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YAP activator PY-60

Chemical Structure : YAP activator PY-60

CAS No.: 2765218-56-0

YAP activator PY-60 (PY-60, PY60)

Catalog No.: PC-38304Not For Human Use, Lab Use Only.

YAP activator PY-60 (PY-60) is a novel small molecule activator of YAP transcriptional activity (EC50=1.5 uM) via targeting annexin A2 (ANXA2).

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Biological Activity

YAP activator PY-60 (PY-60) is a novel small molecule activator of YAP transcriptional activity (EC50=1.5 uM) via targeting annexin A2 (ANXA2).
PY-60 dose-dependently induced luciferase activity in 293A-TEAD-LUC cells, robustly activateed YAP transcriptional activity in vitro.
PY-60 treatment robustly increased the levels of YAP-controlled transcripts (ANRKD1, CYR61 and CTGF) in 293A cells and other human cell lines (MCF10A, HEK293T, H69 and HaCaT), but did not augment the levels of YAP itself (YAP1).
PY-60 promotes YAP-dependent expansion of epidermal keratinocytes in mouse following topical drug administration. Annexin A2 (ANXA2) is a protein that directly associates with YAP at the cell membrane in response to increased cell density.
PY-60 treatment liberates ANXA2 from the membrane, ultimately promoting a phosphatase-bound, nonphosphorylated and transcriptionally active form of YAP.

Physicochemical Properties

M.Wt 313.375
Formula C16H15N3O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-phenyl-N-(3-(thiazol-2-yl)propyl)isoxazole-3-carboxamide

References

1. Shalhout SZ, et al. Nat Chem Biol. 2021 Jul;17(7):767-775. 

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