Catalog No.: PC-25597Not For Human Use, Lab Use Only.
IA107 is a potent and selective inositol-requiring enzyme 1 alpha (IRE1α) inhibitor, inhibitsIRE1α and phosphorylated IRE1α RNase activity in FRET assay with IC50 of 16 nM and 9 nM, respectively.
IA107 is a potent and selective inositol-requiring enzyme 1 alpha (IRE1α) inhibitor, inhibitsIRE1α and phosphorylated IRE1α RNase activity in FRET assay with IC50 of 16 nM and 9 nM, respectively.
IA107 binds to IRE1α with ITC KD of 0.94 uM and MST KD of 1.36 uM.
IA107 shows binding affinity against p-IRE1α with MST KD of 152 nM.
IA107 prefers to bind to the dimeric form of IRE1α to inhibit its RNase activity.
IA107 shows minimal (<10%) to low (<30%) inhibitory activity at 5 uM in a kinase profiling assay, IA107 inhibits the kinase domain of the IRE1β (ERN2) isoform with an IC50 of 1440 nM in the LanthaScreenTM Eu kinase binding assay.
IA107 (5-50 uM) inhibited ER stress induced by tunicamycin and induced XBP1 mRNA splicing in A549 cells.
