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.
Ro3280 is a selective inhibitor of PLK1 with IC50 value of 3 nM .
Polo-like kinase 1 (PLK1) is an enzyme and plays an important role in regulating cell cycles as an early trigger for G2/M phase transition. It has been shown that PLK1 is over-expressed in a variety of cancer cells and thus is regarded as a promising target for cancer drugs .
When tested with a panel of acute leukemia cell lines, Ro3280 showed inhibitory function on U937, HL 60, NB4, K562, MV4-11, and CCRF with IC50 value of 186 nM, 175 nM, 74 nM, 797 nM, 120 nM, and 162 nM, respectively. It was interesting to notice that ALL cells (35.49-110.76 nM) were more sensitive to Ro3280 compared with AML cells (IC50, 52.80-147.50 nM). Further, it was showed that Ro3280 treatment decreased cell viability, induced apoptosis and disrupted cell cycle . In H82 (lung cancer), HT-29 (colon cancer), MDA-MB-468 (breast cancer), PC3 (prostate cancer), and A375 (cutaneum carcinoma), Ro3280 treatment inhibited PLK1 with the IC50 was 5 nM, 10 nM, 19 nM, 12 nM, and 70 nM, respectively .
In nude mice model with HT-29 cells subcutaneous xenograft, administration of Ro3280 caused significant anti-tumor activity with 78% reduction at the dose of 40 mg/kg, once a week and then completely regressed tumor when more drug and more frequent .
. Chen, S., et al., Identification of novel, potent and selective inhibitors of Polo-like kinase 1. Bioorg Med Chem Lett, 2012. 22(2): p. 1247-50.
. Czaplinski, S., et al., Polo-like kinase 1 inhibition sensitizes neuroblastoma cells for vinca alkaloid-induced apoptosis. Oncotarget, 2015.
. Wang, N.N., et al., Molecular targeting of the oncoprotein PLK1 in pediatric acute myeloid leukemia: RO3280, a novel PLK1 inhibitor, induces apoptosis in leukemia cells. Int J Mol Sci, 2015. 16(1): p. 1266-92.
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||≥27.2mg/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°C and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.|
|Description||RO3280 is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with an IC50 value of 3 nM.|