The membrane-bound transcription factor ATF6α plays a cytoprotective role in the unfolded protein response (UPR), required for cells to survive ER (endoplasmic reticulum) stress. Ceapin-A7 is a potent and selective inhibitor of ATF6α signaling in response to ER stress with an IC50 of 0.59 μM. Ceapin-A7 sensitized cells to ER stress. U2-OS cells co-incubated with both Tg and Ceapin-A7 showed an almost two-fold increase in sensitivity to ER stress (IC50 = 4.5 nM). Ceapin (0.6-18.9 μM; 4.5 hours) selectively inhibited ATF6α but not ATF6β[1].
Ceapin-A7 细胞实验
Cell Line
Concentration
Treated Time
Description
References
A549 cells
6 µM
24 to 72 hours
Inhibited ATF6 cleavage, reduced virus titer
mSphere. 2021 Jun 30;6(3):e0036121.
Human chondrocytes
500 nM
24 hours
Inhibited ATF6 activation and reduced FGF2 expression
iScience. 2021 Jun 28;24(7):102791.
PBMCs
6 µM
1 hour
Inhibit ATF6 signaling pathway and reduce the expression of ATF6α
Mol Med. 2024 Nov 29;30(1):237.
RA FLSs
1, 2, or 5 µM
24 hours
Inhibited BIRC3 expression
Front Immunol. 2022 Oct 10;13:965708.
CD4+T cells
6 µM
1 hour
Inhibit ATF6 signaling pathway and reduce the differentiation of Th17 cells
Mol Med. 2024 Nov 29;30(1):237.
Bovine pulmonary artery endothelial cells (BPAEC)
20 µM
16, 20, 24, 36, 48 hours
To evaluate the effects of Ceapin-A7 on ATF6 activation and Cofilin phosphorylation. Ceapin-A7 reduced ATF6 activation and Cofilin phosphorylation.
Cell Signal. 2022 Nov;99:110432.
Bovine pulmonary artery endothelial cells (BPAEC)
15 µM
24 hours
To evaluate the effects of Ceapin-A7 on LPS-induced endothelial barrier dysfunction. Ceapin-A7 enhanced LPS-induced VE-cadherin internalization and barrier dysfunction.
Cell Signal. 2022 Nov;99:110432.
Bovine pulmonary artery endothelial cells (BPAEC)
10, 15, 20 µM
24 hours
To evaluate the effects of Ceapin-A7 on ATF6 activation and Cofilin phosphorylation. Ceapin-A7 decreased ATF6 activation and Cofilin phosphorylation.
Cell Signal. 2022 Nov;99:110432.
Bovine pulmonary artery endothelial cells (BPAEC)
1–150 µM
24 hours and 48 hours
To evaluate the effects of Ceapin-A7 on cell viability. Moderate doses (1–25 μM) were non-toxic, while higher doses (50–150 μM) reduced cell viability.
Cell Signal. 2022 Nov;99:110432.
786-O cells
20 µM
5 hours
Inhibited ATF6 activation, reversed the increased expression of PINK1 and BNIP3 caused by NR3C1 knockdown.
J Transl Med. 2023 Oct 8;21(1):701.
ACHN cells
20 µM
5 hours
Inhibited ATF6 activation, reversed the increased expression of PINK1 and BNIP3, and the decreased expression of LC3 and increased expression of P62 caused by NR3C1 knockdown.
J Transl Med. 2023 Oct 8;21(1):701.
Ceapin-A7 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
SKG mice
Ankylosing spondylitis model
Oral administration in drinking water
1 mM
Continuous administration until the end of the experiment
Reduced the number of vessels and osteophytes, inhibited angiogenesis-osteogenesis coupling
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