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Wnt-C59

Cat. No. M3131
Wnt-C59  Structure
Synonym:

C59

Size Price Availability Quantity
2mg USD 42  USD42 In stock
5mg USD 55  USD55 In stock
10mg USD 85  USD85 In stock
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Quality Control
Biological Activity

Wnt-C59 (C59) is a PORCN inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase with IC50 of 74 pM.

Customer Product Validations & Biological Datas
Source Stem Cells Transl Med (2016). Figure 4. Wnt-C59
Method qPCR
Cell Lines human iPSCs
Concentrations 10 nM
Incubation Time 4 or 5 days
Results qPCR analyses revealed that neural aggregates differentiated with C59 contained more cells with rostral identity compared with DKK1 or XAV
Protocol
Cell Experiment
Cell lines NMuMG (NMG) and MDA-MB 231 cells
Preparation method Cells are seeded at a concentration of 4×103/well in 100 μL culture medium containing various amouts of Wnt-C59 and incubated for 48 hours at 37 ℃. Add 10 μL/well cell proliferation reagent and incubate for 4 hours at 37 ℃. Shake thoroughly for 1 min on a shaker. Measure the absorbance of the samples in a microplate (ELISA) reader.
Concentrations
Incubation time 48 hours
Animal Experiment
Animal models Female nude mice orthotopically transplanted with independent MMTV-WNT1 tumors
Formulation 0.5% methylcellulose and 0.1% Tween-80
Dosages 10 mg/kg
Administration orally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 379.45
Formula C25H21N3O
CAS Number 1243243-89-1
Purity 99.53%
Solubility DMSO 56 mg/mL
Storage at -20°C
References

[1] Jaewoong Jang, et al. Wnt-Signaling Inhibitor Wnt-C59 Suppresses the Cytokine Upregulation in Multiple Organs of Lipopolysaccharide-Induced Endotoxemic Mice via Reducing the Interaction between β-Catenin and NF-κB

[2] Jaewoong Jang, et al. Wnt-C59 inhibits proinflammatory cytokine expression by reducing the interaction between β-catenin and NF-κB in LPS-stimulated epithelial and macrophage cells

[3] Zhengbo Zhao, et al. Wnt-C59 Attenuates Pressure Overload-Induced Cardiac Hypertrophy via Interruption of Wnt Pathway

[4] Masaru Katoh. Multi‑layered prevention and treatment of chronic inflammation, organ fibrosis and cancer associated with canonical WNT/β‑catenin signaling activation (Review)

[5] Masaru Katoh. Canonical and non-canonical WNT signaling in cancer stem cells and their niches: Cellular heterogeneity, omics reprogramming, targeted therapy and tumor plasticity (Review)

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Keywords: Wnt-C59 , C59 supplier, Wnt/beta-catenin, inhibitors

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