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Purity: ≥98%
IWP-O1 is a novel and potent porcn (acyltransferase Porcupine) inhibitor with an EC50 value of 80 pM in a cultured cell reporter assay of Wnt signaling. It effectively suppresses the phosphorylation of Dvl2/3 in HeLa cells. The acyltransferase Porcupine (Porcn) is essential for the secretion of Wnt proteins which contribute to embryonic development, tissue regeneration, and tumorigenesis. Additionally, IWP-O1 has significantly improved metabolic stability over our previously reported Porcn inhibitors.
| ln Vitro |
IWP-O1 (17) is 2.5 times more active than the experimental medication LGK974 and suppresses Wnt signaling in L-Wnt-STF cells with an EC50 value of 80 pM [1].
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| References |
| Molecular Formula |
C26H20N6O
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| Molecular Weight |
432.47660446167
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| CAS # |
2074607-48-8
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| Related CAS # |
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| PubChem CID |
134154594
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
33
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| Complexity |
614
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(CN1C(C2C=CC=CC=2)=C(C2C=CN=CC=2)N=N1)NC1C=CC(=CN=1)C1C=CC=CC=1
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| Chemical Name |
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
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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: ≥ 2.08 mg/mL (4.81 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 20.8 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: ≥ 2.08 mg/mL (4.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3122 mL | 11.5612 mL | 23.1225 mL | |
| 5 mM | 0.4624 mL | 2.3122 mL | 4.6245 mL | |
| 10 mM | 0.2312 mL | 1.1561 mL | 2.3122 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.
he molecular scaffold (9) of interest in this study and the synthetic route for this triazole class of IWP molecules.Bioorg Med Chem Lett.2016 Dec 15;26(24):5891-5895. |
Biochemical characterization of IWP-O1 (17). HeLa cells which exhibit high levels of cell autonomous Wnt signaling,were incubated for 24 h with DMSO,17, or LGK974.Bioorg Med Chem Lett.2016 Dec 15;26(24):5891-5895. |
The general structure of IWP (5) and the effects of the biaryl and phenyl groups (6–8).Bioorg Med Chem Lett.2016 Dec 15;26(24):5891-5895. |
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