yingweiwo

Wnt pathway activator 2

Cat No.:V39093 Purity: ≥98%
Wnt pathway activator 2 is a potent Wnt activator with EC50 of 13 nM.
Wnt pathway activator 2
Wnt pathway activator 2 Chemical Structure CAS No.: 1360540-82-4
Product category: New2
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
Wnt pathway activator 2 is a potent Wnt activator with EC50 of 13 nM. For more details, check and find patent WO2012024404A1, compound 2.
Wnt pathway activator 2 (CAS 1360540-82-4) is a potent small-molecule activator of the Wnt/β-catenin signaling pathway, a crucial cascade that regulates cell proliferation, differentiation, and tissue regeneration. Extracted from patent WO2012024404A1 as compound 2, this research compound has a molecular weight of 297.31 and the chemical name 1-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-pyridin-2-ylbutane-1,4-dione. It serves as a valuable pharmacological tool for dissecting the complex mechanisms of Wnt signaling and exploring its therapeutic potential in regenerative medicine and oncology.
Biological Activity I Assay Protocols (From Reference)
Targets
Wnt/β-catenin signaling pathway.
ln Vitro
Wnt pathway activator 2 is a potent activator of the Wnt/β-catenin pathway, with an EC₅₀ of 13 nM. Its activity is typically demonstrated in cell-based reporter assays where it induces TCF/LEF-dependent transcription, a hallmark of pathway activation.
ln Vivo
Detailed in vivo activity data for this specific compound is limited in the provided references. However, as a potent activator of the Wnt pathway, it is hypothesized to have effects on stem cell proliferation and tissue regeneration in animal models, though this requires further experimental validation.
Enzyme Assay
In vitro activity is typically assessed using cell-based reporter gene assays, such as the TCF/LEF-luciferase reporter system. Cells are transfected with a luciferase reporter construct containing TCF/LEF binding sites and treated with varying concentrations of the compound. The EC₅₀ (13 nM) is determined by measuring the increase in luciferase activity, which reflects the activation of the Wnt/β-catenin pathway.
Cell Assay
For in vitro cellular assays, cells (e.g., HEK293T or other Wnt-responsive cell lines) are cultured and treated with Wnt pathway activator 2 at various concentrations. The activation of the pathway is then quantified by measuring the expression of downstream target genes (such as Axin2 or Cyclin D1) via qPCR, or by using the aforementioned luciferase reporter assay. Cell viability and proliferation can also be assessed to study the compound's effects on cell growth.
Animal Protocol
In vivo efficacy studies are typically conducted in mouse models of tissue injury or disease where Wnt activation is desired. The compound is administered via various routes (e.g., intraperitoneal injection or oral gavage) at different doses. Tissue samples are then collected to analyze the expression of Wnt target genes and assess the extent of tissue regeneration or disease modification.
ADME/Pharmacokinetics
Specific pharmacokinetic data is not available from the provided references. However, as a small molecule (MW 297.31, LogP 1.8) with good solubility in DMSO, it is expected to have reasonable cell permeability. Formulation for in vivo use may require the use of co-solvents such as SBE-β-CD to enhance solubility.
Toxicity/Toxicokinetics
Toxicological data is not available from the provided references. As a research compound, it is intended for laboratory use only and not for human therapeutic applications.
References

[1]. Diketones and hydroxyketones as catenin signaling pathway activators. WO2012024404A1.

Additional Infomation
Wnt pathway activator 2 is a research tool for studying Wnt signaling. Its development is detailed in patent WO2012024404A1. It is not approved for clinical use and is intended solely for research purposes.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H15NO4
Molecular Weight
297.31
Exact Mass
297.1
CAS #
1360540-82-4
PubChem CID
56833973
Appearance
Light yellow to yellow solid powder
LogP
1.8
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
5
Rotatable Bond Count
5
Heavy Atom Count
22
Complexity
412
Defined Atom Stereocenter Count
0
SMILES
C(C1=CC=C2OCCOC2=C1)(=O)CCC(C1=NC=CC=C1)=O
InChi Key
DMBCGEJVWBLNDP-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H15NO4/c19-14(5-6-15(20)13-3-1-2-8-18-13)12-4-7-16-17(11-12)22-10-9-21-16/h1-4,7-8,11H,5-6,9-10H2
Chemical Name
1-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-pyridin-2-ylbutane-1,4-dione
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~100 mg/mL (~336.35 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 5 mg/mL (16.82 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 50.0 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.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.3635 mL 16.8175 mL 33.6349 mL
5 mM 0.6727 mL 3.3635 mL 6.7270 mL
10 mM 0.3363 mL 1.6817 mL 3.3635 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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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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