tankyrase-2

RK-287107 是一种有效且特异性的 tankyrase 抑制剂，可阻断结直肠癌细胞生长，对 tankyrase-1和 tankyrase-2的 IC50分别为 14.3 和 10.6 nM。

MSC2504877 是一种tankyrase 抑制剂，可增强临床CDK4 6 抑制剂的作用。 MSC2504877 抑制由 palbociclib 引起的 Cyclin D2 和 Cyclin E2 的上调，并增强对 phospho-Rb 的抑制。

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) 是一种有效且选择性的 β-catenin 信号通路抑制剂，通过抑制 tankyrase 1 和 tankyrase 2 (TNKS1 2) 的 PARP 结构域起作用。

WIKI4 是tankyrase 有效抑制剂，其对TNKS2的IC50值为 26 nM。它有效抑制Wnt β-catenin 信号传导，其EC50值为 75 nM。它通过抑制TNKS2的酶活性来介导其对Wnt β-catenin 信号传导的影响。它对 SCLC 细胞具有细胞毒性，其IC50值为 0.02 μM。

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)

OM-1700 是一种 tankyrase 的有效抑制剂，作用于 tankyrase 1 (IC50: 127 nM) 和 tankyrase 2 (IC50: 14 nM)。OM-1700 能够抑制结肠癌细胞系的生长，抑制 COLO 320DM 细胞 (GI50: 650 nM)。

OM-153 是 tankyrase 的有效抑制剂，能够作用于 tankyrase 1 (IC50: 13 nM) 和 tankyrase 2 (IC50: 2 nM)，且对 COLO 320DM 中的 WNT β-连环蛋白信号传导和增殖具有抑制作用。

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是一种针对tankyrase TNKS1 2的高效抑制剂，其pIC50值介于7.1至8.2之间。该化合物主要用于癌症、纤维化及其他高增殖性疾病的研究领域。

G244-LM 是一种特异性有效的tankyrase 1 2抑制剂，可抑制Wnt 信号传导。