Interaction of prototypical membrane-permeable sAC inhibitors and the membrane-impermeable P-site inhibitor 2’,5′-dd-3′-ATP with sAC and mACs
pIC50 values are listed. Structures of prototypical sAC inhibitors and 2′,5′-dideoxy-3′-ATP are shown in Figure 15. pIC50 values for ACs 3, 4 and 6 and sGC are not available. 2′,5′-dideoxy-3′-ATP is mechanistically related to the P-site inhibitors documented in Fig. 13 and Table 7.
AC | 2CE | KH7 | RU-0204277 | 2’,5′-dideoxy-3′-ATP |
---|---|---|---|---|
Purified sAC | ∼5.7a | 5.52b | ∼5.0c | 6.16d |
5C1:2C2 | N.D. | N.D. | N.D. | 7.42d |
mAC lysate | ∼4a | no inhibition at 500 μMb | N.D. | 7.40d |
AC1 | ∼4a | N.D. | no inhibition at 50 μMc | 7.43d |
AC2 | ∼4a | N.D. | no inhibition at 50 μMc | 6.66d |
AC5 | ∼4a | N.D. | no inhibition at 50 μMc | 7.43d |
AC7 | ∼5.7a | N.D. | N.D. | N.D. |
AC8 | N.D. | N.D. | no inhibition at 50 μMc | N.D. |
AC9 | N.D. | N.D. | no inhibition at 50 μMc | N.D. |