Pharmacological profile for inhibition of adenylyl cyclase isoforms
Experiments were performed as described in Figs. 1C, 2C, and 3C. Values are reported as pIC50 ± S.E., where pIC50 is calculated as -log(IC50). n = 3, each performed in duplicate. Statistics (t test) were performed on pIC50 of the indicated isoform versus that of AC5.
| Inhibitor | pIC50 ± S.E. (IC50 in µM) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| AC1 | AC2 | AC3 | AC4 | AC5 | AC6 | AC7 | AC8 | AC9 | |
| SQ22,536 | 4.27 ± 0.09** (54) | 3.71 ± 0.23** (210) | 3.96 ± 0.09** (110) | 3.55 ± 0.04** (280) | 5.46 ± 0.08 (3.5) | 5.25 ± 0.14 (5.8) | 3.38 ± 0.16** (440) | >1000# | >1000# |
| NKY80 | 4.04 ± 0.04** (91) | 3.11 ± 0.12** (780)^ | 4.03 ± 0.05** (94) | 3.95 ± 0.03** (110) | 5.15 ± 0.22 (7.7) | 4.80 ± 0.18 (17) | 3.09 ± 0.03** (810) | >1000# | >1000# |
| Ara-A | 4.31 ± 0.09** (50) | 3.61 ± 0.05** (250) | 4.07 ± 0.01** (85) | 4.03 ± 0.22** (100) | 5.67 ± 0.05 (2.2) | 5.34 ± 0.13* (4.7) | 3.64 ± 0.07** (230) | >1000# | >1000# |
↵* P < 0.05; **P < 0.001; #did not reach 50% activity at 1 mM inhibitor; ^did not reach 50% inhibition in one experiment.