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JW 55PARP domain inhibitor

JW 55

Catalog No. A4529
Size Price Stock Qty
10mM (in 1mL DMSO) $99.00 In stock
Evaluation Sample $28.00 In stock
10mg $90.00 In stock
50mg $300.00 In stock
100 mg $520.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

JW 55

Related Biological Data

JW 55

Related Biological Data

JW 55

Biological Activity

JW 55 is an inhibitor of the PARP domain of tankyrase 1 and 2 (TNKS1/2). JW55 decreased auto-PARsylation of TNKS1/2 in vitro with IC50 values of 1.9 uM and 830 nM respectively.
Targets TNKS1 TNKS2        
IC50 1.9 uM 830 nM        

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Chemical Properties

Cas No. 664993-53-7 SDF Download SDF
Chemical Name N-[4-[[4-(4-methoxyphenyl)oxan-4-yl]methylcarbamoyl]phenyl]furan-2-carboxamide
Canonical SMILES COC1=CC=C(C=C1)C2(CCOCC2)CNC(=O)C3=CC=C(C=C3)NC(=O)C4=CC=CO4
Formula C25H26N2O5 M.Wt 434.48
Solubility Soluble in DMSO > 10 mM Storage Store at 4°C
General tips N/A
Shipping Condition N/A

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Background

IC50: 1.9 μM (TNK S1); 0.83 μM (TNK S2)

Increased nuclear accumulation of β-catenin, a mediator of canonical Wnt signaling, is found in numerous tumors and is frequently associated with tumor progression and metastasis. Inhibition of Wnt/b-catenin signaling therefore is an attractive strategy for anticancer drugs.

In vitro: In a previous study, the authors identified a novel small molecule inhibitor of the β-catenin signaling pathway, JW55, that functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2), regulators of the b-catenin destruction complex. Inhibition of TNKS1/2 poly(ADP-ribosyl)ation activity by JW55 led to stabilization of AXIN2, a member of the b-catenin destruction complex, followed by increased degradation of b-catenin. In a dose-dependent manner, JW55 inhibited canonical Wnt signaling in colon carcinoma cells that contained mutations in either the APC (adenomatous polyposis coli) locus or in an allele of b-catenin [1].

In vivo: JW55 was reported to reduce XWnt8-induced axis duplication in Xenopus embryos and tamoxifen-induced polyposis formation in conditional APC mutant mice. These findings provide a novel chemotype for targeting canonical Wnt/b-catenin signaling through inhibiting the PARP domain of TNKS1/2 [1].

Clinical trial: JW55 is currently in the preclinical development and no clinical trial is ongoing.

Reference:
[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.