MKC8866 (IRE1-IN-8866), a salicylaldehyde analog, is a specific IRE1α RNase inhibitor with IC50 of 0.29?μM for human IRE1α in vitro.
MKC8866 is optimized and refined from a family of IRE1α-specific endoribonuclease inhibitors obtained from a chemical library screen. MKC8866 effectively represses IRE1α-mediated XBP1 splicing in PCa cells and has favorable pharmacokinetic and pharmacodynamic properties.[1]
MKC8866 is an IRE1α RNase-specific inhibitor molecule that displays significant therapeutic activity in various preclinical models of PCa in vivo. MKC8866 synergizes with clinical PCa drugs in vivo.[1]
[1] Sheng X, et al. Nat Commun. 2019 Jan 24;10(1):323.