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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 Chemical Structure
XMU-MP-1, CAS 2061980-01-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 48.00
2 mg In stock $ 72.00
5 mg In stock $ 98.00
10 mg In stock $ 155.00
25 mg In stock $ 322.00
50 mg In stock $ 538.00
100 mg In stock $ 778.00
1 mL * 10 mM (in DMSO) In stock $ 96.00
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Purity: 99.68%
Purity: 99.58%
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Biological Description
Chemical Properties
Storage & Solubility Information
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 effectively reduces the phosphorylation of MOB1, LATS1/2, and YAP in HepG2 cells in a concentration-dependent manner, with effective doses ranging from 0.1 to 10 μM. It also inhibits MOB1 phosphorylation induced by hydrogen peroxide and prevents MST1/2 autophosphorylation across various cell lines, including mouse macrophage-like cells, human osteosarcoma, and human colorectal adenocarcinoma cells. By blocking MST1/2 kinase activities, XMU-MP-1 activates the downstream effector, Yes-associated protein (YAP), thereby promoting cell growth. Its action potently and reversibly suppresses the activities of MST1/2 kinases, enhancing 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 416.48
Formula C17H16N6O3S2
CAS No. 2061980-01-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 12.5 mg/mL (30.01 mM)

TargetMolReferences 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.

TargetMolCitations

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 5. Xu W, Shi Z, Yu X, et al.Salvianolic acid B exerts an anti-hepatocellular carcinoma effect by regulating the Hippo/YAP pathway and promoting pSmad3L to pSmad3C simultaneously.European Journal of Pharmacology.2022: 175423.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Kinase Inhibitor Library Stem Cell Differentiation Compound Library Bioactive Compound Library Anti-Cancer Compound Library Anti-Prostate Cancer Compound Library Immunology/Inflammation Compound Library NO PAINS Compound Library Anti-Aging Compound Library Bioactive Compounds Library Max

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Keywords

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

 

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