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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 (ref. 1).
Catalog NO: CT-SCH772
CAS NO: 942183-80-4
Mol. Formula: C33H33N9O2
MW: 587.7 (or refer to Certificate of Analysis, batch-specific)
** The ONLY Optically Pure Source. in vivo Quality Material. >99.5% Pure by Achiral and Chiral HPLCs. A single isomer (100% R-enantiomer, clinically active isomer) (Ref. 2). Bulk Stock! Same day shipping