PY-60 is a robust and specific activator of YAP transcriptional activity that targets annexin A2 (ANXA2) with a K d of 1.4 µM. PY-60 directly binds to ANXA2 and antagonizes its normal cellular function of repressing YAP activity. In Vitro PY-60 targets ANXA2 to activate YAP. ? PY-60, a thiazole-substituted derivative, dose-dependently induces luciferase activity in 293A-TEAD-LUC cells in the presence or absence of serum when cells were plated at high cell density (EC 50 =?1.5 and 1.6?μM, respectively). PY-60 treatment also dose-dependently promoted the association of YAP and TEAD proteins in cells and induced the nuclear localization of YAP in response to increased cell density. PY-60 robustly increases the levels of YAP-controlled transcripts (that is, ANRKD1 , CYR61 and CTGF ) in 293A cells and other human cell lines (that is, MCF10A, HEK293T, H69 and HaCaT), but did not augment the levels of YAP itself ( YAP1 ). ? PY-60 activates a proproliferative, YAP-dependent transcriptional program in the adult animal capable of remodeling the epidermis through proliferation. ? PY-60 liberates the ANXA2-YAP complex from the cell membrane and competes for ANXA2 binding of phosphoinositides. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo PY-60 (10?uM; applied topically to the dorsal skin of wild-type adult C57BL/6 mice over the course of 10?days) promotes a dramatic expansion of keratinocytes and K14-positive precursors, as assessed by hematoxylin and eosin and anti-K14 histological staining at the study end. PY-60 results in an approximate doubling of epidermal thickness, a result derived from an increased number of keratinocytes per unit length of skin . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
PY-60
CAS number：2765218-56-0 molecular formula：C16H15N3O2S
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 2765218-56-0 | molecular formula | C16H15N3O2S |
| molecular weight | 313.37 g/mol | Exact mass | ≥98% |
| PSA | - | logp | - |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
No safety information yet
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
