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Description: DEL-22379 is a novel, potent, selective, and water-soluble ERK (extracellular signal-related kinase 2) dimerization inhibitor with potential antitumor activity. It inhibits ERK with an IC50 of 0.5 uM. Unregulated RAS-ERK signaling is observed in nearly 50% of human malignancies and thus is an excellent target for intervention by antineoplasticagents. DEL-22379 inhibits ERK dimerization without affecting ERK phosphorylation, forestalls tumorigenesis driven by RAS-ERK pathway oncogenes. DEL-22379 readily binds to ERK2 with a Kd estimated in the low micromolar range, though binding is detectable even at low nanomolar concentrations.
References: Cancer Cell. 2015 Aug 10; 28(2):170-82.
Chemical Name: (E)-N-(3-((5-methoxy-1H-indol-3-yl)methylene)-2-oxoindolin-5-yl)-3-(piperidin-1-yl)propanamide
InChi Key: INQUULPXCZAKMS-LPYMAVHISA-N
InChi Code: InChI=1S/C26H28N4O3/c1-33-19-6-8-23-20(15-19)17(16-27-23)13-22-21-14-18(5-7-24(21)29-26(22)32)28-25(31)9-12-30-10-3-2-4-11-30/h5-8, 13-16, 27H, 2-4, 9-12H2, 1H3, (H, 28, 31)(H, 29, 32)/b22-13+
SMILES Code: O=C(NC1=CC2=C(NC(/C2=C/C3=CNC4=C3C=C(OC)C=C4)=O)C=C1)CCN5CCCCC5
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