219332
β-连环蛋白/Tcf抑制剂III，iCRT3
The β-Catenin/Tcf Inhibitor III, iCRT3 controls the biological activity of β-Catenin/Tcf. This small molecule/inhibitor is primarily used for Biochemicals applications.
别名:
β-连环蛋白/Tcf抑制剂III，iCRT3, C3, 2-(((2-(4-乙基苯基)-5-甲基-1,3-恶唑-4-基)甲基)磺酰基)-N-(2-苯基乙基)乙酰胺，β-连环蛋白响应转录的抑制剂，Wnt通路抑制剂VIII
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关于此项目
经验公式（希尔记法）:
C23H26N2O2S
分子量:
394.53
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥95% (HPLC)
Form:
powder
Quality level:
Storage condition:
OK to freeze
protect from light
protect from light
产品名称
β-连环蛋白/Tcf抑制剂III，iCRT3, The β-Catenin/Tcf Inhibitor III, iCRT3 controls the biological activity of β-Catenin/Tcf. This small molecule/inhibitor is primarily used for Biochemicals applications.
assay
≥95% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
tan
solubility
DMSO: 50 mg/mL
shipped in
ambient
storage temp.
−20°C
Quality Level
相关类别
Disclaimer
毒性：标准处理（A）
General description
一种可渗透细胞的恶唑化合物，可通过直接的β-连环蛋白（β-cat）结合干扰β-cat-TCF4相互作用，从而作为选择性CRT（β-连环蛋白响应转录）抑制剂（IC50=8.2 nM，针对HEK293培养物中Wnt3a依赖性SuperTopFlash STF16-luc报告基因活性），同时表现出对音猬因子，JAK/STAT或Notch信号通路依赖性转录激活的活性大大降低。以剂量依赖性方式（25至75 µM）有效抑制CRT靶基因（包括WISP1，AXN2和CYCD1）的细胞表达，并选择性抑制HCT116（75 µM），HT29（75 µM）和几种需要持续Wnt/CRT活性才能存活的原代人结肠癌培养物（6.25至100 µg/mL；平均IC50 ~36 µg/ml）的增殖。
Other Notes
Lee, E., et al. 2013.Proc.Natl.Acad.Sci. USA110, 15710.
Gonsalves, F.C., et al. 2011.Proc.Natl.Acad.Sci. USA108, 5954.
Gonsalves, F.C., et al. 2011.Proc.Natl.Acad.Sci. USA108, 5954.
Packaging
用惰性气体包装
Preparation Note
复溶后，等分并冷冻保存（-20°C）。储备液在-20°C条件下可稳定保存3个月。
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 3
Eugine Lee et al.
Proceedings of the National Academy of Sciences of the United States of America, 110(39), 15710-15715 (2013-09-11)
Androgen receptor (AR) is the major therapeutic target in aggressive prostate cancer. However, targeting AR alone can result in drug resistance and disease recurrence. Therefore, simultaneous targeting of multiple pathways could in principle be an effective approach to treating prostate
Foster C Gonsalves et al.
Proceedings of the National Academy of Sciences of the United States of America, 108(15), 5954-5963 (2011-03-12)
Misregulated β-catenin responsive transcription (CRT) has been implicated in the genesis of various malignancies, including colorectal carcinomas, and it is a key therapeutic target in combating various cancers. Despite significant effort, successful clinical implementation of CRT inhibitory therapeutics remains a
Camille Cohen et al.
Nature communications, 15(1), 743-743 (2024-01-26)
Chronic kidney disease (CKD) is a public health problem driven by myofibroblast accumulation, leading to interstitial fibrosis. Heterogeneity is a recently recognized characteristic in kidney fibroblasts in CKD, but the role of different populations is still unclear. Here, we characterize
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