4µ8C is a potent inhibitor of the ER transmembrane protein IRE1, which mediates the unfolded protein response. 4µ8C inhibits regulated IRE1-dependent degradation (RIDD) and unconventional spicing of XBP1 mRNA in response to endopasmic reticulum (ER) stress, but has no affect on the kinase activity of IRE1.
4?8C is a salicylaldehyde derivative and its inhibitory action targets the K907 lysine residue in RNase (ribonuclease) domain and affects IRE1? (endoplasmic reticulum to nucleus signaling 1) RNase activity. In vitro analysis proved that 4?8C was able to inhibit the release of insulin at high glucose levels.
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