RGNCY-0097 (M36 p32 inhibitor)

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M36 is a unique pharmacophore of C1q and LyP-1 tumor homing peptide associating with p32.  Mitochondrial protein p32 is a validated thearpaeutic target of cancer and is over-expressed in glioma.  M36 binds directly to p32 and inhibits LyP-1 association with p32 in vitro.  Furthermore, M36 effectively inhibits the growth of p32 over-expressed glioma cells and sensitises the cell to glucose depletion.  M36 is worthy of further development as a potent and highly selective brain penetrant targeting mitochondrial p32.

Systematic Name: 1,1'-(propane-1,3-diyl)bis(3-(3-(4,5-dihydro-1H-imidazol-2-yl)phenyl)urea)

SMILES: O=C(NCCCNC(NC1=CC(C2=NCCN2)=CC=C1)=O)NC3=CC=CC(C4=NCCN4)=C3

Formula:  C23H28N8O2

Mol Wt:  448.53

PMID:  21885916