Ceapin-A7

Ceapin-A7 is an inhibitor of activating transcription factor 6α (ATF6α; IC₅₀ = 0.59 ?M in a reporter assay).¹ It is selective for ATF6α over ATF6β at 18.9 ?M. Ceapin-A7 (6 ?M) sensitizes U2OS osteosarcoma cells to the sarcoplasmic/endoplasmic reticulum Ca²⁺-ATPase (SERCA) inhibitor and ER stress inducer thapsigargin . Chondrocyte-conditioned media from primary human chondrocytes pre-incubated with ceapin-A7 (0.5 ?M) prior to stimulation with TNF-α, IFN-γ, or IL-17 has a reduced ability to induce tube formation in human umbilical vein endothelial cells (HUVECs).² Ceapin-A7 (15 ?M) inhibits viral RNA production in Vero cells infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2).³

1.Gallagher, C.M., Garri, C., Cain, E.L., et al.Ceapins are a new class of unfolded protein response inhibitors, selectively targeting the ATF6α branchElife5e11878(2016) 2.Ma, M., Li, H., Wang, P., et al.ATF6 aggravates angiogenesis-osteogenesis coupling during ankylosing spondylitis by mediating FGF2 expression in chondrocytesiScience24(7)102791(2021) 3.Echavarría-Consuegra, L., Cook, G.M., Busnadiego, I., et al.Manipulation of the unfolded protein response: A pharmacological strategy against coronavirus infectionPLoS Pathog.17(6)e1009644(2021)