tankyrase

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

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.

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

Tankyrase Inhibitors 49 is an effective, selective, and orally bioavailable inhibitor of tankyrase (IC50: 0.1nM).

Tankyrase Inhibitors 22 is a potent, selective, and orally bioavailable inhibitor of tankyrase (IC50: 0.1nM).

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

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].

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

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.

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.

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.

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

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

E7449 (UNII-9X5A2QIA7C) is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ～50 and ～50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD+ as substrate.

TIQ-A is a PARP1 inhibitor which involved in DNA single-strand break repair via the base excision repair pathway. PARP1 is triggered by DNA damage and its excessive activation has been proposed as a causative factor in many pathological conditions includi

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.

K-756 is a direct and selective inhibitor of tankyrase (TNKS), inhibiting the ADP-ribosylation activity of TNKS1 [IC50 = 31 nM] and TNKS2 [IC50 = 36 nM].

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).

XAV-939 (NVP-XAV939) is a Tankyrase (TNKS) inhibitor that inhibits TNKS1 and TNKS2 (IC50=11/4 nM). XAV-939 selectively inhibits Wnt/β-catenin-mediated transcription.

G-631 acts as a selective tankyrase inhibitor, effectively hindering tankyrase auto-PARsylation (poly ADP ribosylation) at an IC 50 of 7 nM and suppressing the Wnt signaling pathway. This compound also demonstrates favorable pharmacokinetic properties in mice.

EXQ-2d is an inhibitor of tankyrase, effectively targeting TNKS1 and TNKS2 with IC50 values of 48.8 nM and 13.8 nM (pIC50=7.31 and 7.86), respectively. Additionally, EXQ-2d suppresses the WNT/β-catenin signaling pathway with an IC50 of 515 nM. It demonstrates antiproliferative activity in cancer cells COLO 320DM and RKO, with GI50 values of 4.9 μM and 77 μM, respectively.

ARCher-142 (compound S8) is a potent inhibitor of tankyrase. It selectively binds to ARC4 with an efficacy of 8 µM.

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.