IAP ligand 9 is a SMAC mimetic and a binder of the BIR domain of IAP (inhibitor of apoptosis protein), which selectively targets cIAP1-BIR3, XIAP-BIR3 with extremely weak binding affinity to XIAP-BIR2, showing pKD values of 7.0, 8.0, and 5.0 respectively in SPR assays. IAP ligand 9 serves as an IAP ligand moiety, and conjugates via a linker with degraders targeting the TEAD1 P site to form IAP-recruiting proteolysis-targeting chimeras (PROTACs/IPDs). This IPD recruits IAP E3 ubiquitin ligase to form a TEAD1-IPD-IAP ternary complex, thereby mediating the ubiquitination and proteasome-dependent degradation of TEAD1, while inducing the autodegradation of cIAP1. IAP ligand 9 and its series of degraders are applicable to the research of solid tumors such as malignant pleural mesothelioma associated with aberrant activation of the Hippo pathway[1].
Molecular Weight:
436.52
Formula:
C22H33FN4O4
Target:
IAP,Ligands for E3 Ligase
Application Notes:
MCE Product type: Reference compound
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