ICG-001
ICG-001拮抗Wnt/β-catenin/TCF介导的转录，并特异性结合到启动子结合蛋白（CBP)，IC50为3 μM，但不能结合到相关的转录共激活因子p300上。ICG-001 可诱导凋亡。
ICG-001 Chemical Structure
CAS: 780757-88-2 (relative stereochemistry); 847591-62-2 (absolute stereochemistry)
产品质控
批次：
纯度：
99.75%
99.75
常与ICG-001一起在实验中被使用的化合物
Foscenvivint和Auranofin协同抑制皮下异种移植小鼠模型中结肠癌的生长，并抑制肺转移小鼠模型中的转移。
Foscenvivint可改善Paclitaxel诱导的FOXM1表达和癌症干细胞(CSC)表型以及体外肿瘤启动能力的增加。
Foscenvivint和JQ1联合治疗可在H3.3K27M突变的弥漫性固有脑桥胶质瘤(DIPG)细胞系中诱导强烈的细胞毒性作用。
Foscenvivint和Pyrvinium加Bortezomib可降低RPMI-8226BR和KMS-11BR细胞系的细胞活力并增加细胞凋亡率。
Foscenvivint和Wnt-C59可抑制人胆管癌细胞的生长，并在异种移植模型和硫代乙胺模型中减少肿瘤面积和数量。
ICG-001相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| HK-2 | Function Assay | 10 µM | 3 h | reduced the expression of TGF-β1, α-SMA, and CTGF after treatment with HHE | 23690997 |
| HKC-8 | Function Assay | 10 µM | 24 h | abolishes β-catenin–mediated RAS induction | 25012166 |
| SH-SY5Y | Apoptosis Assay | 10 μM | 24 h | inhibits the neuroprotective effects of hypoxia against PrP (106-126)-mediated neuronal cell death | 23900566 |
| L3.6pl | Growth Inhibition Assay | 1-20 μM | 2/4/6 d | inhibits the cell growth in a dose-dependent manner | 25082960 |
| PANC-1 | Growth Inhibition Assay | 1-20 μM | 2/4/6 d | inhibits the cell growth in a dose-dependent manner | 25082960 |
| MiaPaCa-2 | Growth Inhibition Assay | 1-20 μM | 2/4/6 d | inhibits the cell growth in a dose-dependent manner | 25082960 |
| AsPC-1 | Growth Inhibition Assay | 1-20 μM | 2/4/6 d | inhibits the cell growth in a dose-dependent manner | 25082960 |
| SH-SY5Y | Apoptosis Assay | 50 μm | 24 h | blocks the protective effect of melatonin against PrP (106–126)-induced apoptotic signals | 25251028 |
| HepT1 | Apoptosis Assay | 0-100 μM | 24 h | IC50=34 μM | 23266718 |
| HuH6 | Apoptosis Assay | 0-100 μM | 24 h | IC50=39 μM | 23266718 |
| RLE-6TN | Function Assay | 2.5/5/7.5 μM | 48 h | inhibits TGF-β1-induced α-SMA induction and EMT | 22241478 |
| HKC-8 | Function Assay | 5/10/20 μM | 48 h | blocks β-catenin-driven gene expression | 21816937 |
| LoVo | Cytotoxicity assay | 10 uM | 72 hrs | Cytotoxicity against Wnt/beta-catenin signalling dependent human LoVo cells assessed as cell viability at 10 uM after 72 hrs by ATPlite assay | ChEMBL |
| NCI-H1703 | Function assay | 10 uM | 24 hrs | Inhibition of TNIK in human NCI-H1703 cells transfected with lentiviral vector 7TFP assessed as reduction of GSK3 inhibitor X activated TNIK-mediated Wnt/TCF/beta-catenin-dependent transcription at 10 uM after 24 hrs by luciferase reporter assay | ChEMBL |
| HCT116 | Cytotoxicity assay | 10 uM | 72 hrs | Cytotoxicity against Wnt/beta-catenin signalling dependent human HCT116 cells assessed as cell viability at 10 uM after 72 hrs by ATPlite assay | ChEMBL |
| MCF7 | Function Assay | 5 μm | inhibits leptin-mediated increased expression of Snail, Slug, and Zeb2 | 22270359 | |
| SW480 | Growth Inhibition Assay | 2-100 μM | IC50=5.8±0.68 μM | 15782138 | |
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, GI50 = 6.1 μM. | 24950489 | |
| HepG2 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay, GI50 = 12.7 μM. | 24950489 | |
| LoVo | Antiproliferative assay | 72 hrs | Antiproliferative activity against human LoVo cells after 72 hrs by MTT assay, GI50 = 15.6 μM. | 24950489 | |
| HT-29 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, GI50 = 17.2 μM. | 24950489 | |
| HT29 | Function assay | 24 hrs | Inhibition of Wnt signaling in human HT29 cells assessed as inhibition of beta-catenin-mediated Tcf/Lef transcriptional activity after 24 hrs by dual luciferase reporter gene assay relative to control, IC50 = 18.7 μM. | 24950489 | |
| SW480 | Function assay | Inhibition of CBP binding to beta-casein in human SW480 cells by immunoblot analysis, IC50 = 1.3 μM. | 23232060 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | ICG-001拮抗Wnt/β-catenin/TCF介导的转录，并特异性结合到启动子结合蛋白（CBP)，IC50为3 μM，但不能结合到相关的转录共激活因子p300上。ICG-001 可诱导凋亡。 | ||
|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | ICG-001 作用于TOPFLASH 时，IC50为3 μM，而对含突变TCF位点的相关报告基因结构, FOPFLASH没有作用效果。使用25μM ICG-001处理SW480 细胞8小时后，降低Survivin和 Cyclin D1 RNA和蛋白的稳定水平，这两者都可通过β-catenin上调。ICG-001 作用于转化细胞而不是正常结肠细胞，选择性诱导凋亡，降低结肠癌细胞生长。[1] ICG-001作用于presenilin-1突变细胞，可表型营救正常神经生长因子(NGF)诱导的神经元分化和神经轴突生长，强调TCF/β-catenin 信号通路在神经轴突生长和神经元分化中的重要性。[2] 最新研究显示 5μM ICG-001作用于MCF7细胞，抑制leptin诱导的EMT, 入侵和肿瘤干细胞球形成。[3] |
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|---|---|---|---|---|
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | SOX-2 / CD44 / Survivin / EGFR / FOXM1 / EZH2 / Vimentin pβ-catenin beta-catenin / F-actin ABC / Beta-catenin / E-cadherin / N-cadherin / MMP-9 / c-MYC / Actin / Histone H3 CCNB1 / Cyclin D1 |
|
25897700 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | ICG-001 水溶性类似物处理9周，降低42%结肠和小肠息肉的形成，和非甾体类抗炎试剂效果类似，是一贯治疗这种疾病模型的药物。在整个的处理期间观察不到明显的毒性。类似物按150 mg/kg 剂量静脉注射处理SW620裸鼠肿瘤衰退移植瘤模型，处理19天，显著降低肿瘤体积，没有死亡，体重也没有降低。[1] ICG-001 每天按5 mg/kg剂量处理小鼠，显著抑制beta-catenin信号，且降低 Bleomycin诱导的肺纤维化，同时保护上皮细胞。[4] |
|
|---|---|---|
| 动物实验 | Animal Models | C57BL/6和裸鼠肿瘤模型 |
| Dosages | 20 mg/kg | |
| Administration | 腹腔注射 | |
化学信息&溶解度
| 分子量 | 548.63 | 分子式 | C33H32N4O4 |
| CAS号 | 780757-88-2 (relative stereochemistry); 847591-62-2 (absolute stereochemistry) | SDF | Download ICG-001 SDF |
| Smiles | C1CN(C2CN(C(=O)C(N2C1=O)CC3=CC=C(C=C3)O)CC4=CC=CC5=CC=CC=C54)C(=O)NCC6=CC=CC=C6 | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 30 mg/mL ( (54.68 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 1:
If the compound is stored in DMSO at -80, how long would it be stable? For cell culture, how long should I change for the fresh medium with ICG-001?
回答：
The product in DMSO solution can be stored at 4 degree for 1 week and -20 degree for 1 month. The best storage condition is solid powder, even at -80 the solution is not stable enough for long term storage. For cell culture, you need change medium every 48h.
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