PY-60 |
Catalog No.GC62424
One-Click Copy Product Info
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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).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2765218-56-0
Sample solution is provided at 25 µL, 10mM.
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.
| 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 | |
| Formula | C16H15N3O2S | M.Wt | 313.37 |
| Solubility | DMSO : 100 mg/mL (319.11 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1911 mL | 15.9556 mL | 31.9112 mL |
| 5 mM | 638.2 μL | 3.1911 mL | 6.3822 mL |
| 10 mM | 319.1 μL | 1.5956 mL | 3.1911 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)