型号:
产品价格:电议      采购度:1705      原产地:美洲
发布时间:2021/9/17 9:16:10 所属地区:国外 国外
简要描述:
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 (Kd= 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。
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CAS No. :
MCE 站:PY-60
产品活性: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 (Kd=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。
研究领域:Stem Cell/Wnt
作用靶点:YAP
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 (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 liberates the ANXA2-YAP complex from the cell membrane and competes for ANXA2 binding of phosphoinositides.
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.
相关产品:Verteporfin | AICAR | Cytochalasin D | ML-7 hydrochloride | TED-347 | YAP/TAZ inhibitor-1 | Lats-IN-1 | K-975 | YAP-TEAD-IN-1 TFA | Super-TDU (1-31) (TFA) | Super-TDU | VT107
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更新时间:2024/1/2 10:18:09
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