Wnt-C59 (C59)

製品コードS7037 バッチS703702

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C25H21N3O
分子量 379.45 CAS No. 1243243-89-1
Solubility (25°C)* 体外 DMSO 76 mg/mL (200.28 mM)
Ethanol 19 mg/mL (50.07 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 95% Corn oil
3.8mg/ml Taking the 1 mL working solution as an example, add 50 μL of 76 mg/mL clarified DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG 300 5%Tween80 50% ddH2O
3.8mg/ml Taking the 1 mL working solution as an example, add 50 μL of 76 mg/ml clear DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween-80 to the above system, mix evenly to clarify it; Then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

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。
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]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 NMuMG (NMG) and MDA-MB 231 cells
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.
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

カスタマーフィードバック

, , 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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。