DEL-22379 is a cell-permeable 3-arylidene-2-oxindole derivative that inhibits the dimerization of ERK (IC50 = 500 nM) via directly binding to its dimerization interface. DEL-22379 promotes the transactivation of ELK, and prevents the EGF-induced phosphorylation of the cytoplasmic kinase RSK1 in HEK293 cells (IC50 = 500 nM). DEL-22379 induces apoptosis in various cancer cells harboring RAS-ERK pathway oncogenes (IC50 = 150 – 400 nM). DEL-22379 blocks tumor progression and metastasis in multiple xenograft models such as A375 (BRAF mutant), HCT116 (KRAS mutant) and colorectal cancer patient-derived xenografts (15 mg/kg, i.p. b.i.d.).
DEL-22379 is a cell-permeable 3-arylidene-2-oxindole derivative that inhibits the dimerization of ERK via directly binding to its dimerization interface.
NOTE: Both the cell line and DNA from the cell line may be available for this product. Please choose -1VL or VIAL for cells, or -DNA-5UG for DNA, 98050130, human breast, Epithelial-like
