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ICG-001

SKU: orb1710780

描述

ICG001 is a selective small molecule inhibitor that disrupts the β-catenin/CBP interaction to block Wnt/β-catenin signaling, with an IC50 of 3 μM for CREB binding. It is a valuable research tool for studying oncogenic signaling in cancers, including colorectal carcinoma, in both cellular and animal models.

研究领域

Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

图片与验证

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关键属性

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CAS 号780757-88-2
MW548.63
纯度>99.99% (May vary between batches)
分子式C33H32N4O4
SMILESOc1ccc(C[C@@H]2N3[C@H](CN(Cc4cccc5ccccc45)C2=O)N(CCC3=O)C(=O)NCc2ccccc2)cc1
靶点Wnt/beta-catenin,Apoptosis,Epigenetic Reader Domain
溶解性2% DMSO+40% PEG300+5% Tween 80+53% Saline:10 mg/mL (18.23 mM);DMSO:242 mg/mL (441.1 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:9 mg/mL (16.4 mM)

生物活性

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靶点 IC50
CBP:3 μM
体内
METHODS: In a tumor regression SW620 nude mouse xenograft model, ICG-001 (150 mg/kg, intravenous injection) was administered to observe the effect of the drug on tumor remission in nude mice. RESULTS Tumor volume was significantly reduced during the 19-day treatment, with no mortality or weight loss.
体外
METHODS: SW480 cells were treated with ICG-001 (25 μM, 24 h) and the inhibition of survivin gene transcription was measured by semiquantitative RT-PCR; SW480 and HCT116 cells were treated with ICG-001 (10 and 25 μM, 24 h) and analyzed by immunoblotting for survivin; SW480 cells were treated with ICG-001 (25 μM) and the chromatin immunoprecipitation assay of the cyclin D1 promoter was used; promoter occupancy was assessed with CBP- (AC-22) or p300- (C-20) specific antibodies in the presence of ICG-001 (25 μM, 8 h). RESULTS After 8 h of treatment of SW480 cells with 25 μM ICG-001, approximately 2% of the genes analyzed were upregulated by a factor greater than 2, while only approximately 0.3% of the genes were downregulated by more than 50%. The two genes downregulated were S100A4 and survivin, which are the first and fourth mRNAs upregulated in cancer cells, respectively. ICG-001 effectively reduced the steady-state levels of survivin mRNA and protein in treated colorectal cancer cells. SW480 cells treated with ICG-001 (25 μM) showed a significant decrease in cyclin D1 as early as 4 h after treatment. Using chromatin immunoprecipitation, ICG-001 was shown to selectively inhibit the endogenous cyclin D1 promoter β.

储存与操作

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储存-20°C
有效期12 months from date of receipt.
免责声明For research use only

别名

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inhibit, EpigeneticReaderDomain, Epigenetic Reader Domain, Inhibitor, ICG 001, ICG001, ICG-001, betacatenin, beta-catenin, Beta catenin, CBP, 847591-62-2, bcatenin, Apoptosis, β-catenin, βcatenin, Wnt/β-catenin, Wnt/betacatenin, Wnt/b-catenin, Wnt

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质量保证

质量保证

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our 条款与条件和选购指南.

关键属性

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暂无计算属性。

实验方案信息

可选规格

请在下方选择规格

1 mg
¥ 910.00
5 mg
¥ 1,430.00
1 ml x 10 mM (in DMSO)
¥ 1,560.00
10 mg
¥ 1,950.00
25 mg
¥ 3,380.00
50 mg
¥ 5,460.00
100 mg
¥ 8,190.00
500 mg
¥ 16,900.00
发货Usually dispatched within 5-10 working days
批量询价