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.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
NMS-1286937 (NMS-P937) is a potent and selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 value of 2 nM .
PLK1 is a serine/threonine protein kinase and plays an important role in the cell cycle control machinery. PLK1 is involved in mitotic entry, bipolar mitotic spindle formation, centrosome duplication, transition from metaphase to anaphase, maintenance of genomic stability and cytokinesis .
NMS-1286937 is an orally bioavailable PLK1 inhibitor. In cell lines established from solid tumors, leukemias and lymphomas, NMS-P937 inhibited tumor cell proliferation. In A2780 cells, NMS-P937 caused a G2-M cell-cycle block. In the mitotic phase, NMS-P937 induced apoptotic death with misaligned chromosomes and an aberrant number of spindles poles . In human osteosarcoma (OS) cell lines, NMS-P937 inhibited migration and clonogenic ability of cell lines. In ABCB1-overexpressing, Doxorubicin (DX)-resistant cell lines, combination of NMS-P937 and DX reverted DX-resistance by inhibiting ABCB1 transport activity .
In Harlan nu/nu mice, NMS-P937 exhibited a good pharmacokinetic profile with low clearance, high AUC and Cmax, and acceptable oral bioavailability. In mice xenografted with human HCT116 colon adenocarcinoma cells, NMS-P937 (45 mg/kg) inhibited tumor growth by 83% and reduced body weight by 16% .
. Beria I, Bossi RT, Brasca MG, et al. NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor. Bioorg Med Chem Lett, 2011, 21(10): 2969-2974.
. Valsasina B, Beria I, Alli C, et al. NMS-P937, an orally available, specific small-molecule polo-like kinase 1 inhibitor with antitumor activity in solid and hematologic malignancies. Mol Cancer Ther, 2012, 11(4): 1006-1016.
. Sero V, Tavanti E, Vella S, et al. Targeting polo-like kinase 1 by NMS-P937 in osteosarcoma cell lines inhibits tumor cell growth and partially overcomes drug resistance. Invest New Drugs, 2014, 32(6): 1167-1180.
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||≥13.3mg/mL in DMSO|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|