受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C25H21N3O |
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分子量 | 379.45 | CAS No. | 1243243-89-1 | ||||
Solubility (25°C)* | 体外 | DMSO | 76 mg/mL (200.28 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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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. |
製品説明 | Wnt-C59 (C59) はルシフェラーゼ (luciferase) を駆動する多量体 TCF 結合部位の Wnt3A を介した活性化に対する PORCN 阻害剤 (HEK293 細胞での IC50= 74 pM) です。 |
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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] |
細胞アッセイ | 細胞株 | NMuMG (NMG) and MDA-MB 231 cells |
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濃度 | -- | |
反応時間 | 48 hours | |
実験の流れ | Seed cells at a concentration of 4×103/well in 100 μL culture medium containing various amouts of Wnt-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. |
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動物実験 | 動物モデル | Female nude mice orthotopically transplanted with independent MMTV-WNT1 tumors |
投薬量 | 10 mg/kg | |
投与方法 | orally |
, , 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]
PIBF1 regulates trophoblast syncytialization and promotes cardiovascular development [ Nat Commun, 2024, 15(1):1487] | PubMed: 38374152 |
Ultrasound Mediated Polymerization for Cell Delivery, Drug Delivery, and 3D Printing [ Small Methods, 2024, e2301197.] | PubMed: 38376006 |
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 |
ER stress and lipid imbalance drive diabetic embryonic cardiomyopathy in an organoid model of human heart development [ Stem Cell Reports, 2024, S2213-6711(24)00006-7] | PubMed: 38335962 |
Coactivator condensation drives cardiovascular cell lineage specification [ Sci Adv, 2024, 10(11):eadk7160] | PubMed: 38489358 |
Biohybrid 3D Printing of a Tissue-Sensor Platform for Wireless, Real-Time, and Continuous Monitoring of Drug-Induced Cardiotoxicity [ Adv Mater, 2023, 35(11):e2208983] | PubMed: 36528341 |
Electric-Field-Driven Printed 3D Highly Ordered Microstructure with Cell Feature Size Promotes the Maturation of Engineered Cardiac Tissues [ Adv Sci (Weinh), 2023, 10(11):e2206264] | PubMed: 36782337 |
Single-swap editing for the correction of common Duchenne muscular dystrophy mutations [ Mol Ther Nucleic Acids, 2023, 32:522-535] | PubMed: 37215149 |
Combined lineage tracing and scRNA-seq reveals unexpected first heart field predominance of human iPSC differentiation [ Elife, 2023, 12e80075] | PubMed: 37284748 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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