[CAS NO. 2061980-01-4] XMU-MP-1
PRODUCTS SPECIFICATIONS [2061980-01-4]
DESCRIPTION [2061980-01-4]
Overview
| MDL | MFCD30377214 |
|---|---|
| Molecular Weight | 416.48 |
| Molecular Formula | C17H16N6O3S2 |
| SMILES | O=S(C1=CC=C(NC2=NC=C(C(N(C)C3=C4SC=C3)=N2)N(C)C4=O)C=C1)(N)=O |
29 Publications Citing Use of MCE
- [1]Nature. 2022 Jan;601(7894):600-605.
- [2]Nat Immunol. 2017 Sep;18(9):973-984.
- [3]Ann Rheum Dis. 2021 Jul;80(7):891-902.
- [4]Nat Commun. 2022 Jun 2;13(1):3075.
- [5]EMBO J. 2023 Jan 2;e112184.
- [6]Theranostics. 2021; 11(17):8480-8499.
- [7]Cell Rep. 2021 Jul 13;36(2):109347.
- [8]Cell Rep. 2017 Dec 19;21(12):3612-3623.
- [9]Oncogene. 2021 Oct 6.
- [10]Clin Transl Med. 12 September 2021.
- [11]Stem Cell Reports. 2022 Jan 28;S2213-6711(22)00051-0.
- [12]Br J Pharmacol. 2019 Oct;176(20):3956-3971.
- [13]Aging Cell. 2021 Aug 20;e13465.
- [14]Cell Death Dis. 2021 Oct 5;12(10):907.
- [15]J Med Chem. 2022 Aug 29.
- [16]Stem Cells. 19 January 2022.
- [17]Biochim Biophys Acta Mol Basis Dis. 29 October 2022, 166586.
- [18]Phytomedicine. 2020, Jul 28.
- [19]Arthritis Res Ther. 2022 Nov 2;24(1):247.
- [20]Biochem J. 2019 Mar 12;476(5):875-887.
- [21]Cell Signal. 2020 Sep;73:109697.
- [22]Exp Cell Res. 2022 Nov 2;113407.
- [23]Inflamm Res. 2022 Jun 22.
- [24]Am J Physiol Renal Physiol. 2022 Mar 7.
- [25]Environ Toxicol. 2020 Jun;35(6):643-651.
- [26]Thromb Res. 2022.
- [27]Exp Physiol. 2020 Aug;105(8):1360-1372.
- [28]Clin Exp Hypertens. 2019 Feb 26:1-10.
- [29]Research Square Preprint. 2022 Feb.
Summary
XMU-MP-1 is a reversible and selective MST1/2 inhibitor with IC 50 s of 71.1 and 38.1 nM, respectively [1] .
IC50 & Target
IC50: 71.1 (MST1), 38.1 nM (MST2) [1]
In Vitro
At concentrations ranging from 0.1 to 10 μM, XMU-MP-1 reduces the phosphorylation of endogenous MOB1, LATS1/2, and YAP in HepG2 cells in a dose-dependent manner. 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 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. XMUMP-1 treatment exhibits 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 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 8 mg/mL ( 19.21 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4011 mL | 12.0054 mL | 24.0108 mL |
| 5 mM | 0.4802 mL | 2.4011 mL | 4.8022 mL |
| 10 mM | 0.2401 mL | 1.2005 mL | 2.4011 mL |
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1.
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2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.83 mg/mL (1.99 mM); Clear solution
-
3.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 0.83 mg/mL (1.99 mM); Clear solution
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4.
Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)
Solubility: ≥ 0.4 mg/mL (0.96 mM); Clear solution