Extended Data Fig. 3: Structurally-related PAIRs and KIRAs.
From: ATP-competitive partial antagonists of the IRE1α RNase segregate outputs of the UPR
(a) Chemical structure of (left) and inhibition of IRE1α*’s kinase activity (right, Ki = 140 nM) by compound 6. (b) Chemical structure of (left) and inhibition of IRE1α*’s kinase activity (right, Ki = 98 nM) by compound 7. (c) Chemical structure of (left) and inhibition of IRE1α*’s kinase activity (right, Ki = 220 nM) by compound 8 (PAIR1). (d) Chemical structure of (left) and inhibition of IRE1α*’s kinase activity (right, Ki = 160 nM) by compound 9 (KIRA9). Inhibition of IRE1α*’s RNase activity by (e) compounds 4 and 5, and (f) PAIR1 and KIRA9. All data points shown are the mean of n = 3 independent experiments ± SEM.
