JW55 Chemical Properties

Boiling point:

572.6±50.0 °C(Predicted)

Density 

1.235±0.06 g/cm3(Predicted)

storage temp. 

Inert atmosphere,2-8°C

solubility 

DMSO: soluble15mg/mL, clear

form 

powder

pka

12.41±0.70(Predicted)

color 

white to beige

InChI

1S/C25H26N2O5/c1-30-21-10-6-19(7-11-21)25(12-15-31-16-13-25)17-26-23(28)18-4-8-20(9-5-18)27-24(29)22-3-2-14-32-22/h2-11,14H,12-13,15-17H2,1H3,(H,26,28)(H,27,29)

InChIKey

ZJZWZIXSGNFWQQ-UHFFFAOYSA-N

SMILES

O1C=CC=C1C(NC1=CC=C(C(NCC2(C3=CC=C(OC)C=C3)CCOCC2)=O)C=C1)=O

Safety Information

WGK Germany 

3

Storage Class

11 - Combustible Solids

JW55 Usage And Synthesis

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.