"目錄號(hào): HY-14428
ICG-001 是一種Wnt/β-catenin/TCF -介導(dǎo)的轉(zhuǎn)錄拮抗劑枫甲，特別結(jié)合元件結(jié)合蛋白 (CBP)修档，IC50值為 3 μM忿危。
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生物活性
Description
ICG-001 is an antagonist ofWnt/β-catenin/TCF-mediated transcription and specifically binds to element-binding protein (CBP) withIC50of 3 μM.
IC50& Target
IC50: 3 μM (CBP)
In Vitro
ICG-001 (5μM) inhibits leptin-induced EMT, invasion and tumorsphere formation in MCF7 cells[1].?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[2]. ICG-001 (25μM) treatment reduces the steady-state levels of Survivin and Cyclin D1 RNA and protein in SW480 cells, both of which can be up-regulated by β-catenin. ICG-001 selectively induces apoptosis in transformed cells but not in normal colon cells, and reduces in vitro growth of colon carcinoma cells[3].?
In Vivo
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[2].?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. ICG-001 (150 mg/kg, i.v.) demonstrates a dramatic reduction in tumor volume over the 19-day course of treatment, with no mortality or weight loss in the SW620 nude mouse xenograft model of tumor regression[3].?
References
