SML2330
Ceapin-A7
≥98% (HPLC), ATF6α signaling blocker, powder
Sinónimos:
Ceapin-7, N-(1-{[2,4-bis(Trifluoromethyl)phenyl]methyl}-1H-pyrazol-4-yl)-5-(furan-2-yl)-1,2-oxazole-3-carboxamide
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Fórmula empírica (notación de Hill):
C20H12F6N4O3
Número CAS:
Peso molecular:
470.32
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Servicio técnico
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Permítanos ayudarleNombre del producto
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
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.
Clase de almacenamiento
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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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
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
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.