Table 2 Inhibition of arachidonic acid release

From: Next generation thiazolyl ketone inhibitors of cytosolic phospholipase A2 α for targeted cancer therapy

 

AA release

% Inhib

EC50 µM (95% CI)

GK470

67 ± 4

0.38 (0.25 to 0.58)

GK401

53 ± 6

0.63 (0.45 to 0.88)

GK420

97 ± 14

0.09 (0.05 to 0.16)

GK419

71 ± 21

0.50 (0.31 to 0.78)

GK427

56 ± 5

0.67 (0.58 to 0.78)

GK403

57 ± 12

0.79 (0.59 to 1.07)

GK440

88 ± 8

0.18 (0.11 to 0.30)

GK402

23 ± 8

6.7 (4.4 to 10.67)

GK439

80 ± 10

0.32 (0.23 to 0.46)

GK428

12 ± 7

9.34 (5.72 to 17.07)

GK449

58 ± 15

0.78 (0.49 to 1.26)

  1. SW982 synoviocytes were stimulated with IL-1β for 4 h in the absence or presence of 0.2, 1 or 5 µM inhibitor. The mean % inhibition of arachidonic acid (AA) release ± stdev at 1 µM is shown for each inhibitor as well as the calculated EC50 values with 95% confidence intervals (CI). Data are from 4 or 3 (GK402) biological replicates.
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