ICG 001
目录号 : GC16893
ICG001 是一种靶向 Wnt/β-catenin 通路的小分子抑制剂。
Cas No.:780757-88-2
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment: [1] | |
|
Cell lines |
Rat Epicardial Cells |
|
Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
|
Reaction Conditions |
10 μM, 24 hours |
|
Applications |
The rat EMCs were treated with either ICG-001 or IQ1 and performed co-immunoprecipitation (co-IP) assays. Cells were treated with DMSO, ICG-001 or IQ1 for 24 hours. In the DMSO control treated cells, essentially all of the β-catenin was associated with CBP. Treatment with IQ1 had minimal effects on β-catenin coactivator usage. However, as anticipated, treatment with ICG-001 decreased the β-catenin/CBP interaction, while concomitantly increasing the β-catenin/p300 interaction. |
| Animal experiment: [1] | |
|
Animal models |
Female Sprague-Dawley rats |
|
Dosage form |
Subcutaneous injection, 50 mg/kg/day |
|
Applications |
The left coronary artery of the rats was permanently occluded via surgery to induce regional ischemic injury to the left ventricle. ICG-001 was administered to the rats beginning on the day of surgery for 10 days. Four weeks after surgery (20 days after the last ICG-001 treatment), left ventricular ejection fraction was assessed by angiography as an indicator of cardiac contractile function. ICG-001 significantly improved ejection fraction by 8.4% from 46.2±1.7% to 54.6±3.4% (P < 0.05). This data demonstrates that ICG-001 significantly improved cardiac contractile function after myocardial infarction in the rats. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1] Sasaki T, Hwang H, Nguyen C, et al. The small molecule Wnt signaling modulator ICG-001 improves contractile function in chronically infarcted rat myocardium. PloS one, 2013, 8(9): e75010. |
|
ICG001 is a small molecule inhibitor that targets Wnt/β-catenin pathway. It inhibits TCF/β-catenin mediated transcription by competing with β-catenin for CBP (CREB binding protein) but not p300 binding with an IC50 of 3 μM [1]. It can be used to specifically evaluate the role of CBP/beta-catenin association on WNT signaling and cell physiology.
ICG001 have been shown to selectively inhibit colon carcinoma cell lines (SW480 and HCT-116 cells) but not normal colonic epithelial cells (CCD-841Co). It is also efficacious in the Min mouse and nude mouse xenograft models of colon cancer [1]. ICG-001 is a potent inhibitor of GBM stem cells in culture. ICG001 selectively inhibits Wnt/beta-catenin/CREB binding protein (CBP) signaling to reverses pulmonary fibrosis and ameliorate experimental dermal fibrosis in experimental models [2,3]. ICG001 is currently in clinical trial for colon cancer and leukemias.
References:
[1]Emami KH, Nguyen C, Ma H, Kim DH, Jeong KW, Eguchi M, Moon RT, Teo JL, Kim HY, Moon SH, Ha JR, Kahn M. A small molecule inhibitor of beta-catenin/CREB-binding protein transcription. Proc Natl Acad Sci U S A. 2004 Aug 24;101(34):12682-7.
[2]Henderson WR Jr1, Chi EY, Ye X, Nguyen C, Tien YT, Zhou B, Borok Z, Knight DA, Kahn M. Inhibition of Wnt/beta-catenin/CREB binding protein (CBP) signaling reverses pulmonary fibrosis. Proc Natl Acad Sci U S A. 2010 Aug 10;107(32):14309-14.
[3]Beyer C, Reichert H, Akan H, Mallano T, Schramm A, Dees C, Palumbo-Zerr K, Lin NY, Distler A, Gelse K, Varga J, Distler O, Schett G, Distler JH. Blockade of canonical Wnt signalling ameliorates experimental dermal fibrosis. Ann Rheum Dis. 2013 Jul;72(7):1255-8.
ICG001 是一种靶向 Wnt/β-catenin 通路的小分子抑制剂。它通过与 β-连环蛋白竞争 CBP（CREB 结合蛋白）而不是 p300 结合来抑制 TCF/β-连环蛋白介导的转录,IC50 为 3 μM [1]。它可用于专门评估 CBP/β-连环蛋白结合对 WNT 信号和细胞生理学的作用。
ICG001 已显示可选择性抑制结肠癌细胞系（SW480 和 HCT-116 细胞）,但不抑制正常结肠上皮细胞 (CCD-841Co)。它在 Min 小鼠和裸鼠结肠癌异种移植模型中也有效 [1]。 ICG-001 是培养中 GBM 干细胞的有效抑制剂。 ICG001 选择性地抑制 Wnt/β-连环蛋白/CREB 结合蛋白 (CBP) 信号,以逆转肺纤维化并改善实验模型中的实验性真皮纤维化 [2,3]。 ICG001目前正在进行结肠癌和白血病的临床试验。
| Cas No. | 780757-88-2 | SDF | |
| 化学名 | (6S,9aS)-N-benzyl-6-[(4-hydroxyphenyl)methyl]-8-(naphthalen-1-ylmethyl)-4,7-dioxo-3,6,9,9a-tetrahydro-2H-pyrazino[1,2-a]pyrimidine-1-carboxamide | ||
| Canonical SMILES | C1CN(C2CN(C(=O)C(N2C1=O)CC3=CC=C(C=C3)O)CC4=CC=CC5=CC=CC=C54)C(=O)NCC6=CC=CC=C6 | ||
| 分子式 | C33H32N4O4 | 分子量 | 548.63 |
| 溶解度 | ≥ 27.4315mg/mL in DMSO, ≥ 35.47 mg/mL in EtOH with ultrasonic | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8227 mL | 9.1136 mL | 18.2272 mL |
| 5 mM | 0.3645 mL | 1.8227 mL | 3.6454 mL |
| 10 mM | 0.1823 mL | 0.9114 mL | 1.8227 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。