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(-)-JQ1

(-)-JQ1,是强效、细胞渗透性小分子溴结构域抑制剂(+)-JQ1的非活性立体异构体,可竞争性地与乙酰基赖氨酸识别基团结合。更多视频请关注视频号【艾维缔】。哔哩哔哩【IVDSHOW】。抖音【军哥聊表观】。
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(-)-JQ1是强效、细胞渗透性小分子溴结构域抑制剂(+)-JQ1的非活性立体异构体,可竞争性地与乙酰基赖氨酸识别基团结合。(+)-JQ1能竞争性地与溴结构域结合,将BRD4融合肿瘤蛋白从染色质中置换出来,从而诱导鳞状细胞分化,并在依赖BRD4的细胞系和患者异种移植模型中产生特异性抗增殖作用。然而,研究结果表明,(-)-JQ1 未能与所测试的任何溴链发生显著的相互作用,对 BRD4(1) 的抑制作用 IC50 为 10,000 nM。

Purity

≥98%

Format

Yellowish, white crystalline powder

Formula

C23H25ClN4O2S

MW

456.99

Solubility

Soluble in DMSO or ethanol at 100 mM

Biological Activity

(-)-JQ1 showed no inhibition of BRD4-dependent NMC cells.

CAS Registry #

1268524-71-5

Background

(-)-JQ1 is the inactive stereoisomer of the potent, cell-permeable, small molecule bromodomain inhibitor (+)-JQ1 that competitively binds to acetyl-lysine recognition motifs. (+)-JQ1 competitively binds to the bromodomain displacing the BRD4 fusion oncoprotein from chromatin, which induces squamous differentiation and specific anti-proliferative effect in BRD4-dependent cell lines and patient-derived xenograft models. However, study results have shown that (-)-JQ1 fails to significantly interact with any bromodomain tested and exhibits inhibition against BRD4(1) with and IC50 of 10,000 nM.

References

Filippakopoulos, P., et al. Nature. 2010 Dec 23;468(7327):1067-73.

Application Reference:
1. 
BET bromodomain inhibitors block growth of pancreatic cancer cells in three-dimensional collagen (2014)
2. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology (2014)

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储存温度

(-)-JQ1 27334 5mg -20°C
(-)-JQ1 27335 10mg -20°C

操作手册

1 1

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保存建议 厂家推荐蓝冰运输。当您收到产品后,按照说明书建议保存于-20°C。

 

FAQ

Epigenetic Modulation of Radiation-Induced Diacylglycerol Kinase Alpha Expression Prevents Pro-Fibrotic Fibroblast Response

Chun-Shan Liu, Reka Toth, Pedro Torres-Ayuso

Cancers    |    2021 May 18    |    PubMed ID: 34070078  

BET Inhibition-Induced GSK3β Feedback Enhances Lymphoma Vulnerability to PI3K Inhibitors

Enrico Derenzini, Patrizia Mondello, Anas Younes

Cell reports    |    2020 Aug 29    |    PubMed ID: 30134175 

Bromodomain and extra-terminal domain (BET) proteins regulate melanocyte differentiation

Archit Trivedi, Aanchal Mehrotra, Ivana L. de la Serna

Epigenetics & Chromatin    |    2020 Mar 10    |    PubMed ID: 32151278

Brd4's Bromodomains Mediate Histone H3 Acetylation and Chromatin Remodeling in Pluripotent Cells through P300 and Brg1.

Tao Wu, Yasunao F Kamikawa, Mary E Donohoe

Cell reports    |    2019 Dec 10    |    PubMed ID: 30428346 

The Bromodomain Protein 4 Contributes to the Regulation of Alternative Splicing

Sheetal Uppal, Anne Gegonne, Dinah S. Singer

Cell reports    |    2019 Dec 05    |    PubMed ID: 31747612 

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