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Merck
CN

SML2330

Sigma-Aldrich

Ceapin-A7

≥98% (HPLC)

别名:

Ceapin-7, N-(1-{[2,4-双(三氟甲基)苯基]甲基} -1H-吡唑-4-基)-5-(呋喃-2-基)-1,2-恶唑-3-羧酰胺

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About This Item

经验公式(希尔记法):
C20H12F6N4O3
分子量:
470.32
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77

检测方案

≥98% (HPLC)

形式

powder

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

2-8°C

生化/生理作用

吡唑酰胺Ceapin-A7是一种强效且高度特异性的ER应激诱导的ATF6α信号传导阻滞剂(通过基于HEK293T的ERSE-萤光素酶报告基因检测得出IC50 = 590 nM,U2OS细胞中ATF6α目标转录本GRP78/ERO1B/HERPUD1诱导的IC50 = 459/522/614 nM;由100 nM毒胡萝卜素所引起的ER应激),它不会影响未折叠蛋白应答(UPR)的IRE1或PERK分支,也不会影响与其紧密同源的ATF6β或SREBP的蛋白水解过程。Ceapin-A7可使U2-OS细胞对内质网应激诱导的死亡(在6 μM Ceapin-A7存在或不存在时的毒胡萝卜素EC50 = 4.5/7.1 nM)更加敏感,且不会影响未受应激细胞的活力。

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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Justine Lebeau et al.
Cell reports, 22(11), 2827-2836 (2018-03-15)
Endoplasmic reticulum (ER) stress is transmitted to mitochondria and is associated with pathologic mitochondrial dysfunction in diverse diseases. The PERK arm of the unfolded protein response (UPR) protects mitochondria during ER stress through the transcriptional and translational remodeling of mitochondrial
Ciara M Gallagher et al.
eLife, 5 (2016-07-21)
The membrane-bound transcription factor ATF6α is activated by proteolysis during endoplasmic reticulum (ER) stress. ATF6α target genes encode foldases, chaperones, and lipid biosynthesis enzymes that increase protein-folding capacity in response to demand. The off-state of ATF6α is maintained by its
Shuhong Sun et al.
Cell chemical biology, 30(1), 22-42 (2023-01-12)
Genetic variation in alpha-1 antitrypsin (AAT) causes AAT deficiency (AATD) through liver aggregation-associated gain-of-toxic pathology and/or insufficient AAT activity in the lung manifesting as chronic obstructive pulmonary disease (COPD). Here, we utilize 71 AATD-associated variants as input through Gaussian process
Heike Kroeger et al.
Science signaling, 11(517) (2018-02-15)
ATF6 encodes a transcription factor that is anchored in the endoplasmic reticulum (ER) and activated during the unfolded protein response (UPR) to protect cells from ER stress. Deletion of the isoform activating transcription factor 6α (ATF6α) and its paralog ATF6β
Rossella Benedetti et al.
Biomedicines, 9(9) (2021-09-29)
Polyphenols have been shown to possess several beneficial properties, including properties involved in the prevention or treatment of cancer. Among these polyphenols, a leading role is played by dihydroxyphenylethanol (DPE), the most powerful antioxidant compound contained in the olive oil.

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