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Stem Cells & Wnt
Wnt/beta-catenin inhibitor
-
Apoptosis related activator
-
Epigenetic Reader Domain inhibitor
ICG-001
僅限科研使用
ICG-001
ICG-001拮抗Wnt/β-catenin/TCF介導(dǎo)的轉(zhuǎn)錄，并特異性結(jié)合到啟動(dòng)子結(jié)合蛋白（CBP)，IC50為3 μM，但不能結(jié)合到相關(guān)的轉(zhuǎn)錄共激活因子p300上。ICG-001 可誘導(dǎo)凋亡。
ICG-001 Chemical Structure
CAS: 780757-88-2 (relative stereochemistry); 847591-62-2 (absolute stereochemistry)
產(chǎn)品質(zhì)控
批次：
純度：
99.75%
99.75
常與ICG-001一起在實(shí)驗(yàn)中被使用的化合物
Foscenvivint和Auranofin協(xié)同抑制皮下異種移植小鼠模型中結(jié)腸癌的生長(zhǎng)，并抑制肺轉(zhuǎn)移小鼠模型中的轉(zhuǎn)移。
Foscenvivint和JQ1聯(lián)合治療可在H3.3K27M突變的彌漫性固有腦橋膠質(zhì)瘤(DIPG)細(xì)胞系中誘導(dǎo)強(qiáng)烈的細(xì)胞毒性作用。
Foscenvivint和Pyrvinium加Bortezomib可降低RPMI-8226BR和KMS-11BR細(xì)胞系的細(xì)胞活力并增加細(xì)胞凋亡率。
ICG-001相關(guān)產(chǎn)品
| 相關(guān)靶點(diǎn) | WNT β-catenin Wnt/β-catenin | 點(diǎn)擊展開(kāi) |
|---|---|---|
| 相關(guān)產(chǎn)品 | IWR-1-endo IWP-2 SKL2001 BML-284 (Wnt agonist 1) Foscenvivint (PRI-724) FH535 Salinomycin (from Streptomyces albus) PNU-74654 LF3 KYA1797K KY02111 iCRT3 Adavivint (SM04690) MSAB IQ-1 Isoquercitrin iCRT14 CCT251545 JW55 Methyl Vanillate WAY-262611 M435-1279 JW74 | 點(diǎn)擊展開(kāi) |
| 相關(guān)化合物庫(kù) | 激酶抑制劑庫(kù) FDA藥物庫(kù) 干細(xì)胞小分子化合物庫(kù) GPCR小分子化合物庫(kù) 干細(xì)胞分化化合物庫(kù) | 點(diǎn)擊展開(kāi) |
相關(guān)信號(hào)通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)信息(PMID) |
|---|---|---|---|---|---|
| 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 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | ICG-001拮抗Wnt/β-catenin/TCF介導(dǎo)的轉(zhuǎn)錄，并特異性結(jié)合到啟動(dòng)子結(jié)合蛋白（CBP)，IC50為3 μM，但不能結(jié)合到相關(guān)的轉(zhuǎn)錄共激活因子p300上。ICG-001 可誘導(dǎo)凋亡。 | ||
|---|---|---|---|
| 靶點(diǎn) |
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| 體外研究(In Vitro) | ||||||
| 體外研究活性 | ICG-001 作用于TOPFLASH 時(shí)，IC50為3 μM，而對(duì)含突變TCF位點(diǎn)的相關(guān)報(bào)告基因結(jié)構(gòu), FOPFLASH沒(méi)有作用效果。使用25μM ICG-001處理SW480 細(xì)胞8小時(shí)后，降低Survivin和 Cyclin D1 RNA和蛋白的穩(wěn)定水平，這兩者都可通過(guò)β-catenin上調(diào)。ICG-001 作用于轉(zhuǎn)化細(xì)胞而不是正常結(jié)腸細(xì)胞，選擇性誘導(dǎo)凋亡，降低結(jié)腸癌細(xì)胞生長(zhǎng)。[1] ICG-001作用于presenilin-1突變細(xì)胞，可表型營(yíng)救正常神經(jīng)生長(zhǎng)因子(NGF)誘導(dǎo)的神經(jīng)元分化和神經(jīng)軸突生長(zhǎng)，強(qiáng)調(diào)TCF/β-catenin 信號(hào)通路在神經(jīng)軸突生長(zhǎng)和神經(jīng)元分化中的重要性。[2] 最新研究顯示 5μM ICG-001作用于MCF7細(xì)胞，抑制leptin誘導(dǎo)的EMT, 入侵和腫瘤干細(xì)胞球形成。[3] |
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| 實(shí)驗(yàn)圖片 | 檢測(cè)方法 | 檢測(cè)指標(biāo) | 實(shí)驗(yàn)圖片 | PMID | ||
| Western blot |
SOX-2 / CD44 / Survivin / EGFR / FOXM1 / EZH2 / Vimentin
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