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YAP

YAP inhibitors and activators target Yes-associated protein (YAP), a coactivator of growth genes. YAP was first described in 1994 as a proline-rich phosphoprotein that binds the Src homology 3 (SH3) domain of the Yes kinase. Its paralog, WW domain-containing transcription regulator 1 (TAZ), was reported in 2000 as a coactivator held in check by 14-3-3 proteins. In 2011 YAP and TAZ were shown to sense matrix stiffness and cell shape through actin tension. The actin polymerization inhibitor cytochalasin D is listed for such mechanotransduction work. YAP/TAZ inhibitor-1 and CIL56 act on the coactivators, and IAG933 and MYF-01-37 target their partner transcriptional enhanced associate domain (TEAD) factors. PROTAC YAP degrader-1 removes YAP, whereas PY-60 is a YAP activator.

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  • PROTAC YAP degrader-1
    Cat. No.
    A24091
    CAS No.
    3058483-58-9

    PROTAC YAP degrader-1

    PROTAC YAP degrader-1 (compound YZ-6) is a bifunctional molecule designed to selectively degrade Yes-associated protein (YAP), a key effector of the Hippo signaling pathway involved in cell proliferation, survival, and tumorigenesis. In addition to promoting proteasomal degradation of YAP, it also inhibits YAP's nuclear localization, thereby impairing its transcriptional co-activator functions.YZ-6 is composed of two main components:Target protein ligand: NSC682769 and E3 ubiquitin ligase recruiter with linker: (R,S,R)-AHPC-PEG2-C2-Boc which recruits the VHL E3 ligase complex. The linker used in the PROTAC design is Acid-PEG2-C2-Boc, facilitating optimal spatial orientation for ternary complex formation. The demethylated analog Demethyl-NSC682769 serves as a target ligand activity control. PROTAC YAP degrader-1 represents a novel tool for functional YAP inhibition and offers potential therapeutic applications in YAP-driven cancers and fibrotic diseases.

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