RGNCY-0108 (SR18662 KLF5 inhibitor)

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SR1866 is an inhibitor of Kruppel-like factor 5 (KLF5), a zinc finger transcription factor overexpressed in human colorectal cancer (CRC) and overexpression is associated with aggressive cancer development and progression.  SR1866 significantly reduces growth and proliferation of CRC cells and showed efficacy in reducing viability of multiple CRC cell lines.  SR18662 treatment results in an increase in apoptotic cells and reduces the expression of cyclins and components of MAPK and WNT signalling pathways.  A dose-dependent inhibition of xenograft growth in mice was observed following SR18662 treatment. 

Systematic Name: (E)-3-(3,4-dichlorophenyl)-N-(2-(4-(methylsulfonyl)piperazin-1-yl)-2-oxoethyl)acrylamide

SMILES:  ClC1=C(Cl)C=C(/C=C/C(NCC(N2CCN(S(C)(=O)=O)CC2)=O)=O)C=C1

Formula:   C16H19Cl2N3O4S

Mol Wt:  420.31

PMID:  31358661