4-(2-Methyl-4-pyridinyl)-N-[4-(3-pyridinyl)phenyl]benzeneacetamide Wnt-c59
Wnt-C59 (C59)
CAS: 1243243-89-1
Molecular Formula: C25H21N3O
4-(2-Methyl-4-pyridinyl)-N-[4-(3-pyridinyl)phenyl]benzeneacetamide Wnt-c59 - Names and Identifiers
4-(2-Methyl-4-pyridinyl)-N-[4-(3-pyridinyl)phenyl]benzeneacetamide Wnt-c59 - Physico-chemical Properties
| Molecular Formula | C25H21N3O |
| Molar Mass | 379.45 |
| Density | 1.198±0.06 g/cm3(Predicted) |
| Melting Point | >159°C (dec.) |
| Boling Point | 628.3±55.0 °C(Predicted) |
| Solubility | Soluble in DMSO (up to 7 mg/ml) or in Ethanol (up to 6 mg/mL) |
| Appearance | Off-white powder |
| Color | Tan |
| pKa | 13.78±0.70(Predicted) |
| Storage Condition | +2C to +8C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month. |
| In vitro study | Wnt-C59 (C59) inhibited the activity of PORCN at nanomolar concentrations. Wnt-C59(10 nM) action on HeLa cells transfected with WNT3A-V5 or WNT8A-V5 plasmids inhibited palmitosis-dependent Wnt-WLS interaction. Consistent with inhibition of Palmitate incorporation into WNT3A by Wnt-C59 (100 nM) in WNT3A-V5 transfected HeLa cells, PORCN activity was inhibited. Wnt-C59 (100 nM) action on PORCN-free HT1080 cells transfected with PORCN inhibited the activity of all mouse PORCN splice variants. Wnt-C59 inhibits mammalian PORCN acyltransferase activity at the nanomolar level and inhibits all human Wnts activation. Wnt-C59 treatment at a concentration that completely inhibited PORCN in vitro did not significantly inhibit the proliferation of the 46 cancer cell lines tested. Wnt-C59 treatment of NMuMG(NMG) cells significantly inhibited proliferation, comparable to ICG-001. Wnt-C59 acts on NMuMG(NMG) cells to inhibit threefold spheroid formation, which is dependent on the secretion of Wnt10b. Wnt-C59 inhibited more than 50% of human MDA-MB 231 cell proliferation. Wnt-C59 (Porcupine inhibitor) acts on mouse L-Wnt3a cells transfected with Flag-Porcupine, inhibiting [ |
| In vivo study | Wnt-C59 orally treated mice at a dose of 5 mg/kg alone maintained concentrations greater than 10-fold greater than the in vitro IC50 after at least 16 hours. Wnt-C59(10 mg/kg) inhibited MMTV-WNT1 tumor growth in female nude mice with orthotopic transplantation of MMTV-WNT1 independent tumors. Wnt-C59 (10 mg/kg) reduced Wnt pathway activity and MMTV-WNT1 tumor proliferation by reducing the expression of β-catenin targeted genes in female nude mice with orthotopic transplantation of MMTV-WNT1-independent tumors. Adult K14CREER/Wnt-C59 mice were treated topically on Rosa-SmoM2 (10%) for 4 weeks to reduce the dysplastic size of cells expressing smom2. |
4-(2-Methyl-4-pyridinyl)-N-[4-(3-pyridinyl)phenyl]benzeneacetamide Wnt-c59 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.635 ml | 13.177 ml | 26.354 ml |
| 5 mM | 0.527 ml | 2.635 ml | 5.271 ml |
| 10 mM | 0.264 ml | 1.318 ml | 2.635 ml |
| 5 mM | 0.053 ml | 0.264 ml | 0.527 ml |
Last Update：2024-01-02 23:10:35
4-(2-Methyl-4-pyridinyl)-N-[4-(3-pyridinyl)phenyl]benzeneacetamide Wnt-c59 - Reference Information
| biological activity | Wnt-C59 (C59) is a PORCN inhibitor that acts on Wnt3A mediated activation of luciferase driven by polyTCF binding site, with IC50 of 74 pM in HEK293 cells. |
| target | TargetValue Porcn (HEK293 cells ) 74 pM |
| Target | Value |
| Porcn (HEK293 cells) | 74 pM |
| in vitro study | Wnt-C59 (C59) inhibits PORCN enzyme activity at nanomolar concentration. Wnt-C59(10 nM) acts on HeLa cells transfected with WNT3A-V5 or WNT8A-V5 plasmids to inhibit Palmitoylation-dependent Wnt-WLS interaction. Wnt-C59 (100 nM) acts on HeLa cells transfected with WNT3A-V5 to inhibit the incorporation of Palmitate into WNT3A. Consistent with this, PORCN activity is inhibited. Wnt-C59 (100 nM) acts on PORCN-free HT1080 cells transfected with PORCN to inhibit the activity of all mouse PORCN splice variants. Wnt-C59 inhibits mammalian PORCN acyltransferase activity at nanomolar level and all human Wnts activation. The Wnt-C59 was treated with a concentration that completely inhibited PORCN in vitro and did not significantly inhibit the proliferation of 46 experimental cancer cell lines. Wnt-C59 treatment of NMuMG(NMG) cells significantly inhibited proliferation, similar to ICG-001. Wnt-C59 acts on NMuMG(NMG) cells and inhibits the formation of triploid spheres, which depends on the secretion of Wnt10b. Wnt-C59 inhibit the proliferation of more than 50% human MDA-MB 231 cells. Wnt-C59 (Porcupine inhibitor) acts on L-Wnt3a cells of mice transfected with Flag-Porcupine, inhibiting [ |
| in vivo study | Wnt-C59 the mice were treated orally at a dose of 5 mg/kg, and the concentration was maintained at more than 10 times that of IC50 in vitro after at least 16 hours. Wnt-C59(10 mg/kg) acted on female nude mice with independent tumor MMTV-WNT1 in situ transplantation to inhibit MMTV-WNT1 tumor growth. Wnt-C59 (10 mg/kg) acts on female nude mice with independent tumor MMTV-WNT1 transplanted in situ to reduce Wnt pathway activity and MMTV-WNT1 tumor proliferation by reducing the expression of β-catenin targeting gene. Wnt-C59(10%) local administration of adult K14CREER/Rosa-SmoM2 mice, treatment for 4 weeks, reduce the size of the abnormal development of cells expressing SmoM2. |
Last Update：2024-04-09 21:54:55
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