RGNCY-0116 (CA3 YAP1 inhibitor)

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CA3 is a novel compound with significant inhibitory activity on YAP1 (Hippo co-activator Yes-associated protein 1)/Tead transcriptional activity and demonstrates a potent inhibitory effect on EAC cell growth.  This is particularly evident in high YAP1 expressing EAC cells in vitro and in vivo.  YAP1 is a major mediator of cancer stem cell (CSC) properties, tumor progression and therapy resistance.  Radiation resistant cells acquire strong CSC properties and aggressive phenotype.  CA3 can effectively suppress these phenotypes by inhibiting proliferation, inducing apoptosis, reducing tumor sphere formation and reducing the fraction of ALDH1+ cells.  The combination of.CA3 with 5-FU, results in a synergistic inhibitory effect on EAC cell growth in high YAP1 EAC cells.

Systematic Name: (E)-2-(cyclohexylsulfonyl)-7-(piperidin-1-ylsulfonyl)-9H-fluoren-9-one oxime

SMILES:  O=S(N1CCCCC1)(C2=CC(/C(C3=C4C=CC(S(C5CCCCC5)(=O)=O)=C3)=N/O)=C4C=C2)=O

Formula:   C24H28N2O5S2

Mol Wt:  488.62

PMID:  29167315