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
Mol Wt: 441.50
Tags: Cancer, Apoptosis, small molecule, breast cancer, TGF, TGFB, TGF beta, RGNCY-0127, 8430, SIX1, EYA2