IAP ligand 8 is a SMAC mimetic and a binder of the BIR domain of IAP (inhibitor of apoptosis protein), which selectively targets cIAP1-BIR3, XIAP-BIR2 and XIAP-BIR3, with pKD values of 7.8, 7.0 and 6.7 respectively as determined by SPR. IAP ligand 8 serves as an IAP ligand moiety, which can be conjugated via a linker with degraders targeting the P site of TEAD1 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 8 and its series of degraders can be used for the research of solid tumors such as malignant pleural mesothelioma associated with abnormal activation of the Hippo pathway[1].
Molekulargewicht:
424.48
Formel:
C21H30F2N4O3
Anwendungsbeschreibung:
MCE Product type: Reference compound
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