TEAD ligand-Linker Conjugate 3 (A536) is an ALP2-based, TEAD1-targeting, IAP-recruiting bifunctional degrader (IPD) with a DC50 of 110 nM and a maximum degradation efficiency (Dmax) of 51% for human TEAD1. TEAD ligand-Linker Conjugate 3 also efficiently binds to cIAP1 and induces its self-degradation (IC50=122 nM), exhibiting good cell permeability. TEAD ligand-Linker Conjugate 3 consists of an ALP2 target protein ligand and a PROTAC linker, and can be used to synthesize PROTACs (such as HY-181594). A536 can dose-dependently inhibit the proliferation of Hippo pathway-dependent human malignant mesothelioma cells and downregulate the transcriptional expression of CTGF, a downstream target gene of TEAD1. A536 can be used to study the mechanism of malignant tumors with abnormal activation of the Hippo pathway (especially NF2 mutant mesothelioma)[1].
Molecular Weight:
608.05
Formula:
C32H29ClF3N5O2
Target:
IAP,Target Protein Ligand-Linker Conjugates,YAP
Application Notes:
MCE Product type: Reference compound
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