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受注：045-509-1970 |
技術サポート：tech@selleck.co.jp 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
化学情報
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C17H16N6O3S2 |
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| 分子量 | 416.48 | CAS No. | 2061980-01-4 | |
| Solubility (25°C)* | 体外 | DMSO | 83 mg/mL (199.28 mM) | |
| Ethanol | 2 mg/mL (4.8 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | XMU-MP-1 is an inhibitor of MST1/2 with IC50 values of 71.1±12.9 nM and 38.1±6.9 nM against MST1 and MST2, respectively. |
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| in vitro | XMU-MP-1 blocks MST1/2 kinase activities, thereby activating the downstream effector Yes-associated protein and promoting cell growth. This compound inhibits phosphorylation of MOB1 in a dose-dependent manner. Furthermore, with increasing ATP concentration, it exhibits a proportional increase in IC50 against MST1/2, as well as an attenuated inhibition of the MST2-mediated phosphorylation of MOB1. At concentrations ranging from 0.1 to 10 μM, this chemical reduces the phosphorylation of endogenous MOB1, LATS1/2, and YAP in human liver carcinoma (HepG2) cells in a dose-dependent manner. Similarly, its treatment inhibits hydrogen peroxide (H2O2)-stimulated MOB1 phosphorylation and MST1/2 autophosphorylation in a variety of cell lines, including mouse macrophage-like cells (RAW264.7), human osteosarcoma (U2OS), human colorectal adenocarcinoma (SW480), immortalized human retinal pigment epithelial cells (RPE1), human pleomorphic hepatocellular carcinoma (SNU-423), and HepG2, as well as primary mouse hepatocytes, without affecting the phosphorylation of JNK (c-Jun N-terminal kinase), which is a positive control for H2O2 stimulation. This treatment increases YAP nuclear translocation[1]. |
| in vivo | XMU-MP-1 displays excellent in vivo pharmacokinetics and is able to augment mouse intestinal repair, as well as liver repair and regeneration, in both acute and chronic liver injury mouse models at a dose of 1 to 3 mg/kg via intraperitoneal injection. This compound exhibits favorable pharmacokinetics in rats with a half-life of 1.2 hours and a bioavailability of 39.5%. The maximal phosphorylation inhibition of MOB1 and YAP is achieved between 1.5 and 6 hours after intraperitoneal dosing with this chemical (1 mg/kg). It protects mice from DSS-induced colitis and ameliorates chronic liver injury[1]. |
プロトコル(参考用のみ)
| 細胞アッセイ | 細胞株 | HepG2 |
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| 濃度 | 1 μM or 3 μM | |
| 反応時間 | 6 h | |
| 実験の流れ | Real-time quantitative polymerase polymerase chain reaction (RT-qPCR) analysis of the expression levels of CTGF and CYR61 in HepG2 cells after XMU-MP-1 treatment for 6 hours is conducted. | |
| 動物実験 | 動物モデル | FRG mice |
| 投薬量 | 1 mg/kg | |
| 投与方法 | i.p. |
参考
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カスタマーフィードバック
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Data from [Data independently produced by , , FASEB J, 2019, 33(2):2514-2525]
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Data from [Data independently produced by , , J Cell Physiol, 2019, 234(4):5117-5133]
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Data from [Data independently produced by , , Phytother Res, 2018, 32(12):2456-2465]
Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| Exosome- transported FER inhibitor suppresses progression of diffuse large B-cell lymphoma via regulating AJUBA/Hippo axis [ NPJ Precis Oncol, 2025, 9(1):258] | PubMed: 40707658 |
| Phenylpropanoids of Eleutherococcus senticosus (Rupr. & maxim.) maxim. Alleviate oxidative stress in Alzheimer's disease in vitro and in vivo models by regulating Mst1 and affecting the Nrf2/Sirt3 pathway [ Bioorg Chem, 2025, 159:108347] | PubMed: 40081261 |
| Endometriosis-derived exosomes encapsulated miR-196a-5p mediate macrophage polarization through regulation of the Hippo pathway [ J Cell Commun Signal, 2025, 19(2):e70020] | PubMed: 40416727 |
| Tanshinone IIA attenuates hepatic stellate cell activation, oxidative stress, and liver fibrosis by inhibiting YAP signaling [ Eur J Histochem, 2025, 69(3)4218] | PubMed: 40525818 |
| Targeting metastasis-initiating cancer stem cells in gastric cancer with leukaemia inhibitory factor [ Cell Death Discov, 2024, 10(1):120] | PubMed: 38453889 |
| Wnt2bb signaling promotes pharyngeal chondrogenic precursor proliferation and chondrocyte maturation by activating Yap expression in zebrafish [ J Genet Genomics, 2024, S1673-8527(24)00307-2] | PubMed: 39566725 |
| SLMAP3 is crucial for organogenesis through mechanisms involving primary cilia formation [ Open Biol, 2024, 14(10):rsob240206] | PubMed: 39417621 |
| ACADL-YAP axis activity in non-small cell lung cancer carcinogenicity [ Cancer Cell Int, 2024, 24(1):86] | PubMed: 38402174 |
| CircPOLA2 sensitizes non-small cell lung cancer cells to ferroptosis and suppresses tumorigenesis via the Merlin-YAP signaling pathway [ iScience, 2024, 27(9):110832] | PubMed: 39310771 |
| GPR137 inactivates Hippo signaling to promote gastric cancer cell malignancy [ Biol Direct, 2024, 19(1):3] | PubMed: 38163861 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。