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Merck
CN
所有图片(1)

主要文件

SML0796

Sigma-Aldrich

HI-TOPK-032

≥98% (HPLC)

别名:

N-(12-氰基吲哚并[2,3-b]喹喔啉-2-基)-2-噻吩甲酰胺

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About This Item

经验公式（希尔记法）:
C20H11N5OS
CAS号:
487020-03-1
分子量:
369.40
UNSPSC代码:
12352200
NACRES:
NA.77

质量水平

100

方案

≥98% (HPLC)

表单

powder

颜色

orange to dark red

溶解性

DMSO: 3 mg/mL, clear (warmed)

储存温度

2-8°C

SMILES字符串

[s]1c(ccc1)C(=O)Nc2cc3[n](c4nc5c(nc4c3C#N)cccc5)cc2

InChI

1S/C20H11N5OS/c21-11-13-16-10-12(22-20(26)17-6-3-9-27-17)7-8-25(16)19-18(13)23-14-4-1-2-5-15(14)24-19/h1-10H,(H,22,26)

InChI key

BCSBXWKRZUPFHW-UHFFFAOYSA-N

应用

HI-TOPK-032已被用作PDZ结合激酶（PBK）抑制剂。

生化/生理作用

HI-TOPK-032属于ATP竞争性抑制剂类。它也可以用作大肠癌的有效治疗剂。
HI-TOPK-032是体外和体内的特异性TOPK（源自T-LAK细胞的蛋白激酶）抑制剂。HI-TOPK-032在结肠癌异种移植模型中抑制了肿瘤的生长。

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

从最新的版本中选择一种：

分析证书(COA)

Lot/Batch Number
0000175428
0000175427
0000175428
0000175427
0000053308

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PBK/TOPK enhances aggressive phenotype in prostate cancer via β-catenin-TCF/LEF-mediated matrix metalloproteinases production and invasion.
Brown-Clay J D, et al.
Oncotarget, 6(17), 15594?15609-15594?15609 (2015)
PBK/TOPK mediates geranylgeranylation signaling for breast cancer cell proliferation.
Dou X, et al.
Cancer Cell International, 15(1), 27-27 (2015)
Dong Joon Kim et al.
Cancer research, 72(12), 3060-3068 (2012-04-24)
The serine-threonine mitogen-activated protein kinase kinase family member T-LAK cell-originated protein kinase (TOPK/PBK) is heavily involved in tumor development, cancer growth, apoptosis, and inflammation. Despite the identification of TOPK as a promising novel therapeutic target, no inhibitor of TOPK has
Xiong Zhang et al.
Cancers, 13(7) (2021-05-01)
Metastatic castration-resistant prostate cancer (mCRPC) is a highly aggressive disease with few therapeutic options. Hyperactive androgen receptor (AR) signaling plays a key role in CRPC progression. Previously, we identified RAR-related orphan receptor gamma (RORγ) as a novel key driver of
Xiaoyan Dou et al.
Cancer cell international, 15, 27-27 (2015-03-10)
PDZ binding-kinase (PBK) (also named T-lymphokine-activated killer cell-originated protein kinase (TOPK)), a serine/threonine kinase, is tightly controlled in normal tissues but elevated in many tumors, and functions in tumorigenesis and metastasis. However, the signaling that regulates expression of PBK in

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