Thermal shift concentration-response curves using <i>Sj</i>GST in the absence and presence of 2 mM GSH for A) quercetin, B) myricetin and C) tannic acid.

<p>Thermal shifts represent the differences in T_m between vehicle control and compound-containing samples, respectively.</p

Thermal shift concentration response curves using <i>Sj</i>GST in the absence and presence of GSH for the conjugate-formers NBD-OH (A) and ethacrynic acid (EA, panel B).

<p>Thermal shifts represent the differences in T_m between vehicle control and compound-containing samples, respectively.</p

GST inhibitors tested in this study and their inhibitory activity against <i>Sj</i>GST.

<p>GST inhibitors tested in this study and their inhibitory activity against <i>Sj</i>GST.</p

Thermal shift concentration-response curves using hGSTA1-1 in the absence and presence of 2 mM GSH for A) S-octyl GSH, B) ethacrynic acid (EA), C) quercetin, and using hGSTM1-1 for D) S-octyl GSH, E) EA, and F) quercetin.

<p>Thermal shifts represent the differences in T_m between vehicle control and compound-containing samples, respectively.</p

Thermal denaturation curves for <i>Sj</i>GST alone or with 100 µM S-alkyl GSH in the absence (A) and presence (B) of 2 mM GSH; (C) correlation between thermal shift at 100 µM alkyl-GSH and degree of inhibition against <i>Sj</i>GST.

<p>Thermal shifts, where applicable, represent the differences in T_m between vehicle control and compound-containing samples, respectively.</p

Schematic illustration of different inhibition mechanisms and the associated DSF signatures: A) GSH-competitive inhibition; B) conjugate-formation; C) ligandin-type.

<p>Schematic illustration of different inhibition mechanisms and the associated DSF signatures: A) GSH-competitive inhibition; B) conjugate-formation; C) ligandin-type.</p

Thermal shift concentration-response curves for S-alkyl GSH using <i>Sj</i>GST: A) S-methyl GSH, B) S-butyl GSH, C) S-hexyl GSH, D) S-octyl GSH.

<p>Thermal shifts represent the differences in T_m between vehicle control and compound-containing samples, respectively.</p

Top LOPAC¹²⁸⁰ Hits.

1<p>Top compound concentrations of 144 or 151 µM for the AGP and HSA assays, respectively.</p

LOPAC¹²⁸⁰ Screen.

<p>The robust AGP (•) and HSA (o) screen performance as represented by the reproducible high Z’-factor trend.</p

HSA Assay Protocol for 1,536-well Format.

<p>HSA Assay Protocol for 1,536-well Format.</p