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Submit ReviewWnt-C59
说明： Highly potent PORCN inhibitor
化学名： 4-(2-Methyl-4-pyridinyl)-N-[4-(3-pyridinyl)phenyl]benzeneacetamide
纯度： ≥99% (HPLC)
生物活性 for Wnt-C59
Wnt-C59 is a highly potent inhibitor of the MBOAT (membrane-bound O-acyltranferase) family member, Porcupine (PORCN) (IC50 = 74 pM), that mediates WNT palmitoylation and secretion. Wnt-C59 potently inhibits the processing of both canonical (1, 2, 3a, 6, 7b, 8a, 9a, 9b, 10) and non-canonical (4, 5a, 11, 16) Wnt subtypes. Wnt-C59 blocks progression of mammary tumors in MMTV-WNT1 transgenic mice and downregulates Wnt/β-catenin target genes. Wnt-C59-treated tumors show a decrease in β-catenin, CyclinD1 and c-Myc. Wnt-C59 induces cardiomyocyte differentiation from human iPSCs following culture with CHIR 99021 (Cat. No. 4423). Wnt-C59 efficiently induces neural differentiation of CTIP2+/COUP-TF1- cells from PSCs in culture. When grafted into the cortex of adult mice, Wnt-C59-treated cells develop abundant axonal fiber extensions toward the spinal cord. The compound has also been used in protocols to generate β cells from human PSCs. Cell permeable and orally bioavailable.
化合物库 for Wnt-C59
Wnt-C59 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Stem Cell Library. 了解 Tocris 化合物库的更多信息。
技术数据 for Wnt-C59
| 分子量 | 379.45 |
| 公式 | C25H21N3O |
| 储存 | Store at -20°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 1243243-89-1 |
| PubChem ID | 57519544 |
| InChI Key | KHZOJCQBHJUJFY-UHFFFAOYSA-N |
| Smiles | O=C(CC3=CC=C(C4=CC=NC(C)=C4)C=C3)NC1=CC=C(C2=CC=CN=C2)C=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Wnt-C59
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 7.59 | 20 | |
| ethanol | 7.59 | 20 |
制备储备液 for Wnt-C59
以下数据基于产品分子量 379.45。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 13.18 mL | 65.88 mL | 131.77 mL |
| 1 mM | 2.64 mL | 13.18 mL | 26.35 mL |
| 2 mM | 1.32 mL | 6.59 mL | 13.18 mL |
| 10 mM | 0.26 mL | 1.32 mL | 2.64 mL |
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产品说明书 for Wnt-C59
参考文献 for Wnt-C59
参考文献是支持产品生物活性的出版物。
Proffitt et al (2013) Pharmacological inhibition of the Wnt acyltransferase PORCN prevents growth of WNT-driven mammary cancer. Cancer Res. 73 502 PMID: 23188502
Wend et al (2013) WNT10B/β-catenin signalling induces HMGA2 and proliferation in metastatic triple-negative breast cancer. EMBO Mol.Med. 5 264 PMID: 23307470
Youssef et al (2012) Adult interfollicular tumour-initiating cells are reprogrammed into an embryonic hair follicle progenitor-like fate during basal cell carcinoma initiation. Nat. Cell Biol. 14 1282 PMID: 23178882
Burridge et al (2014) Chemically defined generation of human cardiomyocytes. Nat.Methods 11 855 PMID: 24930130
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 PMID: 26941358
Jiang et al (2021) Generation of pancreatic progenitors from human pluripotent stem cells by small molecules. Stem Cell Rep. 16 2395 PMID: 34450037
If you know of a relevant reference for Wnt-C59, please let us know.
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关键词: Wnt-C59, Wnt-C59 supplier, Highly, potent, porcn, inhibitors, inhibits, membrane-bound, O-acyltransferase, MBOAT, Wnt, signaling, pathways, WntC59, PORCN, Cardiomyocyte, Stem, Cells, ESCs, and, iPSC, Organoids, 5148, Tocris Bioscience
49 篇 Wnt-C59 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Wnt-C59 的部分引用包括：
Timothy C et al (2022) Contribution of Trp63CreERT2-labeled cells to alveolar regeneration is independent of tuft cells. Elife 11 PMID: 36129169
Guanghao et al (2022) Single-cell sequencing reveals lineage-specific dynamic genetic regulation of gene expression during human cardiomyocyte differentiation. PLoS Genet 18 e1009666 PMID: 35061661
Olivier et al (2022) Paraxial mesoderm organoids model development of human somites. Elife 11 PMID: 35088712
Wenqi et al (2022) Reengineering Ponatinib to Minimize Cardiovascular Toxicity. Cancer Res 82 2777-2791 PMID: 35763671
Nathalie et al (2022) Virus-induced inhibition of cardiac pacemaker channel HCN4 triggers bradycardia in human-induced stem cell system. Cell Mol Life Sci 79 440 PMID: 35864219
Gordana et al (2022) STK25 inhibits PKA signaling by phosphorylating PRKAR1A. Cell Rep 40 111203 PMID: 35977512
Aaron M et al (2022) SOX transcription factors direct TCF-independent WNT/β-catenin responsive transcription to govern cell fate in human pluripotent stem cells. Cell Rep 40 111247 PMID: 36001974
Jose E et al (2022) Time-regulated transcripts with the potential to modulate human pluripotent stem cell-derived cardiomyocyte differentiation. Stem Cell Res Ther 13 437 PMID: 36056380
Anna M et al (2022) Functional microvascularization of human myocardium in vitro. Cell Rep Methods 2 100280 PMID: 36160044
Liang et al (2019) Canonical Wnt signaling promotes pacemaker cell specification of cardiac mesodermal cells derived from mouse and human embryonic stem cells. Stem Cells 38 352 PMID: 31648393
Rebecca L et al (2019) Wnt family member 4 (WNT4) and WNT3A activate cell-autonomous Wnt signaling independent of porcupine O-acyltransferase or Wnt secretion. J Biol Chem 294 19950-19966 PMID: 31740580
Kumi et al (2019) Engineering of human cardiac muscle electromechanically matured to an adult-like phenotype. Nat Protoc 14 2781-2817 PMID: 31492957
Fan et al (2019) Long-Term Stability and Differentiation Potential of Cryopreserved cGMP-Compliant Human Induced Pluripotent Stem Cells. Int J Mol Sci 21 PMID: 31877913
Nathalie et al (2020) 4,4'-Diisothiocyanato-2,2'-Stilbenedisulfonic Acid (DIDS) Modulates the Activity of KCNQ1/KCNE1 Channels by an Interaction with the Central Pore Region. Cell Physiol Biochem 54 321-332 PMID: 32259418
Mark et al (2020) Reengineering an Antiarrhythmic Drug Using Patient hiPSC Cardiomyocytes to Improve Therapeutic Potential and Reduce Toxicity. Cell Stem Cell 27 813-821.e6 PMID: 32931730
Melanie et al (2020) Wnt regulates amino acid transporter Slc7a5 and so constrains the integrated stress response in mouse embryos. EMBO Rep 21 e48469 PMID: 31789450
Yoav et al (2020) Systematic Comparison of High-throughput Single-Cell and Single-Nucleus Transcriptomes during Cardiomyocyte Differentiation. Sci Rep 10 1535 PMID: 32001747
Andrew R et al (2020) Modeling polymorphic ventricular tachycardia at rest using patient-specific induced pluripotent stem cell-derived cardiomyocytes. EBioMedicine 60 103024 PMID: 32980690
Hui et al (2020) 16p11.2 microdeletion imparts transcriptional alterations in human iPSC-derived models of early neural development. Elife 9 PMID: 33169669
Nilesh J et al (2020) The role of cathepsin D in the pathophysiology of heart failure and its potentially beneficial properties: a translational approach. Eur J Heart Fail 22 2102-2111 PMID: 31797504
Walter C et al (2020) Accelerated differentiation of human pluripotent stem cells into neural lineages via an early intermediate ectoderm population. Stem Cells 38 1400-1408 PMID: 32745311
Hui et al (2020) Metabolic Maturation Media Improve Physiological Function of Human iPSC-Derived Cardiomyocytes. Cell Rep 32 107925 PMID: 32697997
Yulia V et al (2023) Engineered cardiac tissue model of restrictive cardiomyopathy for drug discovery. Cell Rep Med 4 100976 PMID: 36921598
Tim et al (2023) A pesticide and iPSC dopaminergic neuron screen identifies and classifies Parkinson-relevant pesticides. Nat Commun 14 2803 PMID: 37193692
Guiscard et al (2023) Optimized synthesis and pharmacological evaluation of HCN channel inhibitor EC18. Arch Pharm (Weinheim) 356 e2200665 PMID: 36949271
Sergio et al (2023) IGF-1 boosts mitochondrial function by a Ca2+ uptake-dependent mechanism in cultured human and rat cardiomyocytes. Front Physiol 14 1106662 PMID: 36846332
Pfeiffer et al (2018) Cardiogenic programming of human pluripotent stem cells by dose-controlled activation of EOMES. Nat Commun 9 440 PMID: 29382828
Shafa et al (2018) Human-Induced Pluripotent Stem Cells Manufactured Using a Current Good Manufacturing Practice-Compliant Process Differentiate Into Clinically Relevant Cells From Three Germ Layers. Front Med (Lausanne) 5 69 PMID: 29600249
Hoes et al (2018) Iron deficiency impairs contractility of human cardiomyocytes through decreased mitochondrial function. Eur J Heart Fail 20 910 PMID: 29484788
Montefiori et al (2018) A promoter interaction map for cardiovascular disease genetics. Elife 7 PMID: 29988018
Pavlovic et al (2018) A Comparative Assessment of Human and Chimpanzee iPSC-derived Cardiomyocytes with Primary Heart Tissues. Sci Rep 8 15312 PMID: 30333510
Sharma et al (2018) Stage-specific Effects of Bioactive Lipids on Human iPSC Cardiac Differentiation and Cardiomyocyte Proliferation. Sci Rep 8 6618 PMID: 29700394
Jiang et al (2018) An Ultrasensitive Calcium Reporter System via CRISPR-Cas9-Mediated Genome Editing in Human Pluripotent Stem Cells. iScience 9 27 PMID: 30368079
Nigmatullina et al (2017) Id2 controls specification of Lgr5+ intestinal stem cell progenitors during gut development. EMBO J 36 869 PMID: 28077488
Piccini et al (2017) Adrenergic Stress Protection of Human iPS Cell-Derived Cardiomyocytes by Fast Kv7.1 Recycling. Front Physiol 8 705 PMID: 28959214
Guiscard et al (2015) Universal cardiac induction of human pluripotent stem cells in two and three-dimensional formats: implications for in vitro maturation. Stem Cells 33 1456-69 PMID: 25639979
Alain et al (2021) Oxygen Is an Ambivalent Factor for the Differentiation of Human Pluripotent Stem Cells in Cardiac 2D Monolayer and 3D Cardiac Spheroids. Int J Mol Sci 22 PMID: 33440843
Kenneth R et al (2021) Isolation of human ESC-derived cardiac derivatives and embryonic heart cells for population and single-cell RNA-seq analysis. STAR Protoc 2 100339 PMID: 33644774
David E et al (2021) Functional dynamic genetic effects on gene regulation are specific to particular cell types and environmental conditions. Elife 10 PMID: 33988505
Matthew et al (2021) Dynamic effects of genetic variation on gene expression revealed following hypoxic stress in cardiomyocytes. Elife 10 PMID: 33554857
Joseph C et al (2021) Massive expansion and cryopreservation of functional human induced pluripotent stem cell-derived cardiomyocytes. STAR Protoc 2 100334 PMID: 33615277
Ha Neui et al (2021) The thrombin receptor links brain derived neurotrophic factor to neuron cholesterol production, resiliency and repair after spinal cord injury. Neurobiol Dis 152 105294 PMID: 33549720
Rudolf A et al (2021) Selenoprotein DIO2 Is a Regulator of Mitochondrial Function, Morphology and UPRmt in Human Cardiomyocytes. Int J Mol Sci 22 PMID: 34769334
Nibaldo C et al (2021) Selective Surface and Intraluminal Localization of Wnt Ligands on Small Extracellular Vesicles Released by HT-22 Hippocampal Neurons. Front Cell Dev Biol 9 735888 PMID: 34722516
Yong et al (2021) A Comparative Assessment of Marker Expression Between Cardiomyocyte Differentiation of Human Induced Pluripotent Stem Cells and the Developing Pig Heart. Stem Cells Dev 30 374-385 PMID: 33599158
Rostovskaya et al (2019) Capacitation of human naïve pluripotent stem cells for multi-lineage differentiation. Development 146 PMID: 30944104
Ward and Gilad (2019) A generally conserved response to hypoxia in iPSC-derived cardiomyocytes from humans and chimpanzees. Elife 8 PMID: 30958265
Bernatik et al (2017) A Novel Role for the BMP Antagonist Noggin in Sensitizing Cells to Non-canonical Wnt-5a/Ror2/Disheveled Pathway Activation. Front Cell Dev Biol 5 47 PMID: 28523267
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The role of Wnt signaling in chemotherapy-induced apoptosis..
By
MARINA KOUTSIOUMPA on 06/10/2021
分析类型： In Vitro
种属： Human
Pancreatic cancer cells were incubated for pretreated for 2 hours with WNT-C59 followed by conventional chemotherapeutics. Wnt inhibition had an additive effect on cancer cell’s viability upon 3 days of treatment.