3-Isoxazolecarboxamide, N-[1-[[2,4-bis(trifluoromethyl)phenyl]methyl]-1H-pyrazol-4-yl]-5-(2-furanyl)-

Ceapin-A7 (2323027-38-7) is a selective inhibitor (IC50 = 590 nM) of transcription factor ATF6α, one of the three branches of the unfolded protein response.1 It inhibits activation of ATF6α in response to ER stress without inhibiting ER-bound transcription factors ATF6 or SREBP or the IRE1 or PERK branches of the UPR. Ceapin-A7 also show no toxicity to unstressed cells. It induces neomorphic association of the ER and peroxisomes by directly tethering the cytosolic domain of ATF6a to the peroxisomal transporter ABCD3 without inhibiting its transporter activity.2 See companion activator 10-3973.

Ceapin-A7 is a selective blocker of ATF6α signaling in response to ER stress, with an IC50 of 0.59 μM. Ceapin-A7 can be used to explore both the mechanism of activation of ATF6α and its role in pathological settings[1].

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[1] CIARA M GALLAGHER. Ceapins are a new class of unfolded protein response inhibitors, selectively targeting the ATF6α branch.[J]. eLife, 2016. DOI:10.7554/elife.11878
[2] SANDRA ELIZABETH TORRES. Ceapins block the unfolded protein response sensor ATF6α by inducing a neomorphic inter-organelle tether.[J]. eLife, 2019. DOI:10.7554/elife.46595