RGNCY-0050 ((S)-27 Wnt inhibitor)

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(S)-27 is a Porcupine (membrane-bound O-acetyltransferase that palmitoleates the Wnt proteins) secretion inhibitor  with nanomolar activity and excellent bioavailability.  It demonstrated in vivo efficacy in a Wnt driven murine tumor model.  (S)-27 and its enantiomers show different activity in a reporter assay suggesting that this compound maybe useful for mode of action studies on the Porcupine O-acetyltransferase. STF3A IC50=0.001mM, 



Systematic Name: (S)-N-([3,3'-bipyridin]-6-yl)-2-((6-(1-methyl-1H-pyrazol-5-yl)pyridin-3-yl)amino)propanamide

SMILES: CN1N=CC=C1C2=NC=C(N[C@@H](C)C(NC3=NC=C(C4=CN=CC=C4)C=C3)=O)C=C2

Formula: C22H21N7O

Mol Wt: 399.46

PMID: 26110200




Tags: Cancer, Wnt, Tumor, RGNCY-0050, S-27, Porcupine