Low-molecular-weight kinase inhibitor of MAP-kinase interacting kinase-1 (MNK1) and MNK2 (IC50 values are 0.87 and 1.6 μM, respectively). Inhibits a range of other kinases (IC50 values in μM shown in brackets) including: CKI (0.51) Aurora B (2.5) DYRK3 (3.2) SGK1( 2.7) BRSK2 (1.1) and Lck (2.5).
Store at +4°C. The product can be stored for up to 12 months.
Soluble in DMSO to 100 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
The application notes include recommended starting dilutions; optimal dilutions/concentrations should be determined by the end user.
Use at an assay dependent concentration.
Functional Studies - CGP 57380 (ab120365)
ab76256 staining eIF4E (phospho S209) in serum starved HEK193 cells treated with CGP 57380 (ab120365), by ICC/IF. Decrease in eIF4E (phospho S209) expression correlates with increased concentration of CGP 57380, as described in literature. The cells were incubated at 37°C for 1h in media containing different concentrations of ab120365 (CGP 57380) in DMSO, fixed with 100% methanol for 5 minutes at -20°C and blocked with PBS containing 10% goat serum, 0.3 M glycine, 1% BSA and 0.1% tween for 2h at room temperature. Staining of the treated cells with ab76256 (1/100 dilution) was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight 488 goat anti-rabbit polyclonal antibody (ab96899) at 1/250 dilution was used as the secondary antibody. Nuclei were counterstained with DAPI and are shown in blue.
Knauf U et al. Negative regulation of protein translation by mitogen-activated protein kinase-interacting kinases 1 and 2. Mol Cell Biol21:5500-11 (2001).
Read more (PubMed: 11463832) »
Tschopp C et al. Phosphorylation of eIF-4E on Ser 209 in response to mitogenic and inflammatory stimuli is faithfully detected by specific antibodies. Mol Cell Biol Res Commun3:205-211 (2000).
Read more (PubMed: 10891393) »