RGNCY-0069 (BHX Wnt/β-catenin inhibitor)
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.
Systematic Name: (4S,5R)-N-(4-hydroxybenzyl)-1,3,4-triphenyl-4,5-dihydro-1H-pyrazole-5-carboxamide
Molecular Weight: 447.54
Tags: Cancer, beta-catenin, migration, Wnt, breast cancer, Invasion, RGNCY-0069, BHX, vimentin