RGNCY-0127 (8430 SIX1/EYA2 complex inhibitor )

Compound 8430 reduces SIX1/EYA2 interaction which is involved in breast cancer metastasis.  8430 was shown to partially reverse transcriptional and metabolic profiles mediated by SIX1 over-expression and reversed SIX1 induced TGF-Beta signalling and EMT.  In vivo, 8430 was well tolerated in mice and significantly suppressed breast cancer-associated metastasis without altering primary tumor growth.  This is the first demonstration of the pharmacological inhibition of the SIX1/EYA2 complex is sufficient to inhibit cancer metastasis.  Thus, 8430 is a novel compound that effectively reverses EMT phenotypes suppressing breast cancer metastasis.

Systematic Name:  N-(4-methoxy-3-(morpholinosulfonyl)phenyl)-3-(1H-pyrrol-1-yl)benzamide

SMILES:  COC(C=CC(NC(C1=CC(N2C=CC=C2)=CC=C1)=O)=C3)=C3S(N4CCOCC4)(=O)=O

Formula:  C22H23N3O5S

Mol Wt: 441.50