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Formula | C25H21N3O |
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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) |
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* <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.) |
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. | ||
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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] |
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Animal Study: |
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, , 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]
Bioprinting-assisted Tissue Assembly for Structural and Functional Modulation of Engineered Heart Tissue Mimicking Left Ventricular Myocardial Fiber Orientation [ Adv Mater, 2024, e2400364.] | PubMed: 38717016 |
Tumor Explants Elucidate a Cascade of Paracrine SHH, WNT, and VEGF Signals Driving Pancreatic Cancer Angiosuppression [ Cancer Discov, 2024, 14(2):348-361] | PubMed: 37966260 |
PIBF1 regulates trophoblast syncytialization and promotes cardiovascular development [ Nat Commun, 2024, 15(1):1487] | PubMed: 38374152 |
N-Acetyltransferase 10 represses Uqcr11 and Uqcrb independently of ac4C modification to promote heart regeneration [ Nat Commun, 2024, 15(1):2137] | PubMed: 38459019 |
Hypoxia and TNF-alpha modulate extracellular vesicle release from human induced pluripotent stem cell-derived cardiomyocytes [ J Extracell Vesicles, 2024, 13(11):e70000] | PubMed: 39508403 |
Ultrasound Mediated Polymerization for Cell Delivery, Drug Delivery, and 3D Printing [ Small Methods, 2024, e2301197.] | PubMed: 38376006 |
Cardiac delivery of modified mRNA using lipid nanoparticles: Cellular targets and biodistribution after intramyocardial administration [ J Control Release, 2024, 369:734-745] | PubMed: 38604385 |
The nutrient sensor CRTC and Sarcalumenin/thinman represent an alternate pathway in cardiac hypertrophy [ Cell Rep, 2024, 43(8):114549] | PubMed: 39093699 |
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 |
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