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是可逆的、强效的和选择性的MST1/2抑制剂,IC50值分别为71.1 ± 12.9 nM和38.1 ± 6.9 nM [1]。
MST1和MST2是Hippo级联信号的关键组成部分,在组织再生、干细胞自我更新和器官大小控制中发挥重要作用[1]。
XMU-MP-1是MST1/2的一种有效选择性以及ATP竞争性抑制剂。在基于ELISA的高通量筛选实验中,10 μM的XMU-MP-1抑制50%以上的MST2激酶活性,剂量依赖性地抑制MST2介导的MOB1磷酸化。在人肝癌HepG2细胞中,0.1至10 μM的XMU-MP-1剂量依赖性地降低内源性MOB1、LATS1/2和YAP的磷酸化。此外,在各种细胞系中,包括人骨肉瘤细胞系(U2OS)、人结肠直肠腺癌(SW480)和人多形性肝细胞癌(SNU-423)中,XMU-MP-1抑制H2O2刺激的MOB1磷酸化和MST1/2的自磷酸化[1]。
在野生型小鼠中,在切除三分之二肝脏之前,每天使用XMU-MP-1处理一次,治疗7天,XMU-MP-1显著降低MOB1和YAP的磷酸化水平。部分肝切除后,XMU-MP-1大大提高肝再生能力。在CCl4诱导的肝慢性损伤小鼠中,1 mg/kg剂量的XMU-MP-1处理引起少量胶原沉积,这意味着XMU-MP-1能够部分挽救纤维化[1]。
参考文献:
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 | ≥41.6 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH |
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 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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