JW74

JW74 is a small molecule tankyrase (TNKS) inhibitor that functions as an antagonist of the Wnt/β-catenin signaling pathway. It acts by inhibiting the poly(ADP-ribosyl)ation activity of tankyrases 1 and 2, which leads to the stabilization of AXIN2, a critical component of the β-catenin destruction complex. This stabilization promotes the degradation of cytoplasmic β-catenin, thereby inhibiting the transcription of Wnt target genes involved in cell proliferation, survival, and metastasis. Research has explored JW74's potential in various cancers, including cervical and colorectal cancer, where it has been studied for its ability to reduce cell viability and invasion. However, studies indicate that JW74-mediated β-catenin inhibition can lead to a compensatory increase in PARP-1 expression, which may limit its effectiveness in sensitizing cancer cells to DNA-damaging agents like cisplatin. JW74 is primarily utilized as a chemical probe in laboratory research.

Other names

4-[4-(4-Methoxyphenyl)-5-[[[3-(4-methylphenyl)-1,2,4-oxadiazol-5-yl]methyl]thio]-4H-1,2,4-triazol-3-yl]pyridine