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Table 1 In vitro inhibitory effects of SB-203580 and VX-745 on p38 and cytokine release

From: P38 MAP kinase inhibitors as potential therapeutics for the treatment of joint degeneration and pain associated with osteoarthritis

IC50 (nM)
Compound P38aa TNFab (THP-1 cells) TNFac (PBMC) IL-1ßc (PBMC)
SB-203580 136 ± 64 72 ± 15 16 ± 6 20 ± 8
VX-745 35 ± 14 29 ± 14 14 ± 8 15 ± 4
  1. aHuman p38α kinase was assayed using ATF2.
  2. bTNFα release from the human monocytic cell line THP-1 was measured by ELISA 4 h after stimulation with LPS.
  3. cTNFα and IL-1β release from human peripheral blood mononuclear cells was measured by ELISA 16 h after stimulation with LPS. All data are expressed as the mean ± S.D.