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VPC-18005
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
VPC-18005图片
CAS NO:2242480-48-2
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
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。
Cas No.2242480-48-2
分子式C15H17N3O3S
分子量319.38
溶解度DMSO : 62.5 mg/mL (195.69 mM; Need ultrasonic)
储存条件4°C, protect from light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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].

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].

[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.