8430 SIX1/EYA2 complex inhibitor (RGNCY-0127)
Per 10 mg
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
Zhou H et al. Identification of a Small-Molecule Inhibitor That Disrupts the SIX1/EYA2 Complex, EMT, and Metastasis. Cancer Res (2020) Jun 15;80(12):2689-2702.
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