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アッセイ
≥98% (HPLC)
フォーム
powder
色
white to pink
溶解性
DMSO: 2 mg/mL, clear
保管温度
2-8°C
SMILES記法
FC(F)(F)c1c(ccc(c1)C(F)(F)F)C[n]2ncc(c2)NC(=O)c3n[o]c(c3)c4[o]ccc4
InChI
1S/C20H12F6N4O3/c21-19(22,23)12-4-3-11(14(6-12)20(24,25)26)9-30-10-13(8-27-30)28-18(31)15-7-17(33-29-15)16-2-1-5-32-16/h1-8,10H,9H2,(H,28,31)
InChI Key
UJTDYOXTXGBHEG-UHFFFAOYSA-N
生物化学的／生理学的作用
Potent and specific ER stress-induced ATF6α signaling blocker that does not affect IRE1 or PERK branches of UPR, nor proteolytic processing of ATF6β or SREBP.
The pyrazole amide Ceapin-A7 is a potent and highly specific ER stress-induced ATF6α signaling blocker (IC50 = 590 nM by HEK293T-based ERSE-luciferase reporter assay, ATF6α target transcripts GRP78/ERO1B/HERPUD1 induction IC50 = 459/522/614 nM in U2OS cells; ER stress by 100 nM Thapsigargin) that does not affect IRE1 or PERK branches of the unfolded protein response (UPR), nor proteolytic processing of its close homolog ATF6β or SREBP. Ceapin-A7 sensitizes U2-OS cells to ER stress-induced death (thapsigargin EC50 = 4.5/7.1 nM with/without 6 μM Ceapin-A7) without impacting the viability of unstressed cells.
保管分類コード
11 - Combustible Solids
WGK
WGK 3
引火点(°F)
Not applicable
引火点(℃)
Not applicable
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
Jan Code
SML2330-BULK:
SML2330-25MG:
SML2330-5MG:
SML2330-VAR:
最新バージョンのいずれかを選択してください：
試験成績書（COA）
Lot/Batch Number
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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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