PY-60
目录号 : GC62424
PY-60是一种以5-苯基异噁唑为核心结构的噻唑取代衍生物，能够强效且特异性地激活YAP的转录活性（EC50 = 1.6µM）。
Cas No.:2765218-56-0
Sample solution is provided at 25 µL, 10mM.
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PY-60 is a thiazole-substituted derivative with 5-phenylisoxazole as its core structure, which can potently and specifically activate the transcriptional activity of YAP (EC50 = 1.6µM) [1]. PY-60 promotes the release of ANXA2 from the cell membrane, weakens its binding restriction to YAP, thereby enhancing the dephosphorylation of YAP and promoting its translocation into the nucleus, thereby activating the transcriptional coactivator function of YAP [1-2]. PY-60 is often used for tissue regeneration and repair [3].
In human retinoblastoma (RB) cells Y79 and RB3823, PY-60 (0, 1, 5, 10μM; 24h) treatment induced transcriptionally active YAP, thereby inhibiting the proliferation of RB cells Y79 and RB3823 [4]. In MDA-MB-231 cells, PY-60 (0, 2, 4, 8μM; 24h) promotes proliferation, migration, and invasion of high-density MDA-MB-231 cells [5]. In A549 and NCI-H358 cells, PY-60 (10μM; 24h) reversed the inhibitory effect of RFX2 overexpression on LUAD cells [6]. In HuCCT1 cells, PY-60 (10μM; 24h) reversed the inhibitory effects of PIN1 knockdown on cell migration, adhesion, and invasion [7].
In C57BL/6 WT mice, PY-60 (10mg/mL; smear; 10d) treatment enhances the colony forming potential of primary epidermal keratinocytes in mice [1]. In the rat subarachnoid hemorrhage model, PY-60 (0.2mg/kg; intraventricular administration; single injection) partially abolished the neuroprotective effect of NE-52-QQ57 [8].
References:
[1]. Shalhout SZ, Yang PY, Grzelak EM, et al. YAP-dependent proliferation by a small molecule targeting annexin A2. Nature Chemical Biology. 2021 Jul; 17(7): 767-775.
[2]. Martin JF. Regeneration and rejuvenation of skin by a topical YAP activator. Proceedings of the National Academy of Sciences. 2023 Aug 8; 120(32): e2309991120.
[3]. Grzelak EM, Elshan ND, Shao S, et al. Pharmacological YAP activation promotes regenerative repair of cutaneous wounds. Proceedings of the National Academy of Sciences. 2023 Jul 11; 120(28): e2305085120.
[4]. Zhong L, Meng X, Huang J, et al. Expression of yap suppresses cell proliferation and elevates the sensitivity of chemotherapy in retinoblastoma cells through lipid-peroxidation induced ferroptosis. Chinese Clinical Oncology. 2023 Oct 31; 12(5): 52.
[5]. Chen J, Su X, Tan Q, et al. Effect of cell density on the malignant biological behavior of breast cancer by altering the subcellular localization of ANXA2 and its clinical implications. Clinical and Translational Oncology. 2022 Nov; 24(11): 2136-2145.
[6]. Kong Z, Zhou P, Xu J, et al. RFX2 downregulates RASSF1 expression and YAP phosphorylation through Hippo signaling to promote immune escape in lung adenocarcinoma. Cell Division. 2025 Mar 11; 20(1): 7.
[7]. Wang Y, Liu Y, Chen H, et al. PIN1 promotes the metastasis of cholangiocarcinoma cells by RACK1-mediated phosphorylation of ANXA2. Cellular Oncology. 2024 Aug; 47(4): 1233-1252.
[8]. He Q, Zhou Y, Wu L, et al. Inhibition of acid-sensing receptor GPR4 attenuates neuronal ferroptosis via RhoA/YAP signaling in a rat model of subarachnoid hemorrhage. Free Radical Biology and Medicine. 2024 Nov 20; 225: 333-345.
PY-60是一种以5-苯基异噁唑为核心结构的噻唑取代衍生物，能够强效且特异性地激活YAP的转录活性（EC50 = 1.6µM） [1]。PY-60促进ANXA2从细胞膜上释放，减弱其与YAP的结合限制，从而增强YAP的去磷酸化并促进其转位至细胞核内，进而激活YAP的转录共激活因子功能 [1-2]。PY-60常用于组织再生和修复 [3]。
在人类视网膜母细胞瘤（RB）细胞Y79和RB3823中，PY-60（0、1、5、10μM；24h）处理诱导转录活性YAP，从而抑制RB细胞Y79和RB3823的增殖 [4]。在MDA-MB-231细胞中，PY-60（0、2、4、8μM；24h）促进高密度MDA-MB-231细胞的增殖、迁移和侵袭 [5]。在A549和NCI-H358细胞中，PY-60（10μM；24h）可逆转RFX2过表达对LUAD细胞的抑制作用 [6]。在HuCCT1细胞中，PY-60（10μM；24h）可逆转PIN1敲低对细胞迁移、粘附和侵袭的抑制作用 [7]。
在C57BL/6野生型小鼠中，PY-60（10mg/mL；涂抹；10d）处理可增强小鼠原代表皮角质形成细胞的集落形成潜能 [1]。在大鼠蛛网膜下腔出血模型中，PY-60（0.2mg/kg；脑室内给药；单次注射）部分消除了NE-52-QQ57的神经保护作用 [8]。
| Cell experiment [1]: | |
Cell lines | Human retinoblastoma cells Y79 and RB3823 |
Preparation Method | The cell viability of human retinoblastoma cells Y79 and RB3823 was detected using the MTS kit. The cells were seeded in a 96-well plate at a density of [1-2]×103 cells per well. After 24h of culture, different concentrations of PY-60 (0, 1, 5, 10μM) were added to treat the cells. The treatment lasted for 24h, and 20μL of MTS reagent was added to each well in the last 4h. |
Reaction Conditions | 0, 1, 5, 10μM; 24h |
Applications | Cell proliferation of Y79 and RB3823 cells were suppressed by 10μM PY-60 confirmed by MTS assay. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | C57BL/6 WT mice (8 weeks of age) were treated once per day (topically, on the skin) for ten consecutive days with either vehicle only (acetone) or PY-60 (10mg/mL). The epidermis was assessed for thickness using H&E staining. Anti-K14 and anti-K167 immunofluorescent staining were used to assess cell expansion. In all models, animals were randomly assorted into groups of equal mean body weight before topical dosing. |
Dosage form | 10mg/mL; smear; 10d |
Applications | PY-60 treatment enhances the colony forming potential of primary epidermal keratinocytes in mice. |
References: | |
| Cas No. | 2765218-56-0 | SDF | |
| 分子式 | C16H15N3O2S | 分子量 | 313.37 |
| 溶解度 | DMSO : 100 mg/mL (319.11 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1911 mL | 15.9556 mL | 31.9112 mL |
| 5 mM | 0.6382 mL | 3.1911 mL | 6.3822 mL |
| 10 mM | 0.3191 mL | 1.5956 mL | 3.1911 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
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