XMU-MP-1
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
XMU-MP-1 is a reversible, potent and selective inhibitor of MST1/2 with IC50 values of 71.1 ± 12.9 nM and 38.1 ± 6.9 nM, respectively [1].
The Sterile 20-like kinases MST1 and MST2 are key components of the Hippo signaling cascade that play an important role in tissue regeneration, stem cell self-renewal and organ size control [1].
XMU-MP-1 is a potent, selective and ATP-competitive MST1/2 inhibitor. In ELISA-based high-throughput screening assay, XMU-MP-1 at 10 μM inhibited MST2 kinase activity by more than 50% and dose-dependently inhibited the phosphorylation of MOB1 mediated by MST2. In human liver carcinoma (HepG2) cells, XMU-MP-1 (0.1 to 10 μM) dose-dependently reduced the phosphorylation of endogenous MOB1, LATS1/2, and YAP. Also, in a variety of cell lines, including human osteosarcoma (U2OS), human colorectal adenocarcinoma (SW480) and human pleomorphic hepatocellular carcinoma (SNU-423), XMU-MP-1 inhibited H2O2-stimulated MOB1 phosphorylation and MST1/2 autophosphorylation [1].
In wild-type mice, treatment with XMU-MP-1 once a day before a two-thirds partial hepatectomy followed by daily treatment for 7 days. XMU-MP-1 significantly reduced the phosphorylation levels of MOB1 and YAP. After partial hepatectomy, XMU-MP-1 substantially increased liver regeneration. In CCl4-induced liver chronic injury mice treatment with XMU-MP-1 (1 mg/kg) had a small amount of collagen deposition, suggesting XMU-MP-1 is capable of partially rescuing fibrosis [1].
Reference:
1. Fuqin Fan, Zhixiang He, Lu-Lu Kong, et al. Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration. Science Translational Medicine 17 Aug 2016: Vol. 8, Issue 352, pp. 352ra108.
- 1. Yuan L, Liu X, et al. "Optimized HepaRG is a suitable cell source to generate the human liver chimeric mouse model for the chronic hepatitis B virus infection." Emerg Microbes Infect. 2018 Aug 10;7(1):144. PMID:30097574
- 2. Yuan L, Liu X, et al. "A Chimeric Humanized Mouse Model by Engrafting the Human Induced Pluripotent Stem Cell-Derived Hepatocyte-Like Cell for the Chronic Hepatitis B Virus Infection." Front Microbiol. 2018 May 8;9:908. PMID:29867819
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 416.48 |
| Cas No. | 2061980-01-4 |
| Formula | C17H16N6O3S2 |
| Solubility | ≥41.6mg/mL in DMSO with gentle warming |
| Chemical Name | 4-((5,10-dimethyl-6-oxo-6,10-dihydro-5H-pyrimido[5,4-b]thieno[3,2-e][1,4]diazepin-2-yl)amino)benzenesulfonamide |
| SDF | Download SDF |
| Canonical SMILES | O=S(C1=CC=C(NC2=NC=C3C(N(C)C(C=CS4)=C4C(N3C)=O)=N2)C=C1)(N)=O |
| Shipping Condition | Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request. |
| General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months. |
Quality Control & MSDS
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Chemical structure
Related Biological Data
Related Biological Data
