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. 2017 Mar 22;7:294. doi: 10.1038/s41598-017-00455-7

Table 1.

Summary of I942 and I178 activities in vitro.

Experimental Techniques EPAC1 EPAC2
I942 I178 I942 I178
8NBD-cAMP Competition Assays IC50 ≈ 35 μM IC50 ≈ 40 μM IC50 ≈ 35 μM IC50 ≈ 40 μM
GEF Activation (no cAMP) AC50 ≈ 50 μM AC50 ≈ 200 μM N/A N/A
GEF Inhibition (with cAMP) IC50 ≈ 300 μM IC50 ≈ 500 μM IC50 ≈ 110 μM IC50 ≈ 250 μM
NMR Strong, Specific Interaction Strong, Specific Interaction Strong, Specific Interaction Weak, specific interaction

The table shows the relative activities of I942 and I178 against EPAC1 and EPAC2 in NMR, CNBD binding assays (8NBD-cAMP Competition Assays) and in vitro GEF activity assays, in the presence or absence of cAMP. IC50 refers to the ability of I942 and I178 to compete with 8NBD-cAMP binding to isolated CNBs or inhibit EPAC GEF activity in the presence of cAMP. AC50, refers to the ability of I942 and I178 to promote EPAC GEF activity in the absence of cAMP. N/A refers to the inability of I942 and I178 to promote GEF activity of EPAC2.