XMU-MP-1

製品コードS8334 バッチS833401

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17H16N6O3S2
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
* <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.

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.
in vitro XMU-MP-1 blocks MST1/2 kinase activities, thereby activating the downstream effector Yes-associated protein and promoting cell growth. XMU-MP-1 inhibits phosphorylation of MOB1 in a dose-dependent manner. Furthermore, with increasing ATP concentration, XMU-MP-1 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, XMU-MP-1 reduces the phosphorylation of endogenous MOB1, LATS1/2, and YAP in human liver carcinoma (HepG2) cells in a dose-dependent manner. Similarly, XMU-MP-1 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. XMU-MP-1 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. XMU-MP-1 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 XMU-MP-1 (1 mg/kg). XMU-MP-1 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
濃度 1 μM or 3 μM
反応時間 6 h
実験の流れ Real-time quantitative polymerase chain reaction (RT-qPCR) analysis of the expression levels of CTGF and CYR61 in HepG2 cells after XMUMP- 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.

カスタマーフィードバック

Data from [Data independently produced by , , FASEB J, 2019, 33(2):2514-2525]

Data from [Data independently produced by , , J Cell Physiol, 2019, 234(4):5117-5133]

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：

GPR137 inactivates Hippo signaling to promote gastric cancer cell malignancy [ Biol Direct, 2024, 19(1):3] PubMed: 38163861
WNT5a Signaling through ROR2 Activates the Hippo Pathway to Suppress YAP1 Activity and Tumor Growth [ Cancer Res, 2023, 83(7):1016-1030] PubMed: 36622276
Neutrophil Extracellular Traps Delay Diabetic Wound Healing by Inducing Endothelial-to-Mesenchymal Transition via the Hippo pathway [ Int J Biol Sci, 2023, 19(1):347-361] PubMed: 36594092
Neutrophil Extracellular Traps Delay Diabetic Wound Healing by Inducing Endothelial-to-Mesenchymal Transition via the Hippo pathway [ Int J Biol Sci, 2023, 19(1):347-361] PubMed: 36594092
Genetic and Pharmacological YAP Activation Induces Proliferation and Improves Survival in Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes [ Cells, 2023, 12(17)2121] PubMed: 37681853
Genetic and Pharmacological YAP Activation Induces Proliferation and Improves Survival in Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes [ Cells, 2023, 12(17)2121] PubMed: 37681853
Effects of Oncolytic Vaccinia Viruses Harboring Different Marine Lectins on Hepatocellular Carcinoma Cells [ Int J Mol Sci, 2023, 24(4)3823] PubMed: 36835232
A Comparative Study of Oncolytic Vaccinia Viruses Harboring Different Marine Lectins in Breast Cancer Cells [ Mar Drugs, 2023, 21(2)77] PubMed: 36827118
Comprehensive analysis and molecular map of Hippo signaling pathway in lower grade glioma: the perspective toward immune microenvironment and prognosis [ Front Oncol, 2023, 13:1198414] PubMed: 37251938
Oxidative stress-CBP axis modulates MOB1 acetylation and activates the Hippo signaling pathway [ Nucleic Acids Res, 2022, 50(7):3817-3834] PubMed: 35349706

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。

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