SB 203580 Inhibitor CAS No. 152121-47-6

Cat. No.	Name	Size	Price
KI0457	SB 203580	25 mg	$236
	SB 203580	50 mg	$432
	SB 203580	100 mg	$592
	SB 203580	250 mg	$752

Chemical Characteristic

Product Name	SB 203580
CAS No.	152121-47-6
Molecular Weight	377.43
Formula	C₂₁H₁₆N₃FOS
Chemical Name	4-(4-Fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)-1H-imidazole
Smiles	c1(nc(c([nH]1)c1ccncc1)c1ccc(cc1)F)c1ccc(cc1)S(=O)C
Chemical Structure

Biological activities

SB203580 is a selective cytokine suppressive binding protein/p38 kinase (p38 MAPK) inhibitor. SB203580 inhibits the proliferation of cell in a p38 MAPK independent manner. The IC50 of SB203580 against p38 MAPK is 48 nM.^[1] SB203580 gives rise to autophagy of human hepatocellular carcinoma (HCC) cells. SB203580 not only elevates GFP-LC3-positive cells with GFP-LC3 dots, but also causes accumulation of autophagosomes. In addition, SB203580 increases the levels of microtubule-associated protein light chain 3 and Beclin 1. SB203580 induces the phosphorylation of adenosine monophosphate-activated protein kinase (AMPK) and p53. However, SB203580 suppresses the phosphorylation of death-associated protein kinase (DAPK). Prevention of AMPK, p53, or DAPK attenuates SB203580-caused autophagy.^[2] SB 203580 inhibits reactivating kinase (RK) in vitro with an IC50 of 0.6 μM. SB 203580 prevents the activation of MAPKAP kinase-2 and the phosphorylation of heat shock protein (HSP) 27 in response to interleukin-1, cellular stresses and bacterial endotoxin.^[3] SB 203580 inhibits c-Raf with an IC50 of 2 μM in vitro. SB 203580 also stimulates a significant activation of c-Raf in vivo.^[4] Prevention of p38 induced by SB 203580 leads to the almost complete reduction of phorbol myristate acetate-induced MMP-9 secretion but not of urokinase-type plasminogen activator secretion. Phorbol myristate acetate-enhanced in vitro invasion is fully inhibited by SB 203580, whereas p38 suppression has little effect on growth.^[5] SB203580 prevents platelet aggregation caused by prostaglandin H2 and the conversion of prostaglandin H2 to thromboxane A2 in intact platelets. SB203580 also suppresses this pathway in platelet microsome preparations, suggesting a direct inhibitory effect on thromboxane synthase.^[6] SB203580 inhibits the production of inflammatory cytokine in vivo in both mice and rats with IC50 values of 15 to 25 mg/kg. SB 203580 generates therapeutic activity in collagen-induced arthritis in DBA/LACJ mice. At a dose of 50 mg/kg, SB 203580 leads to significant prevention of paw inflammation and serum amyloid protein levels. SB 203580 which is administered p.o. at the doses of 30 and 60 mg/kg also produces antiarthritic activity in adjuvant-induced arthritis in the Lewis rat. ^[7]

References

[1] Huang M, et al. Inhibition of nucleoside transport by p38 MAPK inhibitors. J Biol Chem. 2002 , 277(32): 28364-28367. [2] Zhang H, et al. Induction of autophagy in hepatocellular carcinoma cells by SB203580 requires activation of AMPK and DAPK but not p38 MAPK. Apoptosis. 2012, 17(4): 325-334. [3] Cuenda A, et al. SB 203580 is a specific inhibitor of a MAP kinase homologue which is stimulated by cellular stresses and interleukin-1. FEBS Lett. 1995, 364(2): 229-233. [4] Hall-Jackson CA, et al. Effect of SB 203580 on the activity of c-Raf in vitro and in vivo. Oncogene. 1999, 18(12): 2047-2054. [5] Simon C, et al. Inhibition of the p38 mitogen-activated protein kinase by SB 203580 blocks PMA-induced Mr 92,000 type IV collagenase secretion and in vitro invasion. Cancer Res. 1998, 58(6): 1135-1139. [6] Simon C, et al. Inhibition of the p38 mitogen-activated protein kinase by SB 203580 blocks PMA-induced Mr 92,000 type IV collagenase secretion and in vitro invasion. Cancer Res. 1998, 58(6): 1135-1139. [7] Badger AM, et al. Pharmacological profile of SB 203580, a selective inhibitor of cytokine suppressive binding protein/p38 kinase, in animal models of arthritis, bone resorption, endotoxin shock and immune function. J Pharmacol Exp Ther. 1996, 279(3): 1453-1461.

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