Wnt-C59 (C59)

Catalog No.S7037 Batch:S703702

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Technical Data

Formula

C25H21N3O
Molecular Weight 379.45 CAS No. 1243243-89-1
Solubility (25°C)* In vitro DMSO 76 mg/mL (200.28 mM)
Ethanol 19 mg/mL (50.07 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 95% Corn oil
3.8mg/ml Taking the 1 mL working solution as an example, add 50 μL of 76 mg/mL clarified DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG 300 5%Tween80 50% ddH2O
3.8mg/ml Taking the 1 mL working solution as an example, add 50 μL of 76 mg/ml clear DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween-80 to the above system, mix evenly to clarify it; Then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Wnt-C59 (C59) is a PORCN inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase with IC50 of 74 pM in HEK293 cells.
Targets
Porcn [1]
(HEK293 cells )
74 pM
In vitro Wnt-C59 (C59) is claimed to inhibit PORCN enzyme activity at nanomolar concentrations. Wnt-C59 (10 nM) blocks the palmitoylation-dependent Wnt–WLS interaction in HeLa cells transfected with either WNT3A-V5 or WNT8A-V5 plasmids. Wnt-C59 (100 nM) prevents incorporation of palmitate into WNT3A in HeLa cells transfected with WNT3A-V5, consistent with inhibition of PORCN activity. Wnt-C59 (100 nM) inhibits the activity of all splice variants of murine PORCN in PORCN-null HT1080 cells transfected with PORCN. Wnt-C59 is a nanomolar inhibitor of mammalian PORCN acyltransferase activity and blocks activation of all evaluated human Wnts. Wnt-C59 does not significantly inhibit the proliferation of any of 46 tested cancer cell lines in vitro at concentrations that completely inhibit PORCN. [1] Wnt-C59 is capable to significantly inhibit proliferation and comparable to the ICG-001 treated NMuMG (NMG) cells. Wnt-C59 inhibits sphere formation by threefold in NMuMG (NMG) cells, which is dependent on Wnt10b-secretion. Wnt-C59 inhibits proliferation of human MDA-MB 231 cells by >50%. [2] Wnt-C59 (a Porcupine inhibitor) blocks radiolabel incorporation of [125I]iodo-pentadecanoate in mouse L-Wnt3a cells transfected with Flag-Porcupine. [3]
In vivo Wnt-C59 concentration remains greater than 10-fold above the in vitro IC50 for at least 16 hours following a single oral dose (5 mg/kg) in mice. Wnt-C59 (10 mg/kg) prevents growth of MMTV-WNT1 tumors in female nude mice orthotopically transplanted with independent MMTV-WNT1 tumors. Wnt-C59 (10 mg/kg) decreases Wnt pathway activity and decreased proliferation in MMTV-WNT1 tumors in female nude mice orthotopically transplanted with independent MMTV-WNT1 tumors as evident by decreased expression of β-catenin target gene expression. [1] Wnt-C59 (10%) topically administered 4 weeks decreases the size of dysplasia of SmoM2-expressing cells in adult K14CREER/Rosa–SmoM2 mice. [4]

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    NMuMG (NMG) and MDA-MB 231 cells

  • Concentrations

    --

  • Incubation Time

    48 hours

  • Method

    Seed cells at a concentration of 4×103/well in 100 μL culture medium containing various amouts of Wnt-C59. Incubate cells 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.
Animal Study:

[1]
  • Animal Models

    Female nude mice orthotopically transplanted with independent MMTV-WNT1 tumors

  • Dosages

    10 mg/kg

  • Administration

    orally

Customer Product Validation

, , Dev Neurobiol, 2016, 76(9):983-1002.

Data from [Data independently produced by , , Nat Commun, 2016, 7:12047]

Data from [Data independently produced by , , Oncogene, 2017, 36(1):13-23]

Data from [Data independently produced by , , J Endocrinol, 2018, 238(1):13-23]

Selleck's Wnt-C59 (C59) has been cited by 146 publications

PIBF1 regulates trophoblast syncytialization and promotes cardiovascular development [ Nat Commun, 2024, 15(1):1487] PubMed: 38374152
Ultrasound Mediated Polymerization for Cell Delivery, Drug Delivery, and 3D Printing [ Small Methods, 2024, e2301197.] PubMed: 38376006
ALK upregulates POSTN and WNT signaling to drive neuroblastoma [ Cell Rep, 2024, 43(3):113927] PubMed: 38451815
Generation of human vascularized and chambered cardiac organoids for cardiac disease modelling and drug evaluation [ Cell Prolif, 2024, e13631.] PubMed: 38453465
ER stress and lipid imbalance drive diabetic embryonic cardiomyopathy in an organoid model of human heart development [ Stem Cell Reports, 2024, S2213-6711(24)00006-7] PubMed: 38335962
Coactivator condensation drives cardiovascular cell lineage specification [ Sci Adv, 2024, 10(11):eadk7160] PubMed: 38489358
Biohybrid 3D Printing of a Tissue-Sensor Platform for Wireless, Real-Time, and Continuous Monitoring of Drug-Induced Cardiotoxicity [ Adv Mater, 2023, 35(11):e2208983] PubMed: 36528341
Electric-Field-Driven Printed 3D Highly Ordered Microstructure with Cell Feature Size Promotes the Maturation of Engineered Cardiac Tissues [ Adv Sci (Weinh), 2023, 10(11):e2206264] PubMed: 36782337
Single-swap editing for the correction of common Duchenne muscular dystrophy mutations [ Mol Ther Nucleic Acids, 2023, 32:522-535] PubMed: 37215149
Combined lineage tracing and scRNA-seq reveals unexpected first heart field predominance of human iPSC differentiation [ Elife, 2023, 12e80075] PubMed: 37284748

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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