Wnt-C59 (C59)

製品コードS7037 バッチS703704

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)
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）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG 300 5%Tween80 50% ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 3.800mg/ml (10.01mM) 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. At 10 nM, it blocks the palmitoylation-dependent Wnt–WLS interaction in HeLa cells transfected with either WNT3A-V5 or WNT8A-V5 plasmids. This compound (100 nM) prevents incorporation of palmitate into WNT3A in HeLa cells transfected with WNT3A-V5, consistent with inhibition of PORCN activity. It (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. It 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. It inhibits sphere formation by threefold in NMuMG (NMG) cells, which is dependent on Wnt10b-secretion. This compound inhibits proliferation of human MDA-MB 231 cells by >50%. [2] As a Porcupine inhibitor, it blocks radiolabel incorporation of [125I]iodo-pentadecanoate in mouse L-Wnt3a cells transfected with Flag-Porcupine. [3]
in vivo Wnt-C59 (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. At 10 mg/kg, it prevents growth of MMTV-WNT1 tumors in female nude mice orthotopically transplanted with independent MMTV-WNT1 tumors. This compound also decreases Wnt pathway activity and proliferation in such tumors, as evident by reduced expression of β-catenin target genes. [1] When topically administered at 10% for 4 weeks, it reduces the size of dysplasia in 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 amounts of Wnt-C59 (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

参考

  • https://pubmed.ncbi.nlm.nih.gov/23188502/
  • https://pubmed.ncbi.nlm.nih.gov/23307470/
  • https://pubmed.ncbi.nlm.nih.gov/23416332/
  • https://pubmed.ncbi.nlm.nih.gov/23178882/

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]

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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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