JW 67CAS# 442644-28-2 |
Quality Control & MSDS
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| Cas No. | 442644-28-2 | SDF | Download SDF |
| PubChem ID | 644733 | Appearance | Powder |
| Formula | C21H18N2O6 | M.Wt | 394.38 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO | ||
| SMILES | C1C2(COC3(O1)C4=CC=CC=C4NC3=O)COC5(C6=CC=CC=C6NC5=O)OC2 | ||
| Standard InChIKey | BTXRSHKJNDFHGA-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C21H18N2O6/c24-17-20(13-5-1-3-7-15(13)22-17)26-9-19(10-27-20)11-28-21(29-12-19)14-6-2-4-8-16(14)23-18(21)25/h1-8H,9-12H2,(H,22,24)(H,23,25) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Inhibitor of canonical Wnt pathway signaling (IC50 = 1.17 μM); targets the β-catenin destruction complex (GSK-3β/AXIN/APC) to induce β-catenin degradation. Selective for the canonical Wnt pathway over the Sonic hedgehog (Shh) and NF-κB pathways. Blocks G1/S cell cycle progression in colorectal cancer (CRC) cell lines (GI50 = 7.8 μM). |
JW 67 Dilution Calculator
JW 67 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.5356 mL | 12.6781 mL | 25.3563 mL | 50.7125 mL | 63.3906 mL |
| 5 mM | 0.5071 mL | 2.5356 mL | 5.0713 mL | 10.1425 mL | 12.6781 mL |
| 10 mM | 0.2536 mL | 1.2678 mL | 2.5356 mL | 5.0713 mL | 6.3391 mL |
| 50 mM | 0.0507 mL | 0.2536 mL | 0.5071 mL | 1.0143 mL | 1.2678 mL |
| 100 mM | 0.0254 mL | 0.1268 mL | 0.2536 mL | 0.5071 mL | 0.6339 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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[1,2,4]triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazoles: antagonists of the Wnt pathway that inhibit tankyrases 1 and 2 via novel adenosine pocket binding.[Pubmed:22260203]
J Med Chem. 2012 Feb 9;55(3):1127-36.
The Wnt signaling pathway is critical to the regulation of key cellular processes. When deregulated, it has been shown to play a crucial role in the growth and progression of multiple human cancers. The identification of small molecule modulators of Wnt signaling has proven challenging, largely due to the relative paucity of druggable nodes in this pathway. Several recent publications have identified small molecule inhibitors of the Wnt pathway, and tankyrase (TNKS) inhibition has been demonstrated to antagonize Wnt signaling via axin stabilization. Herein, we report the early hit assessment of a series of compounds previously reported to antagonize Wnt signaling. We report the biophysical, computational characterization, structure-activity relationship, and physicochemical properties of a novel series of [1,2,4]triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazole inhibitors of TNKS1 and 2. Furthermore, a cocrystal structure of compound 24 complexed to TNKS1 demonstrates an alternate binding mode for PARP family member proteins that does not involve interactions with the nicotinamide binding pocket.
Novel synthetic antagonists of canonical Wnt signaling inhibit colorectal cancer cell growth.[Pubmed:21199802]
Cancer Res. 2011 Jan 1;71(1):197-205.
Canonical Wnt signaling is deregulated in several types of human cancer where it plays a central role in tumor cell growth and progression. Here we report the identification of 2 new small molecules that specifically inhibit canonical Wnt pathway at the level of the destruction complex. Specificity was verified in various cellular reporter systems, a Xenopus double-axis formation assay and a gene expression profile analysis. In human colorectal cancer (CRC) cells, the new compounds JW67 and JW74 rapidly reduced active beta-catenin with a subsequent downregulation of Wnt target genes, including AXIN2, SP5, and NKD1. Notably, AXIN2 protein levels were strongly increased after compound exposure. Long-term treatment with JW74 inhibited the growth of tumor cells in both a mouse xenograft model of CRC and in Apc(Min) mice (multiple intestinal neoplasia, Min). Our findings rationalize further preclinical and clinical evaluation of these new compounds as novel modalities for cancer treatment.
