JW 55

JW 55

Catalog Number:
L002369282APE
Mfr. No.:
APE-A4529
Price:
$244
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      • Overview
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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.

      • Properties
        • Alternative Name
          N-[4-[[4-(4-methoxyphenyl)oxan-4-yl]methylcarbamoyl]phenyl]furan-2-carboxamide
          CAS Number
          664993-53-7
          Molecular Formula
          C25H26N2O5
          Molecular Weight
          434.48
          Appearance
          A solid
          Purity
          99.31%
          Solubility
          insoluble in H2O; ≥19.25 mg/mL in DMSO; ≥3.53 mg/mL in EtOH with ultrasonic
          Storage
          Store at 4°C

          * For Research Use Only

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