PY-60是一种选择性激活膜联蛋白A2 (ANXA2) 的 YAP 转录活性的小分子激动剂 (Kd=1.4 μM)。通过直接与 ANXA2 结合,PY-60 拮抗其抑制 YAP 活性的作用,展现了在癌症治疗中的应用潜力。


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| Concentration | Treated Time | Description | References | |
| HEK293A cells | HEK293A cells | 2 to 24 h | At least 16 h of continuous PY-60 exposure was required for maximal induction of YAP transcriptional response. | Proc Natl Acad Sci U S A. 2023 Jul 11;120(28):e2305085120. |
| primary adult human epidermal keratinocytes (HEKa) | primary adult human epidermal keratinocytes (HEKa) | 24 h | PY-60 induced a robust YAP-driven transcriptional program, reducing terminal differentiation and apoptosis of keratinocytes and increasing proliferative capacity. | Proc Natl Acad Sci U S A. 2023 Jul 11;120(28):e2305085120. |
| HK-2 cells | HK-2 cells | PY-60 increased the expression of Nrf2, while YAP1 knockdown counteracted the effect of TMP on autophagic flux. | Int J Biol Sci. 2025 Jan 13;21(3):1158-1173. | |
| Mouse primary hepatocytes | Mouse primary hepatocytes | PY-60 significantly inhibited H/R-induced apoptosis in RAMP1-KO primary hepatocytes by suppressing YAP phosphorylation. | J Clin Transl Hepatol. 2024 Apr 28;12(4):357-370. | |
| NCI-H358 cells | NCI-H358 cells | To examine the effect of PY-60 on the Hippo pathway, results showed PY-60 increased YAP protein levels and inhibited its phosphorylation | Cell Div. 2025 Mar 11;20(1):7. | |
| A-549 cells | A-549 cells | To examine the effect of PY-60 on the Hippo pathway, results showed PY-60 increased YAP protein levels and inhibited its phosphorylation | Cell Div. 2025 Mar 11;20(1):7. |
| Administration | Dosage | Frequency | Description | References | ||
| Yucatan mini pig | Partial and full thickness wound models | Topical application | 0.15 wt% gel | Every other day for 8 days | PY-60 significantly accelerated the closure of partial and full thickness wounds, increasing the thickness of both epidermal and dermal layers. | Proc Natl Acad Sci U S A. 2023 Jul 11;120(28):e2305085120. |
| Mice | 70% liver ischemia-reperfusion model in RAMP1-KO mice | Intraperitoneal injection | 10 mg/kg | Single dose, lasting 6 hours | PY-60 significantly alleviated liver ischemia-reperfusion injury by inhibiting YAP phosphorylation and reducing hepatocyte apoptosis. | J Clin Transl Hepatol. 2024 Apr 28;12(4):357-370. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
3.19mL 0.64mL 0.32mL |
15.96mL 3.19mL 1.60mL |
31.91mL 6.38mL 3.19mL |
|
| CAS号 | 2765218-56-0 |
| 分子式 | C16H15N3O2S |
| 分子量 | 313.37 |
| SMILES Code | O=C(C1=NOC(C2=CC=CC=C2)=C1)NCCCC3=NC=CS3 |
| MDL No. | MFCD34474253 |
| 别名 | |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
| 溶解方案 |
DMSO: 105 mg/mL(335.06 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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