TABLE 8

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.

AC2CEKH7RU-02042772’,5′-dideoxy-3′-ATP
Purified sAC∼5.7a5.52b∼5.0c6.16d
5C1:2C2N.D.N.D.N.D.7.42d
mAC lysate∼4ano inhibition at 500 μMbN.D.7.40d
AC1∼4aN.D.no inhibition at 50 μMc7.43d
AC2∼4aN.D.no inhibition at 50 μMc6.66d
AC5∼4aN.D.no inhibition at 50 μMc7.43d
AC7∼5.7aN.D.N.D.N.D.
AC8N.D.N.D.no inhibition at 50 μMcN.D.
AC9N.D.N.D.no inhibition at 50 μMcN.D.

  • N.D., not determined. Specific experimental conditions for analysis of inhibitors varied in the different studies and are given in:

  • ↵a Steegborn et al. (2005);

  • ↵b Bitterman et al. (2013);

  • ↵c Ramos-Espiritu et al. (2016);

  • ↵d Gille et al. (2004).