VPC-18005

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

VPC-18005 

VPC-18005 抑制 ERG 诱导的转录，并直接与 ERG-ETS 结构域结合，并破坏 ERG 与 DNA 的结合。VPC-18005是一种荧光素酶活性的有效抑制剂。

VPC-18005

VPC-18005 Chemical Structure

CAS No. : 2242480-48-2

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生物活性

VPC-18005 inhibits ERG-induced transcription and interacts directly with the ERG-ETS domain, and disrupts the ERG binding to DNA. VPC-18005 is a potent inhibitor of luciferase activity[1].

体外研究
(In Vitro)

VPC-18005 is found to inhibit pETS-luc reporter activity in PNT1B-ERG and VCaP cells with IC50 values of 3 and 6 μM, respectively[1].
VPC-18005 could suppress ERG reporter activity without exhibiting overt cytotoxicity[1].
VPC-18005 inhibits migration and invasion of ERG-overexpressing cells in vitro[1].
VPC-18005 can antagonize the metastatic potential of ERG-expressing prostate cells[1].
The exposure of larvae to 1 or 10 µM of VPC-18005 produced a 20–30% decrease in the dissemination of cancer cells in zebrafsh[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: PNT1B-Mock cells and PNT1B-ERG cells.
Concentration: 5 µM.
Incubation Time: 24 h.
Result: Inhibited migration and invasion of prostate cell lines in vitro.

分子量

319.38

Formula

C15H17N3O3S
CAS 号

2242480-48-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Miriam S Butler, et al. Discovery and characterization of small molecules targeting the DNA-binding ETS domain of ERG in prostate cancer. Oncotarget. 2017 Jun 27;8(26):42438-42454.

    [2]. Haneen Amawi, et al. The use of zebrafish model in prostate cancer therapeutic development and discovery. Cancer Chemother Pharmacol. 2021 Mar;87(3):311-325.

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