<生产厂家价格>

iCRT 14

iCRT 14用途

iCRT 14 是一种 β-连环蛋白应答转录（CRT）抑制剂，能够抑制 Wnt 信号通路，IC₅₀ 值为 40.3 nM。

iCRT 14名称

[ CAS 号 ]:
677331-12-3

[ 中文名 ]:
iCRT 14

[ 英文名 ]:
iCRT-14

[英文别名 ]:

iCRT14
iCRT 14

iCRT 14生物活性

[ 描述 ]:

iCRT 14 是一种 β-连环蛋白应答转录(CRT)抑制剂,能够抑制 Wnt 信号通路,IC50 值为 40.3 nM。

[ 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 ]

IC50: 40.3 nM (Wnt responsive STF16 luciferase)[1]

[体外研究]

除了影响TCF-β-cat相互作用的能力外,iCRT14还可以干扰TCF与DNA的结合[1]。 iCRT14(10,25,50μM)以剂量和时间依赖的方式有效抑制BT-549细胞中的细胞增殖,但仍然不如iCRT3有效[2]。

[体内研究]

iCRT14(50mg/kg,ip)显着降低HCT116异种移植物中肿瘤的CycD1增殖[1]。

[细胞实验]

将细胞以20,000个细胞/孔接种到96孔板中。孵育过夜后，用DMSO或每种Wnt抑制剂（iCRT-3,75μM; iCRT-5,200μM; iCRT-14,50μM; IWP-4,5μM和XAV-939,10μM）处理细胞。 48小时。使用Cell Titer-Glo发光细胞活力测定试剂盒测定细胞活力。使用FLUOstar酶标仪测量发光。所有处理一式三份进行，每个实验重复三次。

[参考文献]

[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.

[2]. Bilir B, et al. Wnt signaling blockage inhibits cell proliferation and migration, and induces apoptosis in triple-negative breast cancer cells. J Transl Med. 2013 Nov 4;11:280.

[相关活性小分子]

iCRT 14物理化学性质

[ 分子式 ]:
C₂₁H₁₇N₃O₂S

[ 分子量 ]:
375.44400

[ 精确质量 ]:
375.10400

[ PSA ]:
80.50000

[ LogP ]:
4.79500

[ 储存条件 ]:
2-8°C

iCRT 14安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

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

iCRT 14文献

Sequential actions of β-catenin and Bmp pattern the oral nerve net in Nematostella vectensis.

Nat. Commun. 5 , 5536, (2014)

Animal evolution is closely linked to the emergence of the nervous system. At present it is unknown how the basic mechanisms of neural induction and formation of central nervous systems evolved. We ad...

A switch from canonical to noncanonical Wnt signaling mediates early differentiation of human neural stem cells.

Stem Cells 32(12) , 3196-208, (2014)

Wnt/β-catenin signaling is essential for neurogenesis but less is known about β-catenin-independent Wnt signals. We show here that Wnt/activator protein-1 (AP-1) signaling drives differentiation of hu...

Targeting Wnt pathway in mantle cell lymphoma-initiating cells.

J. Hematol. Oncol. 8 , 63, (2015)

Mantle cell lymphoma (MCL) is an aggressive and incurable form of non-Hodgkin's lymphoma. Despite initial intense chemotherapy, up to 50% of cases of MCL relapse often in a chemoresistant form. We hyp...

更多文献