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上海源叶生物科技有限公司
主营产品： S30260异硫氰酸胍,30259盐酸胍,嗜热菌蛋白酶 |
15
联系电话
15921386130
公司信息
- 联系人：
- 何小姐
- 电话：
- 86-021-61559134
- 手机：
- 15921386130
- 传真：
- 86-021-55068248
- 地址：
- 上海市松江区长塔路465号6幢
- 邮编：
- 200433
- 网址：
- www.shyuanye.com
S50725
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更新时间：2024-07-01 21:59:59浏览次数：140
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- 产品描述：
ICG-001 is a potent and selective Wnt signaling modulator. ICG-001 modulates Wnt signaling and increased the expression of genes beneficial for cardiac regeneration in epicardial cells. ICG-001 binds cAMP-responsive element binding (CREB)-binding protein (CBP) to disrupt its interaction with β-catenin and inhibit CBP function as a coactivator of Wnt/β-catenin-mediated transcription. ICG-001 induces cytotoxicity of multiple myeloma cells in Wnt-independent manner. Note: Chemical structures of ICG-001 and PRI-724 look very close, but they are not the same molecule. Many vendors confused them.
- 靶点： IC50: 3 μM (CBP)
- 体外研究： ICG-001 increases caspase activity in colon carcinoma cell lines (SW480 or HCT116) but not in normal colonic epithelial cells (CCD-841Co). The increased caspase activity is manifested in selective cytotoxicity in colorectal cancer cells. cDNA microarray analysis demonstrated that ICG-001 had a very selective effect on gene transcription. Interestingly, two of the most highly up-regulated mRNAs in cancer cells (survivin and S100A4) are down-regulated by ICG-001. Down-regulation of survivin is notable, because survivin has been shown to inhibit caspase activation. It was also demonstrated that ICG-001 reduces endogenous survivin levels in a TCF/β-catenin fashion in vitro (Fig. 4 A and B). Reference: Proc Natl Acad Sci U S A. 2004 Aug 24;101(34):12682-7. https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/15314234/
- 体内研究： A water-soluble analog of ICG-001 was evaluated in vivo in two mouse models of cancer. The Min mouse, which has a germ-line mutation in one allele of the APC tumor suppressor gene, is a well characterized model for human familial adenomatous polyposis. Administration of the analog for 9 weeks reduced the formation of colon and small intestinal polyps by 42% as effectively as the nonsteroidal antiinflammatory agent Sulindac (Table 1), which has consistently demonstrated efficacy in this model (33). No overt toxicity was detected throughout the course of treatment. In the SW620 nude mouse xenograft model of tumor regression, 150 mg/kg, i.v. of the analog demonstrated a dramatic reduction in tumor volume over the 19-day course of treatment (Fig. 5C Left), with no mortality or weight loss (Fig. 5C Right). Reference: Proc Natl Acad Sci U S A. 2004 Aug 24;101(34):12682-7. https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/15314234/
- 参考文献：
1: Rao P, Pang M, Qiao X, Yu H, Wang H, Yang Y, Ren X, Hu M, Chen T, Cao Q, Wang Y, Khushi M, Zhang G, Wang YM, Heok P'ng C, Nankivell B, Lee VW, Alexander SI, Zheng G, Harris DC. Promotion of β-catenin/Foxo1 signaling ameliorates renal interstitial fibrosis. Lab Invest. 2019 Jun 26. doi: 10.1038/s41374-019-0276-z. [Epub ahead of print] PubMed PMID: 31243340.
2: Bocchicchio S, Tesone M, Irusta G. Convergence of Wnt and Notch signaling controls ovarian cancer cell survival. J Cell Physiol. 2019 May 13. doi: 10.1002/jcp.28775. [Epub ahead of print] PubMed PMID: 31087357.
3: Taiyab A, Holms J, West-Mays JA. β-Catenin/Smad3 Interaction Regulates Transforming Growth Factor-β-Induced Epithelial to Mesenchymal Transition in the Lens. Int J Mol Sci. 2019 Apr 27;20(9). pii: E2078. doi: 10.3390/ijms20092078. PubMed PMID: 31035577; PubMed Central PMCID: PMC6540099.
4: Cui Y, Wu X, Lin C, Zhang X, Ye L, Ren L, Chen M, Yang M, Li Y, Li M, Li J, Guan J, Song L. AKIP1 promotes early recurrence of hepatocellular carcinoma through activating the Wnt/β-catenin/CBP signaling pathway. Oncogene. 2019 Jul;38(27):5516-5529. doi: 10.1038/s41388-019-0807-5. Epub 2019 Apr 1. PubMed PMID: 30936461.
5: Chen Y, Wen H, Zhou C, Su Q, Lin Y, Xie Y, Huang Y, Qiu Q, Lin J, Huang X, Tan W, Min C, Wang C. TNF-α derived from M2 tumor-associated macrophages promotes epithelial-mesenchymal transition and cancer stemness through the Wnt/β-catenin pathway in SMMC-7721 hepatocellular carcinoma cells. Exp Cell Res. 2019 May 1;378
- 溶解度： DMSO 50mg/ml
母液保存：分装冻存，避免反复冻融；-20℃，1个月；-80℃，6个月（稀释后溶液温度低保存可能会析出，尽量现用现配）
细胞实验:先用DMSO溶解：再用培养基进行稀释，稀释过程建议分段进行，避免浓度变化过快导致化合物析出。若稀释过程中出现化合物析出的情况， 可采用超声的方法使其复溶。在稀释时要确保工作液中 DMSO 的终浓度尽量在0.1%以下，不要超过0.5%，并设置相应浓度的DMSO对照组。
动物实验：先用DMSO溶解：再用水或者生理盐水等去稀释，稀释过程建议分段进行，避免浓度变化过快导致化合物析出。若稀释过程中出现化合物析出的情况， 可采用超声的方法使其复溶。可以通过添加助溶剂来帮助溶解，比如植物油、Tween80、甘油、羧甲基纤维素钠和PEG400等。具体方式请参考文献。悬浊液可用于口服和腹腔注射，不会影响产品活性。
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 1.823 ml 9.114 ml 18.227 ml 5 mM 0.365 ml 1.823 ml 3.645 ml 10 mM 0.182 ml 0.911 ml 1.823 ml 50 mM 0.036 ml 0.182 ml 0.365 ml
- 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的性，仅供客户参考交流研究之用。
