ARN5187

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。

ARN5187 

ARN5187 是一种亲溶酶体 REV-ERBβ 配体,抑制 REV-ERB 介导的转录调控和细胞自噬。ARN5187 显示出溶酶体效力和细胞毒性。 ARN5187 诱导细胞凋亡 (apoptosis)。

ARN5187

ARN5187 Chemical Structure

CAS No. : 1287451-26-6

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生物活性

ARN5187 is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 shows lysosomotropic potency and cytotoxicity. ARN5187 induces apoptosis[1][2].

IC50 & Target

REV-ERBβ[1]

体外研究
(In Vitro)

ARN5187 (compound 1) (0-100 µM; 48 h) shows cytotoxicity with EC50 of 23.5 µM in BT-474 cells and IC50 of 30.14 µM, >100 µM for BT-474 and HMEC cells, respectively[1][2].
ARN5187 (0-100 µM) activates the RevRE reporter in a concentration-dependent manner in HEK-293 cells[1].
ARN5187 (25, 50 µM) is a lysosomotropic-independent REV-ERB antagonistic activity[1].
ARN5187 (50 µM; 24 h) shows autophagy inhibition[1].
ARN5187 (50 µM; 2, 8, 24 h) effects autophagy formation and maturation[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: BT-474 cells
Concentration: 0-100 µM
Incubation Time: 48 h
Result: Showed cytotoxicity with EC50 of 23.5 µM.

RT-PCR[1]

Cell Line: BT-474 cells
Concentration: 25, 50 µM
Incubation Time:
Result: Significantly enhanced the expression of BMAL1, PER1 and PEPCK in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: BT-474 cells
Concentration: 50 µM
Incubation Time: 24 h
Result: Significantly increased the expression of α-LC3-II, α-p62, α-Cleaved PARP.

分子量

397.53

Formula

C24H32FN3O

CAS 号

1287451-26-6

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]. De Mei C, et al. Dual inhibition of REV-ERBβ and autophagy as a novel pharmacological approach to induce cytotoxicity in cancer cells. Oncogene. 2015 May 14;34(20):2597-608.

    [2]. Torrente E, et al. Synthesis and in Vitro Anticancer Activity of the First Class of Dual Inhibitors of REV-ERBβ and Autophagy. J Med Chem. 2015 Aug 13;58(15):5900-15.

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