Table 1.
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.