计算溶液所需的质量、体积或浓度。
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
高级数据
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
此产品的引用文献
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
Copyright © 2023至今 上海阿拉丁生化科技股份有限公司 SSE:688179 保留所有权利。
危险品化学品经营许可证（带存储）