mkc-8866

Description: MKC-8866 (ORIN-1001; IRE1-IN-8866) is a salicylaldehyde analog that acts ass a potent, selective IRE1 RNase inhibitor with an IC50of 0.29?uM in human vitro. MKC8866 strongly inhibitsDithiothreitol-induced X-box-binding protein 1-spliced (XBP1s)expression with an EC50 of 0.52?uM and unstresses RPMI 8226 cells with an IC50of 0.14?uM. MKC8866 inhibits IRE1 RNase in breast cancer cells leadingto the decreased production of pro-tumorigenic factors and it caninhibits prostate cancer (PCa) tumor growth.

References: Wilhelm T, Bick F, Peters K, Mohta V, Tirosh B, Patterson JB, Kharabi-MasoulehB, Huber M. Infliction of proteotoxic stresses by impairment of the unfoldedprotein response or proteasomal inhibition as a therapeutic strategy for mastcell leukemia. Oncotarget. 2017 Dec 17; 9(3):2984-3000.