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Chemical Structure : WNTinib
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.
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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 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.
| M.Wt | 498.39 | |
| Formula | C22H16F6N4O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Rialdi A, et al. Nat Cancer. 2023 Aug 3. doi: 10.1038/s43018-023-00609-9.
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