MPI-0479605
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.
MPI-0479605是MPS1的选择性和ATP竞争性抑制剂。对于其它120种激酶无显著抑制。在nocodazole处理的细胞中,MPI-0479605通过促进cyclin B和保全素(securing)的降解来抑制MPS1的功能。在过表达Mps1的HEK293T细胞中,MPI-0479605可以抑制MPS1磷酸化。MPI-0479605导致有丝分裂过程中A549细胞染色体分离的缺陷,破坏细胞分裂中期染色体对准的能力。除此之外,MPI-0479605可以使细胞周期显著延迟或停滞。在HCT-116细胞中,MPI-0479605导致细胞活力显著下降并最终导致细胞死亡,GI50值范围从30 nM到约100 nM。在肿瘤异种移植模型中,MPI-0479605具有一定的抗肿瘤作用。在HCT-116异种移植小鼠中,30mg/kg剂量的MPI-0479605引起了49%的肿瘤生长抑制(TGI)[1]。
参考文献:
[1] Tardif K D, Rogers A, Cassiano J, et al. Characterization of the cellular and antitumor effects of MPI-0479605, a small-molecule inhibitor of the mitotic kinase Mps1. Molecular cancer therapeutics, 2011, 10(12): 2267-2275.
Storage | Store at -20°C |
M.Wt | 407.51 |
Cas No. | 1246529-32-7 |
Formula | C22H29N7O |
Solubility | Soluble in DMSO |
SDF | Download SDF |
Canonical SMILES | CC1=C(C=CC(=C1)N2CCOCC2)NC3=NC4=C(C(=N3)NC5CCCCC5)NC=N4 |
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。 |
描述 | MPI-0479605是有丝分裂激酶MPS1的小分子抑制剂, IC50值为1.8 nM[1]。 | |||||
靶点 | Mps1 | |||||
IC50 | 1.8 nM |