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XMU-MP-1

Catalog No. T4212 CAS 2061980-01-4

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

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XMU-MP-1, CAS 2061980-01-4

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Purity: 98%

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Description	XMU-MP-1 is an inhibitor of the pro-apoptotic, sterile 20-like kinases MST1 and 2.
Targets&IC50	MST2:38.1 nM, MST1:71.1 nM
In vitro	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.
In vivo	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.
Kinase Assay	XMU-MP-1 is dissolved in DMSO (stock concentration, 10 mM). For the in vitro kinase inhibition assays, recombinant GST-tagged MOB1a and various forms of recombinant His-tagged full-length MST1 or MST2 kinase are expressed and purified from Escherichia coli. The assays are performed with the various doses of XMU-MP-1 in the kinase assay buffer for 30 min at 30°C[1].

Molecular Weight	416.47
Formula	C17H16N6O3S2
CAS No.	2061980-01-4

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 30 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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.

Citations

1. Wang H, Shang Y, Wang E, et al. MST1 mediates neuronal loss and cognitive deficits: A novel therapeutic target for Alzheimer’s disease. Progress in Neurobiology. 2022: 102280 2. Yang L, Li N, Yang D, et al. CCL2 regulation of MST1-mTOR-STAT1 signaling axis controls BCR signaling and B-cell differentiation. Cell Death & Differentiation. 2021: 1-18 3. Zhu Y, Gu H, Yang L, et al. Involvement of MST1/mTORC1/STAT1 activity in the regulation of B-cell receptor signalling by chemokine receptor 2. Clinical and Translational Medicine. 2022, 12(7): e887. 4. Shang Y, Yan Y, Chen B, et al. Over‐expressed MST1 impaired spatial memory via disturbing neural oscillation patterns in mice. Genes, Brain and Behavior. 2020: e12678

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Inhibitor Library Immunology/Inflammation Compound Library Stem Cell Differentiation Compound Library Anti-Aging Compound Library Bioactive Compound Library

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Keywords

XMU-MP-1 2061980-01-4 干细胞 Hippo pathway XMU MP 1 Inhibitor Hippo (MST) inhibit XMUMP1 inhibitor

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