Molecular Weight(MW): 587.67
SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 values of 4 nM and 1 nM in cell-free assay, respectively, And show robust efficacy in RAS- or BRAF-mutant cancer cells.
Cited by 10 Publications
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293T cells were transfected with Flag-WT-FBW7. Thirty hours post transfection, cells were pretreated with MG132 and various MEK/ERK inhibitors overnight before harvesting. FBW7 phosphorylation status was examined by immunoblot analysis after immunoprecipitation.
Cell Research, 2015, 25: 561-573. SCH772984 purchased from Selleck.
ERK1/2 influences the effects of TGF-β1 on Cdk5 and Bax in PC12 cells. A. Original western blot showing the level of Cdk5 and respective Actin in PC12 cells with TGF-β1 (40 ng/ml) treatment in the presence of SCH772984(1 μM) and LY294002(1.5 μM) for 2 h. B. Arithmetic means ± SEM (n = 4) of Cdk5 protein abundance in PC12 cells with TGF-β1 treatment in the presence of SCH772984(1 μM) and LY294002(1.5 μM) for 2 h. C. Original western blot showing the level of Bax and respective Actin in PC12 cells with TGF-β1 (40 ng/ml) treatment in the presence of SCH772984(1 μM) for 2 h. D. Arithmetic means ± SEM (n = 4) of Bax protein abundance in PC12 cells with TGF-β1 treatment in the presence of SCH772984(1 μM) for 2 h. **(p < 0.01), ***(p < 0.001) indicate statistically significant difference.
Biochem Biophys Res Commun, 2017.. SCH772984 purchased from Selleck.
Purity & Quality Control
Choose Selective ERK Inhibitors
|Description||SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 values of 4 nM and 1 nM in cell-free assay, respectively, And show robust efficacy in RAS- or BRAF-mutant cancer cells.|
|Features||Does not directly inhibit MEK1, MEK2, BRAF, or CRAF enzyme activity.|
SCH772984 is a novel, selective and ATP competitive inhibitor of ERK1/2. SCH772984 inhibits phosphorylation of the ERK substrate p90 ribosomal S6 kinase (T359/S363 phospho-RSK) in a dose-dependent manner. SCH772984 also inhibits phosphorylation of residues in the activation loop of ERK itself. SCH772984 demonstrates EC50 values <500 nM in approximately 88% and 49% of BRAF-mutant or RAS-mutant tumor lines, respectively. Importantly, SCH772984 effectively inhibited MAPK signaling and cell proliferation in tumor cells resistant to concurrent treatment with BRAF and MEK inhibitors. 
|In vivo||SCH772984 induces tumor regressions in xenograft models at tolerated doses. SCH772984 effectively inhibites MAPK signaling and cell proliferation in BRAF or MEK inhibitor resistant models. |
ERK2 IMAP enzymatic assay:SCH772984 is tested in 8 point dilution curves in duplicate against purified ERK2 or ERK1. The enzyme is added to the reaction plate. and incubated with the compound before adding a solution of substrate peptide and ATP. 14μl of diluted enzyme (0.3ng active ERK2 per reaction) is added to each well of a 384-well plate. The plates are gently shaken to mix the reagents and incubated for 45 minutes at room temperature. The reaction is stopped with 60μl of IMAP Binding Solution (1:2200 dilutions of IMAP beads in 1X Binding Buffer). The plates are incubated at room temperature for an additional 0.5 hours to allow complete binding of phosphopeptides to the IMAP beads. Plates are read on the LJL Analyst.
|In vitro||DMSO||0.1 mg/mL warmed (0.17 mM)|
|In vivo||Add solvents individually and in order:
5% DMSO+30% PEG 300+ddH2O
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