2061980-01-4
XMU-MP-1
CAS: 2061980-01-4
Molecular Formula: C17H16N6O3S2
2061980-01-4 - Names and Identifiers
2061980-01-4 - Physico-chemical Properties
| Molecular Formula | C17H16N6O3S2 |
| Molar Mass | 416.48 |
| Density | 1.523±0.06 g/cm3(Predicted) |
| Boling Point | 714.8±70.0 °C(Predicted) |
| Solubility | DMSO: ≥ 30 mg/mL |
| Appearance | powder |
| Color | white to beige |
| pKa | 9.77±0.12(Predicted) |
| Storage Condition | -20°C |
| In vitro study | XMU-MP-1 inhibits MST1/2 activity and is therefore capable of activating the downstream effector molecule Yap protein and promoting cell growth. XMU-MP-1 can inhibit the phosphorylation of MOB1 in a dose dependent manner. In addition, with the increase of ATP concentration, the IC50 value of XMU-MP-1 to MST1/2 increased in proportion, and the inhibition of MST2 mediated MOB1 phosphorylation decreased. When the concentration was 0.1-10 μm, XMU-MP-1 could reduce the phosphorylation of endogenous MOB1, LATS1/2, YAP in HepG2 cells in a dose-dependent manner. Similarly, XMU-MP-1 were treated in a variety of cell lines (including mouse macrophage-like cells RAW264.7, human osteosarcoma cells U2OS, human colon cancer cells SW480, immortalized human retinal pigment epithelial cells RPE1, human pleomorphic hepatocellular carcinoma cells SNU-423, HepG2 and mouse primary hepatocytes) can inhibit the phosphorylation of MOB1 and MST1/2 caused by H202 without affecting the phosphorylation of JNK. XMU-MP-1 treatment can increase the nuclear localization of YAP. |
| In vivo study | Intraperitoneal injection of 1-3 mg/kg of XMU-MP-1 into the mouse model of acute/chronic liver injury, XMU-MP-1 has good pharmacokinetics in vivo, can improve the intestinal tract, liver repair and regeneration in mice. In rats, the Pharmacokinetics is also very favorable, with a half-life of 1.2 hours and a bioavailability of 39.5%. The highest levels of MOB1 and YAP phosphorylation were reached 1.5-6 hours after I. P. Injection of 1 mg/kg at XMU-MP-1. XMU-MP-1 can protect mice from DSS-induced colitis and reduce chronic liver injury. |
2061980-01-4 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.401 ml | 12.005 ml | 24.011 ml |
| 5 mM | 0.48 ml | 2.401 ml | 4.802 ml |
| 10 mM | 0.24 ml | 1.201 ml | 2.401 ml |
| 5 mM | 0.048 ml | 0.24 ml | 0.48 ml |
Last Update：2024-01-02 23:10:35
2061980-01-4 - Reference Information
| biological activity | XMU-MP-1 is an inhibitor of MST1/2, and the IC50 for inhibiting MST1 and MST2 is 71.1±12.9 nM and 38.1±6.9 nM respectively. |
| target | TargetValue MST2 (Cell-free assay) 38.1 nM MST1 (Cell-free assay) 71.1 nM |
| Target | Value |
| MST2 (Cell-free assay) | 38.1 nM |
| MST1 (Cell-free assay) | 71.1 nM |
| in vitro study | XMU-MP-1 inhibit MST1/2 activity, so it can activate downstream effector Yap protein and promote cell growth. XMU-MP-1 can inhibit phosphorylation of MOB1 in a dose-dependent manner. In addition, with the increase of ATP concentration, the IC50 value of XMU-MP-1 to MST1/2 increased proportionally, and the inhibition of MST2-mediated MOB1 phosphorylation decreased. When the concentration is 0.1-10 μM, XMU-MP-1 can reduce the phosphorylation of endogenous MOB1, LATS1/2, YAP in HepG2 cells in a dose-dependent manner. Similarly, XMU-MP-1 treatment was able to inhibit H202-induced phosphorylation of MOB1 and MST1/2 in a variety of cell lines, including mouse macrophage-like cells RAW264.7, human osteosarcoma cells U2OS, human colon cancer cells SW480, immortalized human retinal pigment epithelial cells RPE1, human pleomorphic hepatocellular carcinoma cells SNU-423, HepG2, and mouse primary hepatocytes, without affecting phosphorylation of JNK. XMU-MP-1 processing can increase the nuclear positioning of YAP. |
| in vivo study | intraperitoneal injection of 1-3 mg/kg XMU-MP-1 into mouse models of acute/chronic liver injury XMU-MP-1 have good pharmacokinetics in vivo and can improve the repair and regeneration of intestinal tract and liver in mice. In rats, its pharmacokinetics is also very favorable, with a half-life of 1.2 hours and a bioavailability of 39.5%. The highest levels of MOB1 and YAP phosphorylation were reached 1.5-6 hours after intraperitoneal injection of 1 mg/kg XMU-MP-1. XMU-MP-1 can protect mice from DSS-induced colitis and reduce chronic liver injury. |
Last Update：2024-04-09 21:04:16
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Spot supply
Product Name: XMU-MP-1 Visit Supplier Webpage Request for quotationCAS: 2061980-01-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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