tankyrase-2

RK-287107 is an effective and specific inhibitor of tankyrase (IC50s: 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively).

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

JW 55 (JW55) is an effective and selective β-catenin signaling pathway inhibitor, works by inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2).

TNKS-2-IN-3 (Compound 5) is a selective and competitive inhibitor of Tankyrase 2 (TNKS2), with an IC50 value of 0.3 nM. It exhibits over 20-fold selectivity for TNKS2 compared to TNKS1 and more than 100-fold selectivity over PARP1/2. By inhibiting TNKS2-mediated ADP ribosylation, TNKS-2-IN-3 stabilizes axin and suppresses the Wnt/β-catenin pathway, demonstrating antiproliferative activity in colorectal cancer cells. TNKS-2-IN-3 holds potential for research in solid tumors with aberrant Wnt pathway activation, such as colorectal cancer.

WIKI4 is a potent inhibitor of Wnt/β-catenin signaling and tankyrase 2 (TNKS2).

CAY10753 is an inhibitor of tankyrase 2 (TNKS2; IC50= 0.3 nM).1It is selective for TNKS2 over TNKS1 (IC50= 6.1 nM), as well as poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 89.6 and 37.8 nM, respectively). CAY10753 inhibits proliferation of DLD-1 colorectal cancer cells when used at a concentration of 1 μM. 1.Tomassi, S., Pfahler, J., Mautone, N., et al.From PARP1 to TNKS2 inhibition: A structure-based approachMed. Chem. Lett.(2020)

MSC2504877 is an inhibitor of tankyrase and enhances the effects of clinical CDK4/6 inhibitors. MSC2504877 suppresses the upregulation of Cyclin D2 and Cyclin E2 caused by palbociclib and enhances the suppression of phospho-Rb.

OM-1700 is a potent inhibitor of tankyrase, acting on tankyrase 1 (IC50: 127 nM) and tankyrase 2 (IC50: 14 nM). OM-1700 inhibits the growth of colon cancer cell lines and inhibits COLO 320DM cells (GI50: 650 nM).

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.

G244-LM, a potent and specific inhibitor of tankyrase 1/2, effectively inhibits Wnt signaling.