MKC8866

MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC₅₀ of 0.29 μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC₅₀ of 0.52 μM and unstresses RPMI 8226 cells with an IC₅₀ of 0.14 μM^[1]. MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth^[2]. IC50 & Target:IC50: 0.29 μM (IRE1 RNase)^[1] In Vitro: MKC8866 (20 μM; 6 days) decreases proliferation of all breast cancer cell lines^[2].
MKC8866 (20 μM; 48 hours) reduces the number of cells entering S phase^[2].
MKC8866 (0.2-10 μM; 3 days) suppresses the viability of all four cell lines in a dose-dependent manner under normal conditions, with the most robust effect in LNCaP cells^[1].
MKC8866 (20 μM; 72 hours) is sufficient to completely block NSC 125973-induced expression of XBP1s ^[1].
In Vivo: MKC8866 (oral ; 300 mg/kg; for 28 days) reduces tumor regrowth post-NSC 125973 withdrawal^[1].