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iCRT3

iCRT3用途

iCRT3 是 Wnt 和 β-连环蛋白应答转录 (β-catenin-responsive transcription) 的抑制剂。

iCRT3名称

[ CAS 号 ]:
901751-47-1

[ 中文名 ]:
iCRT3

[ 英文名 ]:
iCRT3

[英文别名 ]:

iCRT3

iCRT3生物活性

[ 描述 ]:

iCRT3 是 Wnt 和 β-连环蛋白应答转录 (β-catenin-responsive transcription) 的抑制剂。

[ 相关类别 ]:

信号通路 >> 干细胞及 Wnt 通路 >> Wnt信号

研究领域 >> 癌症

[ 靶点 ]

Wnt

[体外研究]

iCRT3是Wnt和β-连环蛋白反应性转录的抑制剂。 iCRT3显着降低TOP Flash活性并降低NTSR1水平。神经降压素(NTS)和Wnt3a的抗细胞凋亡作用可以在很大程度上被iCRT3消除[1]。与DMSO对照相比,用iCRT3长期维持的细胞显示经典多能性基因的表达增强,而分化标志物和T细胞因子(TCF)靶基因的表达同时降低[2]。用12.5,25,50和75μM剂量的iCRT3处理分别使TNF-α水平降低14.7％,18.5％,44.9％和61.3％。使用iCRT3治疗,与载体相比,IκB水平以剂量依赖性方式增加[3]。

[体内研究]

通过iCRT3处理显着延迟肿瘤生长速率。一致地,iCRT3的肿瘤抑制作用伴随着Ki67指数的降低,这是一种增殖标志物[1]。 10mg/kg iCRT3治疗组中的IL-6水平比载体组中的IL-6水平低82.9％。假手术中IL-1β水平检测不到,但脓毒症小鼠达到371 pg/mL,5和10 mg/kg iCRT3分别下降30.2％和53.2％。对于剂量为5和10mg/kg的iCRT3处理,这些脓毒症小鼠的AST水平分别比载体处理的小鼠中的AST水平低15.4％和44.2％。在用10mg/kg iCRT3处理后,与载体组相比,肺形态得到改善,微观恶化大大减少。与载体组相比,iCRT3处理的小鼠肺组织中凋亡细胞的数量显着减少了92.7％[3]。

[细胞实验]

将细胞接种到96孔板中至每孔5×103个细胞的密度，并在含有iCRT3的培养基中再孵育48小时。细胞活力和细胞凋亡测定分别使用Cell Counting kit-8和Caspase-Glo 3/7测定试剂盒根据制造商的说明进行[1]。

[动物实验]

NOD-SCID BALB / c小鼠在右后方皮下接种2×106个A172细胞。每4天记录原发肿瘤的生长情况。当肿瘤生长至~200mm 3时，将iCRT3（5mg / kg）在PBS中稀释三周。用含有5％（v / v）DMSO的空白PBS处理对照小鼠。用以下公式评估肿瘤体积：体积=肿瘤长度×宽度2/2。药物处理后24天处死小鼠。将肿瘤切除并包埋在石蜡中，通过免疫组织化学分析Ki67染色[1]。

[参考文献]

[1]. Xiao H, et al. A Novel Positive Feedback Loop Between NTSR1 and Wnt/β-Catenin Contributes to Tumor Growth of Glioblastoma. Cell Physiol Biochem. 2017 Oct 24;43(5):2133-2142.

[2]. Chatterjee SS, et al. Inhibition of β-catenin-TCF1 interaction delays differentiation of mouse embryonic stem cells. J Cell Biol. 2015 Oct 12;211(1):39-51.

[3]. Sharma A, et al. Mitigation of sepsis-induced inflammatory responses and organ injury through targeting Wnt/β-catenin signaling. doi: 10.1038/s41598-017-08711-6.

[相关活性小分子]

iCRT3物理化学性质

[ 分子式 ]:
C₂₃H₂₆N₂O₂S

[ 分子量 ]:
394.53000

[ 精确质量 ]:
394.17100

[ PSA ]:
80.43000

[ LogP ]:
5.19540

[ 外观性状 ]:
粉末

[ 储存条件 ]:
-20℃

iCRT3安全信息

[ 符号 ]:

GHS05, GHS07

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302-H315-H318-H335

[ 警示性声明 ]:
P261-P280-P305 + P351 + P338

[ 危险品运输编码 ]:
NONH for all modes of transport

iCRT3文献

Mammary epithelial cell phagocytosis downstream of TGF-β3 is characterized by adherens junction reorganization.

Cell Death Differ. 23 , 185-96, (2016)

After weaning, during mammary gland involution, milk-producing mammary epithelial cells undergo apoptosis. Effective clearance of these dying cells is essential, as persistent apoptotic cells have a n...

Both canonical and non-canonical Wnt signaling independently promote stem cell growth in mammospheres.

PLoS ONE 9(7) , e101800, (2014)

The characterization of mammary stem cells, and signals that regulate their behavior, is of central importance in understanding developmental changes in the mammary gland and possibly for targeting st...

Signal integration by the CYP1A1 promoter--a quantitative study.

Nucleic Acids Res. 43 , 5318-30, (2015)

Genes involved in detoxification of foreign compounds exhibit complex spatiotemporal expression patterns in liver. Cytochrome P450 1A1 (CYP1A1), for example, is restricted to the pericentral region of...

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