PY-60 is a potent and specific activator of YAP transcriptional activity, targeting annexin A2 (ANXA2) with a Kd of 1.4 μM. It directly binds to ANXA2, counteracting its normal function of repressing YAP activity. This compound dose-dependently induces luciferase activity in 293A-TEAD-LUC cells and promotes nuclear localization of YAP, while significantly increasing YAP-controlled transcripts in human cell lines.
- Targets annexin A2 to activate YAP
- Induces luciferase activity in 293A-TEAD-LUC cells
- Promotes YAP and TEAD protein association
- Increases YAP nuclear localization at high cell density
- Elevates YAP-controlled transcripts (ANRKD1, CYR61, CTGF)
- Liberates ANXA2-YAP complex from cell membrane
- Activates proproliferative, YAP-dependent program
- Promotes keratinocyte expansion and epidermal thickening in vivo