DEL-22379

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

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Code Description Colour Quality Level Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3575254 DEL-22379 white to beige 100 SIGMA-ALDRICH −20°C
£402.54 (exc VAT) per 25MG
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3575255 DEL-22379 white to beige 100 SIGMA-ALDRICH −20°C
£156.00 (exc VAT) per 5MG
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