MKC8866 (ORIN1001) is a spectific small molecule inhibitor of mammalian IRE1 RNase activity with IC50 of 0.29 uM.
ORIN1001 (MKC8866) prevents the recombinant IRE1 protein from cleaving the synthetic XBP1 RNA probe, but has no effect on RNase A, RNase L and yeast IRE1 (scIRE1).
ORIN1001 (MKC8866) suppresses growth of patient-derived tumors with high MYC expression.|
ORIN1001 (MKC8866) potently sensitizes the tumors to the apoptotic and proliferation inhibitory effects of chemotherapy in vivo.
