Catalog No.: PC-20893Not For Human Use, Lab Use Only.
WNTinib is a multi-kinase inhibitor with specificity against β-catenin (CTNNB1) mutant hepatocellular carcinoma, harnesses the KIT/MAPK/EZH2 pathway, shows durable and selective transcriptional repression of mutant β-catenin/Wnt targets through nuclear translocation of the EZH2 transcriptional repressor.
WNTinib (APS-8-100-2) is a multi-kinase inhibitor with specificity against β-catenin (CTNNB1) mutant hepatocellular carcinoma, harnesses the KIT/MAPK/EZH2 pathway, shows durable and selective transcriptional repression of mutant β-catenin/Wnt targets through nuclear translocation of the EZH2 transcriptional repressor.
WNTinib reduces EZH2 phosphorylation to drive the suppression of essential gene networks in CTNNB1-mutated HCC.
WNTinib depends on EZH2 relocalization to chromatin for its activity in CTNNB1-mutated HCC.
WNTinib utilizes unique polypharmacology to regulate the EZH2–WNT axis.
KIT, BRAF and p38 kinases are critical anti-targets for WNTinib.
WNTinib outperforms clinical compounds across in vivo models of HCC.
