Wnt-C59 (C59)

Catalog No.S7037 Batch:S703704

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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)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG 300 5%Tween80 50% ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 3.800mg/ml (10.01mM) 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. At 10 nM, it blocks the palmitoylation-dependent Wnt–WLS interaction in HeLa cells transfected with either WNT3A-V5 or WNT8A-V5 plasmids. This compound (100 nM) prevents incorporation of palmitate into WNT3A in HeLa cells transfected with WNT3A-V5, consistent with inhibition of PORCN activity. It (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. It does not significantly inhibit the proliferation of any of 46 tested cancer cell lines in vitro at concentrations that completely inhibit PORCN. Wnt-C59 is capable to significantly inhibit proliferation and comparable to the ICG-001 treated NMuMG (NMG) cells. It inhibits sphere formation by threefold in NMuMG (NMG) cells, which is dependent on Wnt10b-secretion. This compound inhibits proliferation of human MDA-MB 231 cells by >50%. As a Porcupine inhibitor, it blocks radiolabel incorporation of [125I]iodo-pentadecanoate in mouse L-Wnt3a cells transfected with Flag-Porcupine.
In vivo Wnt-C59 (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. At 10 mg/kg, it prevents growth of MMTV-WNT1 tumors in female nude mice orthotopically transplanted with independent MMTV-WNT1 tumors. This compound also decreases Wnt pathway activity and proliferation in such tumors, as evident by reduced expression of β-catenin target genes. When topically administered at 10% for 4 weeks, it reduces the size of dysplasia in SmoM2-expressing cells in adult K14CREER/Rosa–SmoM2 mice.

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 amounts of Wnt-C59 (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

References

  • https://pubmed.ncbi.nlm.nih.gov/23188502/
  • https://pubmed.ncbi.nlm.nih.gov/23307470/
  • https://pubmed.ncbi.nlm.nih.gov/23416332/
  • https://pubmed.ncbi.nlm.nih.gov/23178882/

Customer Product Validation

<p>Application of XAV939 or Wnt-c59 with FGF2 blocks the accumulation of nuclear b-catenin in MGPCs, and increases levels of p38MAPK in Muller glia, whereas levels of cFos are unaffected. a, b, Eyes were injected with four consecutive daily injections of FGF2 6 XAV939 or Wnt-c59, BrdU 24 h after the last injection of FGF2, and retinas harvested 24 h later. Wnt-c59 (treated). a, b-catenin in the nuclei of Sox91 Muller glia/MGPCs on 70% grayscale background.</p>

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

In vitro treatment with C59 (Wnt-i) decreased the active (non-phosphorylated) β-catenin level in Eed cKO primary rib chondrocytes. Chondrocytes were cultured for 24 h in the presence of C59 (Wnt-i).

Data from [ , , Nat Commun, 2016, 7:12047 ]

Migration of L428 cells (b) and KM-H2 (c) after 72 h pretreatment with 5 μm Wnt-C59 or DMSO with (+CM) or without (−CM) the simultaneous stimulation with the respective cHL-CM for 24 h (mean±s.d., n=3, one-way ANOVA and Dunn’s post hoc test). Note the inhibition of migration by porcupine inhibitors, which is rescued by CM. (d) Invasion of L428 or KM-H2 cells after 72 h pretreatment with 5 μm Wnt-C59 or DMSO (mean±s.d., n=3 two-way ANOVA and Bonferroni’s post hoctest). (e) Adhesion of DMSO- or Wnt-C59-pretreated L428 cells on either HUVECs (white) or collagen I (gray) (mean±s.d., n=5, 2-way ANOVA and Bonferroni’s post hoc test). Note the decrease of adhesion after WNT inhibition (*P<0.05 and ***P<0.001).

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

(A) Body weight changes over the study by treatment group (LGK low: LGK974 at 3 mg/kg/day; LGK high: LGK974 at 6 mg/kg/kg/day; C59: Wnt-C59). (B) Femur length at necropsy. (C) Total body bone mineral density (BMD) at necropsy. (D) Spine BMD at necropsy.

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

Selleck's Wnt-C59 (C59) Has Been Cited by 193 Publications

Modeling early human heart development using an iPSC-based 3D bioprinted model of embryonic heart tube [ Nat Commun, 2026, 17(1):5689] PubMed: 42031752
Drug-induced gastrointestinal toxicity and barrier integrity: cytoskeleton-mediated impairment in a clinically relevant human intestinal epithelium model [ Exp Mol Med, 2026, 58(2):487-500] PubMed: 41680471
Unbiased cleavage site prediction uncovers viral antagonism of host innate immunity by SARS-CoV-2 3C-like protease [ JCI Insight, 2026, 11(4)e185739] PubMed: 41729072
Sustained β-catenin activation via GSK3 inhibition promotes direct fibroblast-to-cardiomyocyte reprogramming [ J Biol Chem, 2026, S0021-9258(26)00330-3] PubMed: 41999895
Iron deficiency drives pathological cardiac remodeling and diastolic dysfunction associated with inhibition of AMPK-mTORC1 signaling [ Cardiovasc Pathol, 2026, 83:107828] PubMed: 42019832
Spatial relationships between vinculin tension and actin at cell adhesions define cell colony positioning and identity [ Biophys J, 2026, 125(7):1583-1596] PubMed: 41691376
DHX15 overexpression suppresses colorectal cancer cell line proliferation [ Oncol Lett, 2026, 31(2):80] PubMed: 41635546
Generation of the human induced pluripotent stem cell (hiPSC) line AUMCi015-A from a heterozygous carrier of the LMNA p.Q493X rare pathogenic variant [ Stem Cell Res, 2026, 92:103962] PubMed: 41797063
MYC ecDNA promotes intratumour heterogeneity and plasticity in PDAC [ Nature, 2025, 10.1038/s41586-025-08721-9] PubMed: 40074906
Epithelial WNT secretion drives niche escape of developing gastric cancer [ Mol Cancer, 2025, 25(1):1] PubMed: 41398956

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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.

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