n = 3).

Article Snippet: RdRp inhibitor NITD008 was purchased from Tocris Biosciences (Cat. #6045), and mycophenolic acid from Sigma-Aldrich (Cat. #M5255).

Techniques: In Vitro, In Vivo, Binding Assay, Enzymatic Assay, Proliferation Assay, Activity Assay, Infection, XTT Assay