iCRT 14
目录号 : GC16640
An inhibitor of β-catenin-responsive transcription
Cas No.:677331-12-3
Sample solution is provided at 25 µL, 10mM.
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iCRT 14 is a potent and specific inhibitor of β-catenin responsive transcription (CRT) with IC50 value of 40.3 nM [1].
iCRT 14 belongs to the thiazolidinedione class and is screened out by the dTF12-luciferase reporter assay. It inhibits the direct interaction between β-catenin and TCF4 and does not affect the interaction of β-catenin with other cognate protein partners. iCRT 14 also inhibits the mammalian Wnt responsive STF16 luciferase reporter in HEK293 cells with IC50 value of 40.3 nM. Besides that, iCRT 14 is specific against CRT over other conserved cell signaling pathways. It had no effect on the phosphorylation of Dvl induced by Wnt [1].
iCRT 14 can also interfere with TCF binding to DNA. Moreover, the inhibition of CRT resulted in the modulation of CRT-induced molecular and morphological changes including cell transformation phenotype and cell invasion. Furthermore, the treatment of HCT116 and HT29 cells with iCRT 14 exhibited cell cycle arrest in the G0/G1 phase. In the xenograft models of HCT116 and HT29, administration of iCRT 14 at dose of 50 mg/kg caused significant decrease in CycD1 and the subsequent suppression of tumor growth [1].
References:
[1] Gonsalves F C, Klein K, Carson B B, et al. An RNAi-based chemical genetic screen identifies three small-molecule inhibitors of the Wnt/wingless signaling pathway. Proceedings of the National Academy of Sciences, 2011, 108(15): 5954-5963.
Cell experiment: | Cells are seeded at 20,000 cells/well into 96-well plates. After overnight incubation, cells are treated with DMSO or each Wnt inhibitor (iCRT-3, 75 μM; iCRT-5, 200 μM; iCRT-14, 50 μM; IWP-4, 5 μM and XAV-939, 10 μM) for 48 hours. Cell viability is determined using the Cell Titer-Glo luminescent cell viability assay kit. Luminescence is measured using FLUOstar microplate reader. All treatments are performed in triplicate, and each experiment is repeated three times. |
References: [1]. Gonsalves FC, et al. An RNAi-based chemical genetic screen identifies three small-molecule inhibitors of the Wnt/wingless signaling pathway. Proc Natl Acad Sci USA. 2011 Apr 12;108(15):5954-63. | |
| Cas No. | 677331-12-3 | SDF | |
| 分子式 | C21H17N3O2S | 分子量 | 375.44 |
| 溶解度 | ≥ 18.75mg/mL in DMSO with ultrasonic and warming | 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。 |
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| 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 | 2.6635 mL | 13.3177 mL | 26.6354 mL |
| 5 mM | 0.5327 mL | 2.6635 mL | 5.3271 mL |
| 10 mM | 0.2664 mL | 1.3318 mL | 2.6635 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。
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
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