| Identification | Back Directory | [Name]
Wnt-C59 | [CAS]
1243243-89-1 | [Synonyms]
C59
CS-876
Wnt-C59
Wnt-C59 (C59)
Wnt-C59, >=98%
Wnt-C59 USP/EP/BP
WNT C59; C59;WNTC59
WNT-C59 (C59);WNT C59;C59
Porcn Inhibitor II, C59 - CAS 1243243-89-1 - Calbiochem
2-[4-(2-Methyl-4-pyridyl)phenyl]-N-[4-(3-pyridyl)phenyl]acetamide
Wnt-C59, 98%, a potent PORCN enzymatic activity and Wnt inhibitor
4-(2-Methyl-4-pyridinyl)-N-[4-(3-pyridinyl)phenyl]benzeneacetamide
Benzeneacetamide, 4-(2-methyl-4-pyridinyl)-N-[4-(3-pyridinyl)phenyl]-
2-(4-(2-Methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetaMide
4-(2-Methyl-4-pyridinyl)-N-[4-(3-pyridinyl)phenyl]benzeneacetamide Wnt-c59 | [Molecular Formula]
C25H21N3O | [MDL Number]
MFCD22201167 | [MOL File]
1243243-89-1.mol | [Molecular Weight]
379.45 |
| Chemical Properties | Back Directory | [Melting point ]
>159°C (dec.) | [Boiling point ]
628.3±55.0 °C(Predicted) | [density ]
1.198±0.06 g/cm3(Predicted) | [storage temp. ]
+2C to +8C | [solubility ]
Soluble in DMSO (up to 7 mg/ml) or in Ethanol (up to 6 mg/mL) | [form ]
Off-white powder | [pka]
13.78±0.70(Predicted) | [color ]
Tan | [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. | [InChI]
InChI=1S/C25H21N3O/c1-18-15-22(12-14-27-18)20-6-4-19(5-7-20)16-25(29)28-24-10-8-21(9-11-24)23-3-2-13-26-17-23/h2-15,17H,16H2,1H3,(H,28,29) | [InChIKey]
KHZOJCQBHJUJFY-UHFFFAOYSA-N | [SMILES]
C1(CC(NC2=CC=C(C3=CC=CN=C3)C=C2)=O)=CC=C(C2C=CN=C(C)C=2)C=C1 |
| Hazard Information | Back Directory | [Description]
Wnt-C59 (1243243-89-1) is a potent (IC50 = 74 pmol/L) inhibitor of Porcupine (PORCN), a Wnt-acyltransferase.1 Blockage of Wnt-acyltransferase prevents secretion of all Wnt isoforms.? It was able to block progression of mammary tumors in MMTV-WNT1 transgenic mice.1? Wnt-C59 strongly inhibited the growth of intestinal neoplasia in RZ-mutant mice.2? Wnt-C59 was able to efficiently differentiate pluripotent stem cells into cortical neurons (CTIP2+/COUP-TF1).3? Wnt-C59 was also able to dramatically attenuate kidney fibrosis via inhibition of collagen mRNA expression and expression of inflammatory cytokines.4 | [Uses]
Wnt-C59 is a porcupine homolog – Drosophila (PORCN) inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase. | [in vivo]
Wnt-C59 displays good bioavailability in mice. Wnt-C59 blocks progression of mammary tumors in MMTV-WNT1 transgenic mice while downregulating Wnt/β-catenin target genes[1]. Wnt-C59 has the potential to eradicate cancer stem cells in human tumors. Wnt-C59 inhibits stemness properties of NPC cells in a dosage-dependent manner by arresting sphere formation in both HNE1 and SUNE1 cells[2]. | [storage]
-20°C | [References]
1) Proffitt et al. (2013), Pharmacological Inhibition of the Wnt Acyltransferase PORCN Prevents Growth of Wnt-Driven Mammary Cancer; Cancer Res., 73 502
2) Koo et al. (2015), Porcupine inhibitor suppresses paracrine Wnt-driven growth of Rnf43;Znrf3-mutant neoplasia; Proc. Natl. Acad. Sci.USA, 112 7548
3) Motono et al. (2016), Wnt-C59, a Small-Molecule Wnt Inhibitor, Efficiently Induces Anterior Cortex That Includes Cortical Motor Neurons From Human Pluripotent Stem Cells; Stem Cells Transl.Med., 5 552
4) Madan et al. (2016), Experimental inhibition of porcupine-mediated Wnt O-acylation attenuates kidney fibrosis; Kidney Int., 89 1062 |
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