Extracellular signal regulated kinase (ERK) is a pivotal enzyme in the pathway downstream of Ras, Raf, and MEK, acting as a central link between multiple signaling pathways. SCH772984 is a potent, specific and ATP competitive inhibitor of ERK1 and ERK2 with IC50s at low nMs. It inhibits phosphorylation of the ERK substrate p90 ribosomal S6 kinase (T359/S363 phospho-RSK) in a dose-dependent manner, and also inhibits phosphorylation of residues in the activation loop of ERK itself. More importantly, it effectively inhibits MAPK signaling and cell proliferation in BRAF or MEK inhibitor-resistant models as well as in tumor cells resistant to concurrent treatment with BRAF and MEK inhibitors.

KEYWORDS: SCH772984 hydrochloride | Supplier | ERK1 and ERK2 inhibitor | SCH-772984 | SCH 772984 | SCH984 | SCH 984 | CT-SCH772 | CAS [N.A.] | [942183-80-4] | MAPK | ERK | Inhibitor | Enzymes