Effects of acyclophostin and Ins(1,4,5)P3 on Ca++release and 3H-Ins(1,4,5)P3 binding measured under identical conditions at pH 8.3 in permeabilized hepatocytes
| Kd | EC50 | EC50/Kd | ||
|---|---|---|---|---|
| nM | ||||
| Ins(1,4,5)P3 | 43 ± 8 | 33 ± 2 | 0.77 ± 0.15 | |
| (0.83 ± 0.05) | (2.69 ± 0.14) | |||
| 2.2 | ||||
| Acyclophostin | 19 ± 6 | 32 ± 5 | 1.69 ± 0.62 | |
| (0.78 ± 0.08) | (2.90 ± 0.84) | |||
Permeabilized hepatocytes loaded with Ca++ and resuspended in modified BM at 2°C (see Experimental Procedures) were used to measure the effects of acylophostin and Ins(1,4,5)P3 on Ca++ release and 3H-Ins(1,4,5)P3 binding under identical conditions. Results are mean ± S.E.M. of four or five independent determinations; h are shown in parentheses. Bold text denotes the acylophostin/Ins(1,4,5)P3 ratio.