Ceapin-A7

Ceapin-A7 is an inhibitor of activating transcription factor 6α (ATF6α; IC₅₀ = 0.59 µM in a reporter assay).¹ It is selective for ATF6α over ATF6β at 18.9 µM. Ceapin-A7 (6 µM) sensitizes U2OS osteosarcoma cells to the sarcoplasmic/endoplasmic reticulum Ca²⁺-ATPase (SERCA) inhibitor and ER stress inducer thapsigargin (Item No. 10522). Chondrocyte-conditioned media from primary human chondrocytes pre-incubated with ceapin-A7 (0.5 µM) 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 µM) inhibits viral RNA production in Vero cells infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2).³

WARNING This product is not for human or veterinary use.

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 branch. Elife 5, e11878 (2016).

2. Ma, M., Li, H., Wang, P., et al. ATF6 aggravates angiogenesis-osteogenesis coupling during ankylosing spondylitis by mediating FGF2 expression in chondrocytes. iScience 24(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 infection. PLoS Pathog. 17(6), e1009644 (2021).