Wnt-C59 (C59)

製品コードS7037 バッチS703704

印刷

化学情報

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 1 40%PEG 300 2 5%Tween80 3 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. 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%. As a Porcupine inhibitor, it blocks radiolabel incorporation of [¹²⁵I]iodo-pentadecanoate in mouse L-Wnt3a cells transfected with Flag-Porcupine.
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. When topically administered at 10% for 4 weeks, it reduces the size of dysplasia in SmoM2-expressing cells in adult K14CREER/Rosa–SmoM2 mice.

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/

+ 展开

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：

Modeling early human heart development using an iPSC-based 3D bioprinted model of embryonic heart tube [ Nat Commun, 2026, 17(1):5689]	PubMed: 42031752
Drug-induced gastrointestinal toxicity and barrier integrity: cytoskeleton-mediated impairment in a clinically relevant human intestinal epithelium model [ Exp Mol Med, 2026, 58(2):487-500]	PubMed: 41680471
Unbiased cleavage site prediction uncovers viral antagonism of host innate immunity by SARS-CoV-2 3C-like protease [ JCI Insight, 2026, 11(4)e185739]	PubMed: 41729072
Sustained β-catenin activation via GSK3 inhibition promotes direct fibroblast-to-cardiomyocyte reprogramming [ J Biol Chem, 2026, S0021-9258(26)00330-3]	PubMed: 41999895
Iron deficiency drives pathological cardiac remodeling and diastolic dysfunction associated with inhibition of AMPK-mTORC1 signaling [ Cardiovasc Pathol, 2026, 83:107828]	PubMed: 42019832
Spatial relationships between vinculin tension and actin at cell adhesions define cell colony positioning and identity [ Biophys J, 2026, 125(7):1583-1596]	PubMed: 41691376
DHX15 overexpression suppresses colorectal cancer cell line proliferation [ Oncol Lett, 2026, 31(2):80]	PubMed: 41635546
Generation of the human induced pluripotent stem cell (hiPSC) line AUMCi015-A from a heterozygous carrier of the LMNA p.Q493X rare pathogenic variant [ Stem Cell Res, 2026, 92:103962]	PubMed: 41797063
MYC ecDNA promotes intratumour heterogeneity and plasticity in PDAC [ Nature, 2025, 10.1038/s41586-025-08721-9]	PubMed: 40074906
Epithelial WNT secretion drives niche escape of developing gastric cancer [ Mol Cancer, 2025, 25(1):1]	PubMed: 41398956

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。