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.
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.
Store lyophilized at -20ºC, keep desiccated. In lyophilized form, the chemical is stable for 36 months. In solution, store at -20ºC and use within 1 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
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