JW74

JW74 Chemische Eigenschaften,Einsatz,Produktion Methoden

• Beschreibung

  Tankyrases (TNKS) are poly(ADP-ribose) polymerases (PARPs) that cleave NAD⁺ to produce nicotinamide and ADP-ribose, which is then covalently attached to an acceptor protein in a process known as poly(ADP-ribosyl)ation. TNKS have key roles in the Wnt signaling pathway as part of the β-catenin destruction complex. JW 74 is an inhibitor of the catalytic PARP domain of TNKS1/2 that blocks canonical Wnt signaling with an IC₅₀ value of 790 nM. It increases the levels of Axin2 and decreases β-catenin levels in colorectal cancer (CRC) cells, leading to down-regulation of Wnt target genes. JW 74 inhibits the growth of CRC xenograft tumors in mice. JW 74 induces apoptosis and differentiation in osteosarcoma cell lines.

• Verwenden

  JW 74 is an inhibitor that affects cell cycle progression and induces apoptosis and differentiation in osteosarcoma cell lines.

• 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].

• IC 50

  790 nm for canonical wnt signaling

• Lager

  Store at +4°C

• Einzelnachweise

  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.

JW74 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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