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ETC-159

Name: ETC-159
Brand: TargetMol
SKU: T4043
Price: 258 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.30%

货号 T4043Cas号 1638250-96-0

别名 ETC-1922159, ETC159, ETC 159

ETC-159 (ETC-1922159) 是一种具有口服活性的，有效 PORCN 抑制剂。抑制β-catenin 报告基因活性的 IC50值为2.9 nM。

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ETC-159

一键复制产品信息

很棒

纯度: 99.30%

货号 T4043 别名 ETC-1922159, ETC159, ETC 159Cas号 1638250-96-0

ETC-159 (ETC-1922159) 是一种具有口服活性的，有效 PORCN 抑制剂。抑制β-catenin 报告基因活性的 IC50值为2.9 nM。

规格	价格	库存
2 mg	¥ 258	现货
5 mg	¥ 397	现货
10 mg	¥ 663	现货
25 mg	¥ 1,230	现货
50 mg	¥ 1,980	现货
100 mg	¥ 3,730	现货
1 mL x 10 mM (in DMSO)	¥ 455	现货

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COA HNMR LCMS 产品操作手册

产品介绍

ETC-159 AI Summary

ETC-159 exhibits potent inhibitory activity against porcupine enzymes, demonstrating significant bioactivity across various cell types. Remarkably, it inhibits Wnt secretion by suppressing beta-catenin reporter activity in human HEK293 cells with an IC50 value of 2.9 nM, and shows inhibitory effects on mouse and xenopus porcupine expressed in human HT1080 cells, with IC50 values of 18.1 nM and 70.0 nM, respectively. The compound also displays promising antitumor activity, effectively inhibiting tumor growth by 90.0% in human HPAF2 cells xenografted in Balb/c mice at a dose of 100 mg/kg. Additionally, ETC-159 has exhibited antiviral activity against SARS-CoV-2 in various assays. It inhibited the cytotoxicity of Caco-2 cells at 10 µM after 48 hours with an inhibition rate of -5.76%, and demonstrated inhibitory activity against the SARS-CoV-2 3CL-Pro protease at 20 µM with inhibition percentages of 8.02% and 11.27%. Despite these promising findings, its inhibitory effects varied when tested on VERO-6 cells, showing a range from -0.02% to -0.15%. ETC-159 also inhibits human HDAC6, displaying 41.83% inhibition with a commercial peptide substrate, although showing minimal activity with a custom substrate (-1.95%). The compound is orally bioavailable with 100.0% in mice at a dosage of 10 mg/kg and also exhibits strong antitumor activity against human HEK293 cells xenografted in Sprague-Dawley mice, resulting in a tumor growth inhibition of 94.0% at the same dosage..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	ETC-159 (ETC-1922159) is a potent, orally available PORCN inhibitor. It inhibits β-catenin reporter activity with an IC50 of 2.9 nM.
靶点活性	β-catenin:2.9 nM.
别名	ETC-1922159, ETC159, ETC 159

化学信息

分子量	391.38
分子式	C₁₉H₁₇N₇O₃
CAS No.	1638250-96-0
Smiles	Cn1c2ncn(CC(=O)Nc3ccc(nn3)-c3ccccc3)c2c(=O)n(C)c1=O
密度	1.47 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 55 mg/mL (140.53 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.11 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.5551 mL	12.7753 mL	25.5506 mL	127.7531 mL
5 mM	0.5110 mL	2.5551 mL	5.1101 mL	25.5506 mL
10 mM	0.2555 mL	1.2775 mL	2.5551 mL	12.7753 mL
20 mM	0.1278 mL	0.6388 mL	1.2775 mL	6.3877 mL
50 mM	0.0511 mL	0.2555 mL	0.5110 mL	2.5551 mL
100 mM	0.0256 mL	0.1278 mL	0.2555 mL	1.2775 mL