Synonym
XMU-MP-1; XMU-MP1; XMU-MP 1; XMUMP-1; XMUMP1; XMUMP 1.
IUPAC/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
InChi Key
YRDHKIFCGOZTGD-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H16N6O3S2/c1-22-12-7-8-27-14(12)16(24)23(2)13-9-19-17(21-15(13)22)20-10-3-5-11(6-4-10)28(18,25)26/h3-9H,1-2H3,(H2,18,25,26)(H,19,20,21)
SMILES Code
O=S(C1=CC=C(NC2=NC=C3C(N(C)C(C=CS4)=C4C(N3C)=O)=N2)C=C1)(N)=O
Appearance
Light yellow to yellow solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
XMU-MP-1 is a reversible and selective MST1/2 inhibitor with IC50s of 71.1 and 38.1 nM, respectively.
In vitro activity:
To determine whether the Hippo signaling pathway mediated the biological functions of MST1 in BCa, the Hippo signaling pathway inhibitor, XMU-MP-1 (an inhibitor of MST1/2), was used to inhibit the function of the Hippo signaling pathway in BCa cells overexpressing MST1. RT-qPCR analysis demonstrated that the treatment of MST1-overexpressing cells with the inhibitor downregulated the expression levels of MST1 (Fig. 5A). The results of the CCK-8 and EdU incorporation assays revealed that the inhibited proliferative ability in the LV-MST1 group was partially restored in the LV-MST1 + XMU-MP-1 group (Fig. 5B and C). BCa cell migration was analyzed using wound healing assays; the results revealed that cell migration was also significantly increased in the MST1 + XMU-MP-1 cell group compared with the LV-MST1 group (Fig. 5D). Finally, western blotting analysis was performed to analyze the expression levels of key proteins in the Hippo signaling pathway. The expression levels of LATS1 and Bax were significantly downregulated, while the expression levels of YAP, Bcl-2 and Ki-67 were significantly upregulated in the LV-MST1 + XMU-MP-1 group compared with the LV-MST1 group in both cell lines (Fig. 6A and B).
Reference: Mol Med Rep. 2021 May; 23(5): 383. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7986037/
In vivo activity:
XMU-MP-1 administration attenuated AngII-induced aortic medial destruction in the ascending mouse aorta. In agreement with previous studies, AngII-induced medial destruction was associated with the accumulation of CD68+ macrophages throughout the intralamellar spaces on the adventitial site of the vessel wall. The beneficial effect of XMU-MP-1 on the attenuation of elastin fiber destruction in the aortic media is mainly due to its effect on the suppression of AngII-induced matrix metalloproteinases-2 (MMP2) production by infiltrated macrophages in the ascending aorta. In support, present data clearly suggested that XMU-MP-1 administration had no effect on AngII-induced macrophage infiltration into the ascending aortic medial layer or the total number of nuclei in the ascending aortic media, whereas it preserved or protected AngII-induced aortic medial destruction. These data suggest that XMU-MP-1 may exert its beneficial effect by suppressing MMP production or secretion by infiltrated macrophages into the aortic media.
Reference: Circ Rep. 2021 May 10; 3(5): 259–266. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8099673/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
33.9 |
81.33 |
| Ethanol |
1.3 |
3.00 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
416.47
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Jin X, Zhu L, Xiao S, Cui Z, Tang J, Yu J, Xie M. MST1 inhibits the progression of breast cancer by regulating the Hippo signaling pathway and may serve as a prognostic biomarker. Mol Med Rep. 2021 May;23(5):383. doi: 10.3892/mmr.2021.12022. Epub 2021 Mar 24. PMID: 33760220; PMCID: PMC7986037.
2. Tian Y, Song H, Qin W, Ding Z, Zhang Y, Shan W, Jin D. Mammalian STE20-Like Kinase 2 Promotes Lipopolysaccharides-Mediated Cardiomyocyte Inflammation and Apoptosis by Enhancing Mitochondrial Fission. Front Physiol. 2020 Aug 6;11:897. doi: 10.3389/fphys.2020.00897. PMID: 32848850; PMCID: PMC7424023.
3. Okuyama M, Jiang W, Yang L, Subramanian V. Mst1/2 Kinases Inhibitor, XMU-MP-1, Attenuates Angiotensin II-Induced Ascending Aortic Expansion in Hypercholesterolemic Mice. Circ Rep. 2021 Apr 20;3(5):259-266. doi: 10.1253/circrep.CR-20-0104. PMID: 34007939; PMCID: PMC8099673.
4. Faizah Z, Amanda B, Ashari FY, Triastuti E, Oxtoby R, Rahaju AS, Aziz MA, Lusida MI, Oceandy D. Treatment with Mammalian Ste-20-like Kinase 1/2 (MST1/2) Inhibitor XMU-MP-1 Improves Glucose Tolerance in Streptozotocin-Induced Diabetes Mice. Molecules. 2020 Sep 24;25(19):4381. doi: 10.3390/molecules25194381. PMID: 32987643; PMCID: PMC7582334.
In vitro protocol:
1. Jin X, Zhu L, Xiao S, Cui Z, Tang J, Yu J, Xie M. MST1 inhibits the progression of breast cancer by regulating the Hippo signaling pathway and may serve as a prognostic biomarker. Mol Med Rep. 2021 May;23(5):383. doi: 10.3892/mmr.2021.12022. Epub 2021 Mar 24. PMID: 33760220; PMCID: PMC7986037.
2. Tian Y, Song H, Qin W, Ding Z, Zhang Y, Shan W, Jin D. Mammalian STE20-Like Kinase 2 Promotes Lipopolysaccharides-Mediated Cardiomyocyte Inflammation and Apoptosis by Enhancing Mitochondrial Fission. Front Physiol. 2020 Aug 6;11:897. doi: 10.3389/fphys.2020.00897. PMID: 32848850; PMCID: PMC7424023.
In vivo protocol:
1. Okuyama M, Jiang W, Yang L, Subramanian V. Mst1/2 Kinases Inhibitor, XMU-MP-1, Attenuates Angiotensin II-Induced Ascending Aortic Expansion in Hypercholesterolemic Mice. Circ Rep. 2021 Apr 20;3(5):259-266. doi: 10.1253/circrep.CR-20-0104. PMID: 34007939; PMCID: PMC8099673.
2. Faizah Z, Amanda B, Ashari FY, Triastuti E, Oxtoby R, Rahaju AS, Aziz MA, Lusida MI, Oceandy D. Treatment with Mammalian Ste-20-like Kinase 1/2 (MST1/2) Inhibitor XMU-MP-1 Improves Glucose Tolerance in Streptozotocin-Induced Diabetes Mice. Molecules. 2020 Sep 24;25(19):4381. doi: 10.3390/molecules25194381. PMID: 32987643; PMCID: PMC7582334.
1: Fan F, He Z, Kong LL, Chen Q, Yuan Q, Zhang S, Ye J, Liu H, Sun X, Geng J, Yuan L, Hong L, Xiao C, Zhang W, Sun X, Li Y, Wang P, Huang L, Wu X, Ji Z, Wu Q, Xia NS, Gray NS, Chen L, Yun CH, Deng X, Zhou D. Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration. Sci Transl Med. 2016 Aug 17;8(352):352ra108. doi: 10.1126/scitranslmed.aaf2304. PubMed PMID: 27535619.
