Table 2

Effects of analogs of adenophostin A on Ca2+ release from the intracellular stores of permeabilized hepatocytes

EC50nHnReference
nM
 1, InsP3 145  ± 102.20  ± 0.1610
 2, Adenophostin A14.7  ± 2.42.26  ± 0.156
 3, Purinophostin18  ± 12.04  ± 0.2410 Marwood et al., 2000b
 4 47  ± 71.82  ± 0.214
 5, Imidophostin108  ± 202.51  ± 0.647 Marwood et al., 2000b
 6, Ribophostin329  ± 202.88  ± 1.407
 7, Furanophostin329  ± 482.18  ± 0.105 Marwood et al., 1999
 8, Glc(2′,3,4)P3 1867  ± 642.76  ± 0.104 Marchant et al., 1997a
 9 2414  ± 1734.99  ± 1.843 Rosenberg et al., 2000
10 ∼10 μMnd5 Rosenberg et al., 2000
11, xylo -Adenophostin28  ± 82.50  ± 0.778
12, manno -Adenophostin180  ± 162.85  ± 0.558
13, Uridophostin34  ± 22.45  ± 0.2910
14 48  ± 61.55  ± 0.144
15 99  ± 32.47  ± 0.074
16 62  ± 32.03  ± 0.094
17 491  ± 692.32  ± 0.354
18 Inactive2-a nd3
19, Acyclophostin209  ± 122.48  ± 0.186 Beecroft et al., 1999
20 487  ± 582.51  ± 1.003 Rosenberg et al., 2001
21 2694  ± 2761.78  ± 0.433 Rosenberg et al., 2001
22 >10 μM2-b nd5 Rosenberg et al., 2001
23 Inactive2-a nd5 Rosenberg et al., 2001
24, FuranophostinPS2 1682  ± 3462.30  ± 0.273
25 33  ± 3 μM3.05  ± 0.393 Beecroft et al., 1999
26 ∼20 μMnd6
27, Sucr(3,4,3′)P3 5409  ± 1102.60  ± 0.083 Marchant et al., 1997a
28, Trehal(3,4,2′,4′)P4 1271  ± 462.53  ± 0.433 Marchant et al., 1997a
29, Trehal(3,4,3′,4′)P4 2466  ± 292.37  ± 0.273 Marchant et al., 1997a
30 1372  ± 2912.29  ± 0.364

The EC50 and Hill coefficient (nH) for Ca2+ mobilization evoked by each of the ligands is shown for n independent experiments. Because the experiments were performed over a substantial period, each assay was accompanied by a parallel measurement of InsP3-evoked Ca2+ release to allow the activity of each analog to be calibrated relative to the response to InsP3 (see under Experimental Procedures). The data shown in this table show the results before calibration to the relevant InsP3 response.

    • ↵2-a  No significant release of Ca2+ with 10 μM of the analog.

    • ↵2-b  27 ± 5% of the InsP 3-sensitive Ca2+ stores released by 10 μM of 22.

    • nd, not determined.