ICG-001

CAS: 780757-88-2 货号: I409283 分子式: C33H32N4O4 分子量: 548.63 PubChem CID: 11238147
有货
级别和纯度: 10mM in DMSO
储存条件
-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
I409283-1ml
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¥1,090.90
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 1 篇同行评审文献引用。

概述


Information

ICG-001 ICG-001 antagonizes Wnt/β-catenin /TCF-mediated transcription and specifically binds to CREB-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300. ICG-001 induces apoptosis .
In vitro

ICG-001 has no effect on the related reporter construct, FOPFLASH, which contains mutated TCF sites. After treatment with 25μM of ICG-001 for 8 hours, SW480 cell reduces the steady-state levels of Survivin and Cyclin D1 RNA and protein, both of which can be up-regulated by β-catenin. ICG-001 selectively induces apoptosis in transformed cells but not in normal colon cells, reduces in vitro growth of colon carcinoma cells. ICG-001, can phenotypically rescue normal nerve growth factor (NGF) -induced neuronal differentiation and neurite outgrowth in the presenilin-1 mutant cells, emphasizing the importance of the TCF/β-catenin signaling pathway on neurite outgrowth and neuronal differentiation. A recent study demonstrates that 5μM ICG-001 inhibits leptin-induced EMT, invasion and tumorsphere formation in MCF7 cells.

In vivo

Administration of a water-soluble analog of ICG-001 for 9 weeks reduces the formation of colon and small intestinal polyps by 42% as effectively as the nonsteroidal antiinflammatory agent Sulindac, which has consistently demonstrated efficacy in this model. No overt toxicity is detected throughout the course of treatment. In the SW620 nude mouse xenograft model of tumor regression, 150 mg/kg, i.v. of analog demonstrates a dramatic reduction in tumor volume over the 19-day course of treatment, with no mortality or weight loss. ICG-001 (5 mg/kg per day) significantly inhibits beta-catenin signaling and attenuates bleomycin-induced lung fibrosis in mice, while concurrently preserving the epithelium.
Cell Data

cell lines:wt-p53 cancer cell lines (SJSA1, RKO, HCT116)

Concentrations:~25 μM

Incubation Time:24 hours

Powder Purity:≥98%

规格

英文别名
(6S,9aS)-6-(4-hydroxybenzyl)-N-benzyl-8-(naphthalen-1-ylmethyl)-4,7-dioxo-hexahydro-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide
规格或纯度
10mM in DMSO
英文名称
ICG-001
生化机理
ICG-001 可拮抗 Wnt/β-catenin/TCF 介导的转录,并能与 CREB 结合蛋白(CBP)特异性结合,IC50 为 3 μM,但不是相关的转录辅激活剂 p300。ICG-001 可诱导细胞凋亡。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
C1CN([C@H]2CN(C(=O)[C@@H](N2C1=O)CC3=CC=C(C=C3)O)CC4=CC=CC5=CC=CC=C54)C(=O)NCC6=CC=CC=C6
PubChem CID
分子量
548.63

技术文档

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高级数据

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