IRE1α kinase-IN-1 is a selective inhibitor of the kinase domain of IRE1α (inositol-requiring enzyme 1 alpha), a key sensor in the unfolded protein response (UPR). It is widely used in research to modulate endoplasmic reticulum (ER) stress signaling pathways. By inhibiting IRE1α kinase activity, this compound helps suppress the downstream activation of pathways involved in inflammation, cell survival, and apoptosis, making it a valuable tool for studying diseases linked to chronic ER stress.

It has been applied in studies related to neurodegenerative disorders, diabetes, and cancer, where dysregulated UPR contributes to disease progression. In cancer research, IRE1α kinase-IN-1 is used to sensitize tumor cells to apoptosis, especially in multiple myeloma and solid tumors that rely on UPR for survival under stress conditions. Additionally, it aids in dissecting the dual kinase and endoribonuclease functions of IRE1α, allowing researchers to explore selective therapeutic strategies without fully blocking IRE1α’s RNase activity. Its use is primarily confined to in vitro and preclinical models due to ongoing development for clinical applications.