IRE1 Degrader
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G6374
0 ImagesCat. No.: HY-180787G6374 is a IRE1 PRORAC degrader with DC50 values of 0.04 μM (AMO1) and 0.13 μM (KMS27), an EC50 value of 0.11 μM, and KD values of 0.56 nM and 90.2 nM for IRE1 and VHL, respectively. G6374 binds to the ATP pocket of the IRE1 kinase domain and VHL to form a ternary complex that recruits CRL2VHL, inducing K48-linked polyubiquitination of IRE1 at lysine residues K704 and K717, which in turn drives proteasomal degradation of monomeric and dimeric IRE1. G6374 can be used for the research of multiple myeloma.
