| References: |
DEL-22379 is an ERK dimerization inhibitor with IC50 of 0.5 μM.
in vitro: DEL-22379 inhibits ERK dimerization without affecting its
phosphorylation. DEL-22379 blocks proliferation of tumor cells harboring RASERK pathway oncogenes. Pretreating cells with DEL-22379 inhibits EGF-stimulated RSK1 phosphorylation, with estimated IC50 values of 500 nM for DEL-22379.
in vivo: In animal tumor models, DEL-22379 induces apoptosis,
preventing tumor progression.DEL-22379 abolishes EGF-induced co-immunoprecipitation of ectopic ERK2 molecules tagged with hemagglutinin (HA) or FLAG epitopes, with an estimated half-maximal inhibitory concentration (IC50) of 0.5 uM. |
