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ICG001

ICG001

产品编号 T2237   CAS 847591-62-2

ICG001 (PRI-724 isomer) 拮抗 Wnt/β-catenin/TCF 介导的转录,并特异性结合元件结合蛋白(CREB) 结合蛋白 (CBP),IC50 为 3 μM,但不是相关的转录共激活因子 p300。

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ICG001 Chemical Structure
ICG001, CAS 847591-62-2
规格 价格/CNY 货期 数量
1 mg ¥ 322 现货
5 mg ¥ 762 现货
10 mg ¥ 993 现货
25 mg ¥ 2,090 现货
50 mg ¥ 3,730 现货
100 mg ¥ 5,690 现货
500 mg ¥ 11,700 现货
1 mL * 10 mM (in DMSO) ¥ 919 现货
其他形式的 ICG001:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
产品目录号及名称: ICG001 (T2237)
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纯度: 99.95%
纯度: 98.63%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 ICG001 (PRI-724 isomer) antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to element-binding protein (CREB)-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300.
靶点活性 CBP:3 μM
体外活性 PRI-724 binds specifically to CBP but not the related transcriptional coactivator p300, thereby disrupting the interaction of CBP with β-catenin. Treatment with PRI-724 selectively induces apoptosis in colon carcinoma cells but not in normal colonic epithelial cells and reduces in vitro growth of colon carcinoma cells[1][2].
体内活性 PRI-724 exhibits antitumor activity in the mouse xenograft models of colon cancer. The initial results of the Phase I clinic trial of PRI-724 has been disclosed publically. The drug exhibits an acceptable toxicity profile with only one dose-limiting toxicity of grade 3 reversible hyperbilirubinaemia. An Open-Label dose-escalation phase I/II study of PRI-724 for patients with advanced myeloid malignancies is still ongoing[2].
细胞实验 ICG-001 is dissolved in DMSO. To evaluate effects of ICG-001 on α-SMA and collagen type 1 expression, RLE-6TN cells are treated with TGF-β1 (0.25 ng/mL) in the presence or absence of ICG-001 (5.0 μM). After 24 h, cells are harvested and mRNA isolated for analysis by qPCR. RNA is reverse-transcribed using SuperScript reverse transcriptase. Quantitative PCR is performed with SYBR-Green PCR using Real-Time PCR System HT7900. The amplification protocol is set as follows: 95°C denaturation for 10 min followed by 40 cycles of 15-s denaturation at 95°C, 1 min of annealing/extension, and data collection at 60°C.
分子量 548.63
分子式 C33H32N4O4
CAS No. 847591-62-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 54.9 mg/mL (100 mM)

Ethanol: 27.4 mg/mL (50 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 1.8227 mL 9.1136 mL 18.2272 mL 45.5681 mL
5 mM 0.3645 mL 1.8227 mL 3.6454 mL 9.1136 mL
10 mM 0.1823 mL 0.9114 mL 1.8227 mL 4.5568 mL
20 mM 0.0911 mL 0.4557 mL 0.9114 mL 2.2784 mL
50 mM 0.0365 mL 0.1823 mL 0.3645 mL 0.9114 mL
DMSO 100 mM 0.0182 mL 0.0911 mL 0.1823 mL 0.4557 mL

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TargetMol Library Books参考文献

1. Sasaki T, et al. Transl Respir Med. 2:8. 2. Zhang X, et al. Am J Cancer Res. 2015, 5(8):2344-2360. 3. Yosuke Osawa, et al. EBioMedicine. 2015, 2(11):1751-1758. 4. Liu F, Yu F, Lu Y Z, et al. Crosstalk between pleural mesothelial cell and lung fibroblast contributes to pulmonary fibrosis[J]. Biochimica et Biophysica Acta (BBA)-Molecular Cell Research. 2020, 1867(11): 118806.

TargetMol Library Books文献引用

1. Liu F, Yu F, Lu Y Z, et al. Crosstalk between pleural mesothelial cell and lung fibroblast contributes to pulmonary fibrosis. Biochimica et Biophysica Acta (BBA)-Molecular Cell Research. 2020, 1867(11): 118806. 2. Xiao K, Liu C, Wang H, et al.Umbilical cord mesenchymal stem cells overexpressing CXCR7 facilitate treatment of ARDS-associated pulmonary fibrosis via inhibition of Notch/Jag1 mediated by the Wnt/β-catenin pathway.Biomedicine & Pharmacotherapy.2023, 165: 115124. 3. Wang J, Sheng N, Li Y, et al.Ly6D facilitates chemoresistance in laryngeal squamous cell carcinoma through miR-509/β-catenin signaling pathway.American Journal of Cancer Research.2023, 13(5): 2155.
CBP/p300-IN-2 PBRM1-BD2-IN-2 FT001 ML367 MRS2698 GSK620 GNE-272 NEO2734

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抗癌药物库 抗癌临床化合物库 药物功能重定位化合物库 抗纤维化化合物库 组蛋白修饰化合物库 抗前列腺癌化合物库 细胞凋亡化合物库 NO PAINS 化合物库 表观遗传库

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母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

ICG001 847591-62-2 Chromatin/Epigenetic Cytoskeletal Signaling Stem Cells Epigenetic Reader Domain Wnt/beta-catenin 780757-88-2 PRI 724 ICG 001 PRI724 ICG-001 Inhibitor inhibitor inhibit

 

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