tankyrase 1

Niraparib (MK-4827) is a PARP inhibitor that selectively targets PARP1 and PARP2 (IC50=3.8 2.1 nM), exhibiting antitumor activity, inhibiting DNA damage repair, and inducing apoptosis.

Olaparib (KU0059436) is a small molecule inhibitor of PARP1 PARP2 (IC50=5 1 nM), with weak inhibitory activity against PARP tankyrase-1 (IC50=1.5 μM), and is selective and orally active. Olaparib exhibits autophagy and mitochondrial autophagy activation activity.

Niraparib, also know as MK-4827, is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. MK4827 inhibits PARP activity, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. The PARP family of proteins detect and repair single strand DNA breaks by the base-excision repair (BER) pathway.

exo-IWR-1 (exo-IWR 1) is an inactive stereoisomer of Endo-IWR-1,and is a negative control of IWR-1. IWR-1 is a tankyrase inhibitor which inhibits Wnt β-catenin signaling pathway.

MN-64 is a tankyrases inhibitor, showed 6 nM potency against tankyrase 1, isoenzyme selectivity, and Wnt signaling inhibition.

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

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.

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)

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.

Tankyrase-IN-5 (Compound 30f), structurally related to MSC2504877, effectively inhibits tankyrase isoforms TNKS1 and TNKS2 with IC50 values of 2.3 nM and 7.9 nM, respectively [1].

Tankyrase-IN-4 is a potent inhibitor of tankyrase 1 (TNKS1), exhibiting an IC50 of 0.8 nM, and is utilized in cancer research.

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).

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.

Niraparib tosylate (MK-4827 (tosylate))(with IC50 of 3.8 nM 2.1 nM) is a selective PARP1 PARP2 inhibitor.

Niraparib hydrochloride (MK-4827 hydrochloride) is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. By inhibiting PARP activity, niraparib hydrochloride increases DNA strand breaks, leading to genomic instability and apoptosis. The PARP family of proteins detects and repairs single-strand DNA breaks via the base-excision repair (BER) pathway.

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

TNKS-IN-1 is a highly potent and selective inhibitor of tankyrase.

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.

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).

PARP1-IN-15 (Compound 6) is a PARP1 inhibitor that also inhibits tankyrase (TNKS) and promotes DNA double-strand breaks, leading to tumor cell apoptosis. It exhibits anti-cancer activity in triple-negative breast cancer (TNBC) cells and patient-derived organoids, making it useful for TNBC research, including cases with or without BRCA1 mutations [1].

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.