| Name | JW74 |
| Description | JW74 antagonizes LiCl-induced activation of the canonical Wnt signaling pathway (IC50: 420 nM). |
| In vitro | Ki-67 expression is reduced from 97.5% in DMSO-treated cells to 86.7% in JW74-treated cells. Relative to DMSO-treated cells, the cellular viability of U2OS cells treated for 72 h treatment with 10 μM JW74 is reduced to 80%. The effect of tankyrase inhibition on cellular viability is tested by performing an MTS assay. Flow cytometry is also performed to determine the expression marker Ki-67 in U2OS following 48 h treatment with DMSO or 10 uM JW74 [2]. JW74 displays a reduction of canonical Wnt signaling in the ST-Luc assay (IC50: 790 nM) [1]. |
| In vivo | The in vivo efficacy of JW74 is evaluated using SW480 cell xenografts, with high doses (150 or 300 mg/kg) administered due to rapid degradation in the organism, as shown by human liver microsome analysis (t1/2=2.5 minutes) and pharmacokinetic analyses (t1/2=30 minutes after peroral injections and t1/2=15 minutes after intravenous injections). JW74 concentrations in tumors range from 4.2 to 72.1 μmol/kg for 150 mg/kg, 1.9 to 11.1 μmol/kg for 300 mg/kg, and reach 2.8 μM in plasma for both doses [1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 45 mg/mL (98.57 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.38 mM), Sonication is recommended.
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| Keywords | βcatenin | Wnt/β-catenin | Wnt/betacatenin | Wnt/b-catenin | Wnt | JW-74 | JW74 | JW 74 | Inhibitor | inhibit | beta-catenin | betacatenin | bcatenin |
| Inhibitors Related | Chlorquinaldol | Urea | Wnt pathway activator 1 | Neohesperidin | XAV-939 | Ethyl linoleate | Monensin sodium salt | Nimbolide | Isoquercetin | (±)-Nornicotine | Methyl Vanillate | Bisdemethoxycurcumin |
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