JW 74 |
| Catalog No.GC13978 |
JW 74 antagonise l'activation induite par LiCl de la signalisation canonique Wnt avec une IC50 de 420 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 863405-60-1
Sample solution is provided at 25 µL, 10mM.
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IC50: 790 nM for canonical Wnt signaling
JW 74 is an inhibitor of the catalytic PARP domain of TNKS1/2.
Wnt/β-catenin, a major regulator of stem cell self-renewal and differentiation, is aberrantly activated in a several cancers, including osteosarcoma. Thus, attenuation of Wnt/β-catenin activity by tankyrase inhibitors is an appealing strategy in osteosarcoma treatment.
In vitro: Previous study found that JW74 at the molecular level induced stabilization of AXIN2, a key component of the β-catenin destruction complex, leading to reduced levels of nuclear β-catenin. In addition, JW74 could induce reduced cell growth in all tested cell lines, partially due to a delay in cell cycle progression and partially because of an induction of caspase-3-mediated apoptosis. Moreover, JW74 was able to induce the differentiation in U2OS cells and also enhance differentiation of OS cell lines that did not harbor a differentiation block [1].
In vivo: Previous animal study found that the dose of 150 mg/kg of JW74 in ApcMin model could reduce the small intestinal adenoma by 48% and was comparable with celecoxib or rofecoxib. Furthermore, it was noteworthy that JW74 became rapidly cleared from the blood stream due to its poor in vivo stability [2].
Clinical trial: Up to now, JW 74 is still in the preclinical development stage.
References:
1. E. W. Stratford, J. Daffinrud, E. Munthe, et al. The tankyrase-specific inhibitor JW74 affects cell cycle progression and induces apoptosis and differentiation in osteosarcoma cell lines. Cancer Med. 3(1), 36-46 (2014).
2. Waaler J et al. Novel synthetic antagonists of canonical Wnt signaling inhibit colorectal cancer cell growth. Cancer Res. 2011 Jan 1;71(1):197-205.
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