RGNCY-0069 (BHX Wnt/β-catenin inhibitor)

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BHX exhibits potent anti-tumor activity by blocking the Wnt/β-catenin signalling pathway.  BHX suppresses MDA-MB-231 breast cancer cell viability and colony formation and induces apoptosis and G0/G1 phase arrest.  BHX also inhibits cell migration and invasion associated with increased E-cadherin mRNA and protein expression and down regulation of SNAIL and vimentin.  BHX also induces the generation of intracellular ROS and decreased β-catenin protein and mRNA expression.  BHX suppresses the growth of MDA-MB-231 xenograft tumors in nude mice.  The pharmacokinetic parameters of BHX have also been determined.  

SMILE: OC1=CC=C(CNC([C@@H]2N(C3=CC=CC=C3)N=C(C4=CC=CC=C4)

[C@H]2C5=CC=CC=C5)=O)C=C1

Systematic Name: (4S,5R)-N-(4-hydroxybenzyl)-1,3,4-triphenyl-4,5-dihydro-1H-pyrazole-5-carboxamide

Molecular Weight: 447.54

Formula:  C29H25N3O2

PMID: 28831201