IWP-L6Porcupine inhibitor,highy potent CAS# 1427782-89-5 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 1427782-89-5 | SDF | Download SDF |
| PubChem ID | 71601111 | Appearance | Powder |
| Formula | C25H20N4O2S2 | M.Wt | 472.58 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 1.43 mg/mL (3.03 mM; Need ultrasonic) | ||
| Chemical Name | 2-[(4-oxo-3-phenyl-6,7-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(5-phenylpyridin-2-yl)acetamide | ||
| SMILES | C1CSC2=C1N=C(N(C2=O)C3=CC=CC=C3)SCC(=O)NC4=NC=C(C=C4)C5=CC=CC=C5 | ||
| Standard InChIKey | QESQGTFWEQMCMH-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C25H20N4O2S2/c30-22(28-21-12-11-18(15-26-21)17-7-3-1-4-8-17)16-33-25-27-20-13-14-32-23(20)24(31)29(25)19-9-5-2-6-10-19/h1-12,15H,13-14,16H2,(H,26,28,30) | ||
| 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 | Potent inhibitor of Porcupine (PORCN), a membrane-bound O-acyltransferase (MBOAT) (EC50 = 0.5 nM). Shown to inhibit Wnt-dependent processes such as tailfin regeneration and posterior axis formation in zebrafish; also reduces branching morphogenesis in cultured mouse embryonic kidneys. |
IWP-L6 Dilution Calculator
IWP-L6 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.116 mL | 10.5802 mL | 21.1604 mL | 42.3209 mL | 52.9011 mL |
| 5 mM | 0.4232 mL | 2.116 mL | 4.2321 mL | 8.4642 mL | 10.5802 mL |
| 10 mM | 0.2116 mL | 1.058 mL | 2.116 mL | 4.2321 mL | 5.2901 mL |
| 50 mM | 0.0423 mL | 0.2116 mL | 0.4232 mL | 0.8464 mL | 1.058 mL |
| 100 mM | 0.0212 mL | 0.1058 mL | 0.2116 mL | 0.4232 mL | 0.529 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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IWP-L6 is an inhibitor of Porcupine with IC50 value of 0.5nM [1].
IWP-L6 is developed as a sub-nanomolar inhibitor.of Porcupine. It targets the Wnt signaling since Porcupine is the enzyme to catalyze the palmitoylation of Wnt proteins. In HEK293 cells, IWP-L6 is found to inhibi the phosphorylation of dishevelled 2 (Dvl2) significantly. IWP-L6 has good stability in human plasma but weaker stability in rat and mouse plasma. In vivo assay shows that IWP-L6 is quite active in zebrafish. It blocks the regeneration of the tailfin effectively. It also shows inhibition of posterior axis formation at low micromolar concentrations. Additionally, in cultured mouse embryonic kidneys, 10nM IWP-L6 can significantly reduce branching morphogenesis while 50nM IWP-L6 completely blocks Wnt signaling [1].
References:
[1] Wang X, Moon J, Dodge ME, Pan X, Zhang L, Hanson JM, Tuladhar R, Ma Z, Shi H, Williams NS, Amatruda JF, Carroll TJ, Lum L, Chen C. The development of highly potent inhibitors for porcupine. J Med Chem. 2013 Mar 28;56(6):2700-4.
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The development of highly potent inhibitors for porcupine.[Pubmed:23477365]
J Med Chem. 2013 Mar 28;56(6):2700-4.
Porcupine is a member of the membrane-bound O-acyltransferase family of proteins. It catalyzes the palmitoylation of Wnt proteins, a process required for their secretion and activity. We recently disclosed a class of small molecules (IWPs) as the first reported Porcn inhibitors. We now describe the structure-activity relationship studies and the identification of subnanomolar inhibitors. We also report herein the effects of IWPs on Wnt-dependent developmental processes, including zebrafish posterior axis formation and kidney tubule formation.
