Extended Data Fig. 4: Gel-based analysis of compound interactions using clickable probes.
From: Targeting STING with covalent small-molecule inhibitors
a, Structures of C-176-AL and C-176-AZ. b, HEK293T cells transfected with Flag–mmSTING and an IFNβ luciferase reporter were treated with C-176-AL, and luciferase activity was then assessed. Data are mean of n = 2. c, Labelling events of wild-type HEK293T cells and HEK293T with Flag–mmSTING incubated with C-176-AL (0.25 μM). d, Distinct labelling of mmSTING and hsSTING by C-176-AL (0.25 μM). e, Concentration-dependent competitor blockage of C-176-AL (0.25 μM) against C-178 and C-176-09 in HEK293T cells that express Flag–mmSTING. f, Labelling events of HEK293T cells that express Flag–mmSTING (wild-type mmSTING or mmSTING(C91S)) when exposed to iodoacetamide azide or C-176-AZ (both at 0.25 μM). g, HEK293T cells expressing Flag–mmSTING, GSTO1–Flag, MAP27K–Flag, MGMT–Flag or GSTP1–Flag were treated with C-176-AZ (0.25 μM). For in-gel fluorescence imaging, TAMRA azide (c–e) or SiR alkyne (f, g) was used. Immunoblots against Flag or β-actin are shown and data are representative of n = 3 independent experiments (c–g). h, Proposed reaction mechanism. For gel source data, see Supplementary Fig. 1.
