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.
IC50: 0.004 to 0.013 mM for RSK1, 2, and 3.
LJI308 is a potent and selective inhibitor of RSK. The p90 ribosomal S6 kinase (RSK) comprises a family of serine/threonine kinase which is expressed in various human cancers. RSK is the cytosolic substrate for the ERK (extracellular sianal-regulated kinase), involved in direct regulation of cell survival, proliferation, and cell polarity. Previous studies have demonstrated that RSK pathway is important for the growth and proliferation of cancer stem cells [1,2].
The IC50 values of LJI308 against RSK1, 2, and 3 were about 0.004 - 0.013 mmol/L. 10 μM LJI308 could bind to nearly 100% of the RSK2. LJI308 bound the N-termini of RSK1, RSK3, and RSK4 to a similar extent. LJI308 inhibited S6K1 with an IC50 of 0.8 mM. In both MDA-MB-231 and H358 cell lines, 1 μM and 10 μM LJI308 exihibited an inhibitory effect on colony formation and cell growth with a different sensitivity . In HTRY-LT cell lines, treating with LJI308 (1-10 µM) after 4 or 8 days decreased the cell viability by up to 90%; while little to no effect was observed in the non-tumorigenic HTRZ cells .
LJI308, the RSK inhibitor, could be used in combination with conventional chemotherapy to overcome the drug resistance and improve survival in patients with the triple-negative breast cancer (TNBC) .
Aronchik I, Appleton B A, Basham S E, et al. Novel potent and selective inhibitors of p90 ribosomal S6 kinase reveal the heterogeneity of RSK function in MAPK-driven cancers[J]. Molecular Cancer Research, 2014, 12(5): 803-812.
Davies A H, Reipas K, Hu K, et al. Inhibition of RSK with the novel small-molecule inhibitor LJI308 overcomes chemoresistance by eliminating cancer stem cells[J]. Oncotarget, 2015, 6(24): 20570.
|Physical Appearance||A crystalline solid|
|Storage||Store at -20°C|
|Solubility||Soluble in DMSO|
|Shipping Condition||Evaluation sample solution: ship with blue ice. All other available sizes: 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.|