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Purity: ≥98%
JW-55 (JW55) is a potent and selective small molecule inhibitor of β-catenin signaling pathway with anticancer activity. It inhibits the β-catenin destruction complex regulators tankyrase 1 and tankyrase 2 (TNKS1/2) PARP domains. TNKS1/2 auto-PARsylation is reduced in vitro by JW 55, with IC50 values of 1.9 μM and 830 nM, respectively. When JW55 inhibited the poly(ADP-ribosyl)ation activity of TNKS1/2, AXIN2, a component of the β-catenin destruction complex, stabilized. This was followed by an increase in the degradation of β-catenin. In colon carcinoma cells with mutations in either the β-catenin allele or the APC (adenomatous polyposis coli) locus, JW55 inhibited canonical Wnt signaling in a dose-dependent manner. Furthermore, JW55 inhibited the formation of polyposis in conditional APC mutant mice induced by tamoxifen and the axis duplication induced by XWnt8 in Xenopus embryos.
| Targets |
TNKS2 ( IC50 = 0.83 μM ); TNKS1 ( IC50 = 1.9 μM )
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
JW 55, also known as JW55, is a strong and specific inhibitor of the Wnt pathway. JW55 exhibits inhibition of Wnt3a-induced HEK293 cells with an IC50 value of 470 nM, when the cells contain a transiently transfected ST-Luc (SuperTop-luciferase) reporter. JW55 exhibits efficacy within the concentration range of 1 to 5 μM in SW480 cells and 0.01 to 5 μM in HCT-15 cells. JW55 exhibits efficacy within the concentration range of 1 to 5 μM in SW480 cells and 0.01 to 5 μM in HCT-15 cells.
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| Cell Assay |
In 96-well plates, 1,000 SW480 or RKO cells are seeded. The following day, solutions containing 0.1% DMSO or 10 μM JW55 for RKO cells and 0.1% DMSO or 10, 5, or 1 μM JW55 for SW480 cells are substituted for the original cell culture medium. Every sample has at least six duplicates. Within a cell culture incubator, the plate is incubated in an IncuCyte. Every two hours, pictures are taken to track proliferation.
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| Animal Protocol |
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| References | ||
| Additional Infomation |
N-[4-[[[4-(4-methoxyphenyl)-4-oxanyl]methylamino]-oxomethyl]phenyl]-2-furancarboxamide is a member of furans and an aromatic amide.
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| Molecular Formula |
C₂₅H₂₆N₂O₅
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| Molecular Weight |
434.48
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| Exact Mass |
434.184
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| Elemental Analysis |
C, 69.11; H, 6.03; N, 6.45; O, 18.41
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| CAS # |
664993-53-7
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| Related CAS # |
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| PubChem CID |
2946601
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| Appearance |
White solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
572.6±50.0 °C at 760 mmHg
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| Flash Point |
300.1±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.601
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| LogP |
3.54
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
32
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| Complexity |
620
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C([H])([H])C([H])([H])C(C2C([H])=C([H])C(=C([H])C=2[H])OC([H])([H])[H])(C([H])([H])N([H])C(C2C([H])=C([H])C(=C([H])C=2[H])N([H])C(C2=C([H])C([H])=C([H])O2)=O)=O)C([H])([H])C1([H])[H]
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| InChi Key |
ZJZWZIXSGNFWQQ-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
N-[4-[[4-(4-methoxyphenyl)oxan-4-yl]methylcarbamoyl]phenyl]furan-2-carboxamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.75 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.75 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3016 mL | 11.5080 mL | 23.0160 mL | |
| 5 mM | 0.4603 mL | 2.3016 mL | 4.6032 mL | |
| 10 mM | 0.2302 mL | 1.1508 mL | 2.3016 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 JW55 specifically reduces canonical Wnt signaling in reporter cells and inXenopusembryos.Cancer Res.2012 Jun 1;72(11):2822-32. |
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 JW55 inhibits canonical Wnt signaling in CRC cells.Cancer Res.2012 Jun 1;72(11):2822-32. |
 JW55 mediates increased AXIN2 stability and induces β-catenin degradation.Cancer Res.2012 Jun 1;72(11):2822-32. |
JW55 specifically inhibits TNKS1, TNKS2 but not PARP1 in biochemical assays.Cancer Res.2012 Jun 1;72(11):2822-32. |
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 Scheme showing the proposed effect of JW55 on protein stability in the β-catenin destruction complex.
Inhibition of canonical Wnt signaling by JW55 promotes cell-cycle arrest and specifically reduces proliferation in SW480 CRC cells.Cancer Res.2012 Jun 1;72(11):2822-32. |
JW55 treatment decreases development of adenomas in conditionalApcknockout mice.Cancer Res.2012 Jun 1;72(11):2822-32. |
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