PY-60 |
カタログ番号GC62424
One-Click Copy Product Info
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PY-60は、5-フェニルイソオキサゾールを核心構造とするチアゾール代替の誘導体であり、YAP (EC50 = 1.6µM)の転写活性を強力かつ特異的に活性化できる。
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は、5-フェニルイソオキサゾールを核心構造とするチアゾール代替の誘導体であり、YAP (EC50 = 1.6µM)の転写活性を強力かつ特異的に活性化できる[1]。PY-60は、細胞膜からのANXA2の放出を促進し、YAPへのその結合制限を弱め、よってYAPの脱リン酸化を増強し、核へのその転座を促進し、よってYAPの転写共同活性剤機能を活性化する[1-2]。PY-60はよく組織の再生と修復に使われている[3]。
ヒト網膜芽細胞腫（RB）細胞Y79とRB3823では、PY-60 (0, 1, 5, 10μM；24時間)の処理は、転写的に活発なYAPを誘発し、よってRB細胞Y79とRB3823の増殖を阻害する[4]。MDA-MB-231細胞で、PY-60 (0, 2, 4, 8μM；24時間)は、高密度のMDA-MB-231細胞の増殖、移動と浸潤を促進する[5]。A549とNCI-H358細胞で、PY-60 (10μM；24時間)は、LUAD細胞に対するRFX2過剰発見の阻害効果を逆転させた[6]。HuCCT1細胞で、PY-60 (10μM；24時間)は、細胞の移動、接着と浸潤に対するPIN1ノックダウンの阻害効果を逆転させた[7]。
C57BL/6 WTマウスで、PY-60 (10mg/mL；塗抹；10日間)の処理は、マウスで、初代表皮角化細胞のコロニー形成能力を増強する[1]。ラットくも膜下出血モデルで、PY-60 (0.2mg/kg；脳室内投与；単回投与)はNE-52-QQ57の神経保護作用を部分的に廃止した[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.
| 細胞実験[1]: | |
細胞株 | ヒト網膜芽細胞腫細胞Y79とRB3823 |
準備方法 | ヒト網膜芽細胞腫細胞Y79とRB3823の細胞生存率を、MTSキットで検出した。1ウェルあたり[1-2]×103細胞の密度で、細胞を96ウェルのプレートに播種した。24時間の培養後、様々な濃度のPY-60(0, 1, 5, 10μM)を添加し、細胞を処理した。処理は24時間続き、20μLのMTS試薬を最後の4時間に、各ウェルに添加した。 |
反応条件 | 0, 1, 5, 10μM；24時間 |
アプリケーション | MTSアッセイで確認されたところ、Y79とRB3823細胞の増殖は、10μM PY-60で抑制された。 |
| 動物実験 [2]: | |
動物モデル | C57BL/6マウス |
準備方法 | 十日間連続で、溶媒のみ（アセトン）またはPY-60 (10mg/mL)で、C57BL/6 WTマウス（8週齢）を1日1回（皮膚に局所的に塗布）処理した。H&E染色で、表皮の厚さを評価した。抗K14と抗K167免疫蛍光染色を使い、細胞の拡張を評価した。全てのモデルで、塗布の前に、動物をランダムに同じ平均体重のグループに分けた。 |
投与形態 | 10mg/mL；塗布；10日間 |
アプリケーション | PY-60の処理は、マウスで、初代表皮角化細胞のコロニー形成能力を増強する。 |
References: | |
| Cas No. | 2765218-56-0 | SDF | |
| Formula | C16H15N3O2S | M.Wt | 313.37 |
| 溶解度 | 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 | |||
|
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 |
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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.
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Quality Control & SDS
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- 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.)