SML2330
Ceapin-A7
≥98% (HPLC)
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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About This Item
Fórmula empírica (notación de Hill):
C20H12F6N4O3
Número de CAS:
Peso molecular:
470.32
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
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assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
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.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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The membrane-bound transcription factor ATF6α plays a cytoprotective role in the unfolded protein response (UPR), required for cells to survive ER stress. Activation of ATF6α promotes cell survival in cancer models. We used cell-based screens to discover and develop Ceapins
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