Figure 7

A representative inhibitor (Compound 12) that strongly decreases FRET and inhibits both Ca²⁺-ATPase activities and Ca²⁺-transport. (A) Table showing the four subcategories (C) of inhibitors (N, Compounds 11–18) and their effects on the Ca²⁺ATPase activity and Ca²⁺-uptake as strong (S), moderate (M), or mild. (B) Chemical structure of DS27464324 (Compound 12). (C) CRC of normalized FRET E shows decreasing FRET in response to [Compound 12] in 2CS biosensor in live HEK cells. (D) CRC shows inhibition of Ca²⁺-ATPase activity in pCSR under both [Ca²⁺]_MAX (black) and [Ca²⁺]_MID (red). (E) CRC shows inhibition of Ca²⁺-uptake in pCSR under [Ca²⁺]_MAX (black) and [Ca²⁺]_MID (red). ΔF_MAX, ΔF_MID, C₁₀, and EC₅₀ are defined and reported in Table 1 for panels C, D, and E. Data are presented as mean ± SEM, n = 3, *p < 0.05.