GLPBio

PY-60

Catalog No.: GC62424Purity:>98.00%
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).

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PY-60
Cas No.: 2765218-56-0
10mM (in 1mL DMSO)In Stock
$76.00
1
5mgIn Stock
$69.00
1
10mgIn Stock
$111.00
1
25mgIn Stock
$168.00
1
50mgIn Stock
$284.00
1

Citations

1 publicationsPublications from researchers using this product

Description

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.

Protocol

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:
[1]. 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.
[2]. 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.

Product Documents

Purity:>98.00%Appearance:A solid

Chemical Properties

CAS No.
2765218-56-0
Molecular Formula
C16H15N3O2S
Molecular Weight
313.37
Solubility
DMSO : 100 mg/mL (319.11 mM; Need ultrasonic)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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