NCB-0846 is a novel, orally small-molecule Wnt inhibitor that inhibits TNIK (TRAF2 and NCK-Interacting Kinase) with an IC50 value of 21 nM.
PNU-75654 disrupts the Wnt signaling pathway via inhibition of the interaction (KD50=450 nM) between β-catenin and Tcf4.
LF3 is a specific inhibitor of canonical Wnt signaling by disrupting the interaction between β-catenin and TCF4 with an IC50 less than 2 μM.
Amcasertib (BBI503), a first-in-class cancer stemness kinase inhibitor, is claimed to inhibit Nanog and other CSC pathways by targeting kinases with potential anticancer activity.
LYN-1604 is a potential ULK1 agonist with IC50 of 1.66 μM against MDA-MB-231 cells and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants.
GNF-6231 is a potent, orally active and selective Porcupine inhibitor with IC50 of 0.8 nM.
IWP-O1 is a porcn inhibitor with an EC50 value of 80 pM in a cultured cell reporter assay of Wnt signaling and effectively suppresses the phosphorylation of Dvl2/3 in HeLa cells.
iCRT3 is an antagonist of Wnt/β-catenin signaling with an IC50 of 8.2 nM in the Wnt responsive STF16-luc reporter assays.