PY-60 是一种靶向膜联蛋白A2 (ANXA2) 的 YAP 转录活性的特异的激活剂 (K_d=1.4 µM)。PY-60 直接与 ANXA2 结合并拮抗其抑制 YAP 活性的正常细胞功能。

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.

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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 (EC50=?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 (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. has not independently confirmed the accuracy of these methods. They are for reference only.

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[1]. Shalhout SZ, et al. YAP-dependent proliferation by a small molecule targeting annexin A2. Nat Chem Biol. 2021;17(7):767-775.

In Vitro: DMSO : 100 mg/mL (319.11 mM; Need ultrasonic)配制储备液