DEL-22379
Biochem/physiol Actions
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.).
Packaging
5, 25 mg in glass bottle
| Colour | white to beige |
|---|---|
| Quality Level | 100 |
| Manufacturer | SIGMA-ALDRICH |
| Storage Temp. | −20°C |
| Solubility | DMSO: 10 mg/mL, clear |
| Form | powder |
| Assay | ≥98% (HPLC) |
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