tankyrase-in-2

Tankyrase-IN-2 is a selective, potent and orally active inhibitor of tankyrase with IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively

OM-153 is a potent inhibitor of tankyrase, acting on tankyrase 1 (IC50: 13 nM) and tankyrase 2 (IC50: 2 nM), and inhibiting WNT β-linked protein signaling and proliferation in COLO 320DM.

JPI 547, also known as NOV 1402, is an oral inhibitor of PARP 1 2 and Tankyrase 1 2. JPI-547 demonstrated anti-tumor activity in BRCA-deficient xenograft models as a single-agent and in combination with chemotherapy and immune checkpoint inhibitors.

AZ0108 is an orally bioavailable, potent PARP1,2,6 inhibitor that potently inhibits centrosome clustering and is suitable for in vivo efficacy and tolerability studies. AZ0108 has been utilized as in vitro tools and in vivo probes to investigate the biological consequences of inhibiting centrosome clustering through PARP enzymes. AZ0108 is more selective in its enzyme inhibition profile and effects on cellular pathways and phenotypes. Specifically, AZ0108 inhibits PARPs 1, 2, and 6 with approximately 100-fold selectivity against PARP3 and TNKS1. Consistent with this lack of potencytowards tankyrase, AZ0108 is not active in a DLD-1 Wnt luciferase reporter assay.

TNKS1 2-IN-1 is a potent tankyrase (TNKS1 2) inhibitor with pIC50 values ranging from 7.1 to 8.2, used in research targeting cancer, fibrosis, and other hyperproliferative diseases.