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Merck
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重要文件

SML0796

Sigma-Aldrich

HI-TOPK-032

≥98% (HPLC)

同義詞:

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

經驗公式(希爾表示法):
C20H11N5OS
CAS號碼:
分子量::
369.40
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

orange to dark red

溶解度

DMSO: 3 mg/mL, clear (warmed)

儲存溫度

2-8°C

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 密鑰

BCSBXWKRZUPFHW-UHFFFAOYSA-N

應用

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。

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


分析證明 (COA)

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存取文件庫

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
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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