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XMU-MP-1

XMU-MP-1 是一种促凋亡、无菌的 20 样激酶 MST1 和 2 的抑制剂。

CAS号

2061980-01-4

分子式

C17H16N6O3S2

主要靶点

Hippo pathway

仅限科研使用

Cat No : CM05215

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Synonyms

验证数据展示

  • CAS No.: 2061980-01-4

    XMU-MP-1
    CAS#: 2061980-01-4

产品信息

XMU-MP-1 is an inhibitor of the pro-apoptotic, sterile 20-like kinases MST1 and 2.

CAS号 2061980-01-4
分子式 C17H16N6O3S2
主要靶点 Hippo pathway
主要通路 干细胞
分子量 416.47
纯度 99.68%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

MST1:71.1 nM|MST2:38.1 nM

体内活性

XMU-MP-1 displays excellent in 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 treatment exhibited substantially greater repopulation rate of human hepatocytes in the Fah-deficient mouse model than in the vehicle-treated control, indicating that XMU-MP-1 treatment might facilitate human liver regeneration. Thus, the pharmacological modulation of MST1/2 kinase activities provides a novel approach to potentiate tissue repair and regeneration, with XMU-MP-1 as the first lead for the development of targeted regenerative therapeutics.

体外活性

XMU-MP-1 reduces the phosphorylation of endogenous MOB1, LATS1/2, and YAP in HepG2 cells in a dose-dependent manner at concentrations ranging from 0.1 to 10 μM. XMU-MP-1 treatment inhibits hydrogen peroxide-stimulated MOB1 phosphorylation and MST1/2 autophosphorylation in a variety of cell lines, including mouse macrophage-like cells, human osteosarcoma, human colorectal adenocarcinoma cells. XMU-MP-1 blocks MST1/2 kinase activities, thereby activating the downstream effector Yes-associated protein and promoting cell growth. XMU-MP-1 can potently and reversibly suppress the activities of kinases MST1/2 and enhance their downstream YAP activation in cells.

溶解度

DMSO:30 mg/mL

参考文献

1.Fan F, et al. Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration. Sci Transl Med. 2016 Aug 17;8(352):352ra108.
2.Zhu Y, Gu H, Yang L, et al. The sequential role of Mst1/mTORC1/STAT1 activity in chemokine receptor 2-regulated B cell receptor signaling[J]. Authorea Preprints. 2021
3.Shang Y, Yan Y, Chen B, et al. Over‐expressed MST1 impaired spatial memory via disturbing neural oscillation patterns in mice[J]. Genes, Brain and Behavior. 2020: e12678.
4.Yang L, Li N, Yang D, et al. CCL2 regulation of MST1-mTOR-STAT1 signaling axis controls BCR signaling and B-cell differentiation[J]. Cell Death & Differentiation. 2021: 1-18.

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The dilution calculator equation

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