Description

JW 55 is an inhibitor of the PARP domain of tankyrases (TNKS) 1 and 2 (IC₅₀s = 1.9 and 0.83 μM, respectively). By inhibiting TNKS1/2, JW 55 stabilizes Axin2 and increases degradation of β-catenin, inhibiting the β-catenin signaling pathway (IC₅₀ = 470 nM). It has been shown to decrease canonical Wnt signaling in SW480 and HCT15 colon carcinoma cell lines and to reduce proliferation of SW480 cells in vitro.

Uses

JW-55 is an inhibitor of the PARP domain of tankyrase 1 and 2 (TNKS1/2). Activity results in stabilization of Axin2 and increased degradation of β-catenin. JW-55 inhibits the β-catenin signaling pathway. Also shown to decrease canonical Wnt signaling in SW480 and HCT-15 colon carcinoma cell lines. JW-55 reduces cell cycle progression and proliferation in SW480 cells in vitro.

Definition

ChEBI: N-[4-[[[4-(4-methoxyphenyl)-4-oxanyl]methylamino]-oxomethyl]phenyl]-2-furancarboxamide is a member of furans and an aromatic amide.

in vivo

IC 50

TNKS2: 0.83 μM (IC₅₀); TNKS1: 1.9 μM (IC₅₀)

storage

Store at +4°C

References

[1] waaler j, machon o, tumova l, dinh h, korinek v, wilson sr, paulsen je, pedersen nm, eide tj, machonova o, gradl d, voronkov a, von kries jp, krauss s. a novel tankyrase inhibitor decreases canonical wnt signaling in colon carcinoma cells and reduces tumor growth in conditional apc mutant mice. cancer res. 2012;72(11):2822-32.