| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
Porcupine-IN-1 targets the enzyme Porcupine, an acyltransferase that catalyzes the addition of palmitoleic acid to Wnt proteins. This post-translational modification is essential for the secretion and activity of Wnt proteins. By inhibiting Porcupine, the compound blocks the secretion of Wnt ligands, thereby attenuating Wnt signaling. It is also an inhibitor of the Hedgehog signaling pathway, with an IC50 of 71 nM.
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| ln Vitro |
The enzyme porcupine catalyzes the process of adding palmitoleic acid to the serine residues of Wnt proteins, which is necessary for Wnt protein secretion. Porcupine-IN-1 demonstrated the same efficacy in cell-based STF reporter assays as the therapeutic drug LGK974. It has been established that porcupine inhibitor Porcn-IN-1 is able to efficiently block Wnt3A secretion [1].
In vitro, Porcupine-IN-1 is a potent inhibitor of Wnt signaling. It has an IC50 of 0.5 ± 0.2 nM in cell-based reporter assays. It has also been shown to be effective in Wnt3A-transfected HEK293T cells when used at a concentration of 0.1 μM. Its activity is characterized by its ability to inhibit the secretion of Wnt proteins and consequently block downstream signaling events. |
| ln Vivo |
In response to rat liver microsomes (24 mL/min/kg) and human liver microsomes (57 mL/min/kg), porccn-IN-1 demonstrated a modest clearance. There is a high clearance rate (109 mL/min/kg) when treated with mouse microsomes [1].
In vivo, Porcupine-IN-1 is used in research to study the role of Wnt signaling in various diseases, including cancer. By inhibiting Porcupine, it can block the secretion of Wnt ligands, thereby attenuating the pathway that is often hyperactivated in tumors. While specific in vivo efficacy data are not detailed in the provided sources, its potent in vitro activity makes it a valuable tool for such studies. |
| Enzyme Assay |
In vitro enzyme/receptor binding studies for Porcupine-IN-1 are not typical, as its target is an enzyme (Porcupine). However, its activity is assessed in cell-based reporter assays that measure Wnt signaling. In these assays, cells containing a Wnt-responsive reporter are treated with the compound, and the reporter activity is measured. The IC50 of 0.5 ± 0.2 nM confirms its potent inhibition of the Wnt pathway.
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| Cell Assay |
In vitro cellular assays for Porcupine-IN-1 are the primary method for evaluating its activity. These assays involve treating cells with the compound and measuring the inhibition of Wnt signaling. Typically, cells transfected with a Wnt-responsive reporter construct are used. The compound's ability to inhibit the secretion of Wnt proteins and the subsequent activation of the signaling cascade is assessed, with an IC50 of 0.5 ± 0.2 nM.
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| Animal Protocol |
In vivo animal studies for Porcupine-IN-1 are conducted in models where Wnt signaling is a key driver of disease, such as cancer xenografts. Tumor-bearing mice are treated with the compound, and endpoints include tumor growth inhibition and the analysis of Wnt target gene expression in the tumor tissue. These studies are essential for validating the therapeutic potential of targeting Porcupine in vivo.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Porcupine-IN-1 are indicated by its molecular weight of 410.44 g/mol and a molecular formula of C₂₅H₁₉FN₄O. It is a solid powder and is soluble in DMSO. For storage, it is recommended to keep the powder at -20°C to maintain stability. These properties are important for its formulation and use in both in vitro and in vivo experiments.
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| Toxicity/Toxicokinetics |
Toxicological data for Porcupine-IN-1 are limited, as it is a research compound. Its primary value is as a tool for studying Wnt signaling. While specific toxicity profiles are not detailed, its mechanism of inhibiting a key enzyme in the Wnt pathway could have significant biological effects. Comprehensive safety studies are not available in the public domain.
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| References | |
| Additional Infomation |
Porcupine-IN-1 free base is a research-use-only compound that acts as a potent inhibitor of the Porcupine enzyme. Its CAS number is 2036044-77-4. It is also known as Porcn-IN-1. This compound is a valuable tool for researchers studying the Wnt signaling pathway and its role in development and disease. It is not an approved drug.
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| Molecular Formula |
C25H19FN4O
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|---|---|
| Molecular Weight |
410.442968606949
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| Exact Mass |
410.154
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| CAS # |
2036044-77-4
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| Related CAS # |
2036044-77-4;
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| PubChem CID |
132578555
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| Appearance |
White to off-white solid powder
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| LogP |
4.2
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
633
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C(C2C=CN=C(C)C=2)=NC=C(C=1)CNC(C1C=CC2C3C=CC=CC=3NC=2C=1)=O
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| InChi Key |
GOMFFTZBKYVUOE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H19FN4O/c1-15-10-17(8-9-27-15)24-21(26)11-16(13-28-24)14-29-25(31)18-6-7-20-19-4-2-3-5-22(19)30-23(20)12-18/h2-13,30H,14H2,1H3,(H,29,31)
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| Chemical Name |
N-((3-Fluoro-2’-methyl[2,4’-bipyridin]-5-yl)methyl)-9H-carbazole-2-carboxamide
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| Synonyms |
Porcupine-IN-1 Porcupine-IN 1 Porcupine-IN1
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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 |
| 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) |
DMSO : ≥ 100 mg/mL (~243.64 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4364 mL | 12.1820 mL | 24.3641 mL | |
| 5 mM | 0.4873 mL | 2.4364 mL | 4.8728 mL | |
| 10 mM | 0.2436 mL | 1.2182 mL | 2.4364 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.
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