Biological Activity

• Target

  p38 MAPK IC50:0.3-0.5μM

• DescriptionThe stress-activated protein kinase (SAPK) p38 isoforms are mitogen-activated protein kinase (MAPK) family members. MAPKs act as an integration point for multiple biochemical signals, and are involved in a wide variety of cellular processes such as proliferation, differentiation, transcription regulation and development. SB 203580 is a p38 MAPK inhibitor. SB 203580 inhibited the ATPase activity of non-phosphorylated p38 MAPK with a K_m of 9.6 mM. SB 203580 was competitive with ATP with a K_i of 21 nM, detected in a kinetic study of yeast expressed active p38 MAPK^[3]. 24h treatment of SB 203580 dose-dependently inhibited IL-1β-induced PGE₂ release with an EC₅₀ of 0.18 μM^[4]. SB 203580 was dissolved in drinking water at the concentration of 250 μM and orally administrated 0.4 ml/day to MRL/lpr mice aged from 14 to 22 weeks. SB203580 improved renal function by decreasing the levels of proteinuria and serum BUN, ameliorating the pathologic changes of kidney and reducing Ig and C3 depositions in the kidney. Moreover, hepatocytes necrosis, recruitment and proliferation of leucocytes in liver and spleen were found to be inhibited by administration of SB203580^[5].
• Cell Study
• Cell Data

  Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
  HCA2	2.5 μM	Function Assay	-	Inhibits p38 mediated MK2 activation	17964780
  Hela	-	Function Assay	-	Inhibits Tat-induced HIV1 LTR transactivation in human HeLa cells with IC50 of 0.1 μM	18926711
  hESCs	5 μM	Growth Inhibition Assay	-	Induces cardiomyogenic activity assessed as cell growth	23602399

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