SML2330
Ceapin-A7
≥98% (HPLC), ATF6α signaling blocker, powder
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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关于此项目
经验公式（希尔记法）:
C20H12F6N4O3
化学文摘社编号:
分子量:
470.32
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
产品名称
Ceapin-A7, ≥98% (HPLC)
assay
≥98% (HPLC)
form
powder
color
white to pink
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
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
Biochem/physiol Actions
一种有效且特异性的ER应激诱导的ATF6α信号传导阻滞剂，不会影响UPR的IRE1或PERK分支，也不会影响ATF6β或SREBP的蛋白水解过程。
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。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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
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
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
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| SML2330-25MG | 04061838694652 |
| SML2330-5MG | 04061838694669 |