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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

ICG-001 Chemical Structure

CAS: 780757-88-2 (relative stereochemistry); 847591-62-2 (absolute stereochemistry)

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1377.83 現(xiàn)貨
5mg 976.49 現(xiàn)貨
25mg 3835.04 現(xiàn)貨
100mg 10401.3 現(xiàn)貨
1g 13677.3 現(xiàn)貨
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常與ICG-001一起在實驗中被使用的化合物

Auranofin

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，并抑制肺轉(zhuǎn)移小鼠模型中的轉(zhuǎn)移。

Lin Z, et al. Front Oncol. 2021; 11: 738085.

Paclitaxel

Foscenvivint可改善Paclitaxel誘導(dǎo)的FOXM1表達和癌癥干細胞(CSC)表型以及體外腫瘤啟動能力的增加。

Ring A, et al. Cancers (Basel). 2018 Dec 19;10(12):525.

(+)-JQ1

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)細胞系中誘導(dǎo)強烈的細胞毒性作用。

Wiese M, et al. Cell Death & Disease 11.8 (2020): 673.

Pyrvinium pamoate

Foscenvivint和Pyrvinium加Bortezomib可降低RPMI-8226BR和KMS-11BR細胞系的細胞活力并增加細胞凋亡率。

Wu C, Oncol Lett. 2022 Jul; 24(1): 205.

Wnt-C59 (C59)

Foscenvivint和Wnt-C59可抑制人膽管癌細胞的生長，并在異種移植模型和硫代乙胺模型中減少腫瘤面積和數(shù)量。

Noll AT, et al. World J Hepatol. 2016 Sep 18;8(26):1093-6.

ICG-001相關(guān)產(chǎn)品

相關(guān)信號通路圖

Epigenetic Reader Domain Signaling Pathways

Epigenetic Reader Domain信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
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
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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
CBP [1]
(Cell-free assay)
3 μM
體外研究(In Vitro)
體外研究活性

ICG-001 作用于TOPFLASH 時，IC50為3 μM，而對含突變TCF位點的相關(guān)報告基因結(jié)構(gòu), FOPFLASH沒有作用效果。使用25μM ICG-001處理SW480 細胞8小時后，降低Survivin和 Cyclin D1 RNA和蛋白的穩(wěn)定水平，這兩者都可通過β-catenin上調(diào)。ICG-001 作用于轉(zhuǎn)化細胞而不是正常結(jié)腸細胞，選擇性誘導(dǎo)凋亡，降低結(jié)腸癌細胞生長。[1] ICG-001作用于presenilin-1突變細胞，可表型營救正常神經(jīng)生長因子(NGF)誘導(dǎo)的神經(jīng)元分化和神經(jīng)軸突生長，強調(diào)TCF/β-catenin 信號通路在神經(jīng)軸突生長和神經(jīng)元分化中的重要性。[2] 最新研究顯示 5μM ICG-001作用于MCF7細胞，抑制leptin誘導(dǎo)的EMT, 入侵和腫瘤干細胞球形成。[3]
實驗圖片 檢測方法 檢測指標(biāo) 實驗圖片 PMID
Western blot SOX-2 / CD44 / Survivin / EGFR / FOXM1 / EZH2 / Vimentin

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