AZ-6102

AZ-6102 is a potent TNKS1/2 inhibitor (Tankyrase) that displays >100-fold selectivity against other poly (ADP-ribose) polymerase (PARP) family enzymes and inhibits Wnt pathway with IC₅₀ value of 5 nM in DLD-1 cells. Inhibition of the PARP catalytic domain of the tankyrases is known to inhibit the Wnt pathway via increased stabilization of Axin. Wnt pathway plays important role in cancer, tissue homeostasis; germline mutations of various Wnt pathway components as Axin can lead to oncogenesis.