Extended Data Fig. 10: Activity of H-151 against mmSTING.
From: Targeting STING with covalent small-molecule inhibitors
a, HEK293T cells were transfected with plasmids encoding mmSTING in combination with cdG-Syn or were transfected with a plasmid for TBK1, and an IFNβ luciferase reporter, and then treated with H-151 (concentration 0.02–2 μM). Reporter activity was measured after overnight incubation. Data are mean ± s.e.m. (n = 3; nonlinear regression analysis). Experiments were performed together with those that generated the data displayed in Fig. 5b. b, BMDMs were pretreated with H-151 (0.5 μM) and levels of Ifnb1 mRNA expression induced by cGAMP were assessed by RT–qPCR. Data are mean ± s.e.m. (n = 3); P value was calculated by two-tailed t-test. c, Mean plasma concentration profiles of H-151 following a single-dose intraperitoneal injection into wild-type mice (n = 3 mice per time point). d, Schematic, and in vivo detection of H-176-AL binding to mmSTING. Visualization by in-gel fluorescence was performed using SiR azide. One representative of n = 2. For gel source data, see Supplementary Fig. 1. For source data, see Supplementary Table 1.
