SB 202190 Inhibitor CAS No. 152121-30-7

Cat. No.	Name	Size	Price	Add Cart
KI0261	SB 202190	25 mg	$163.8
KI0261	SB 202190	100 mg	$414.4

Chemical Characteristic

Product Name	SB 202190
CAS No.	152121-30-7
Molecular Weight	331.34
Formula	C₂₀H₁₄N₃OF
Chemical Name	4-(4-(4-fluorophenyl)-5-(pyridin-4-yl)-1H-imidazol-2-yl)phenol
Smiles	c1(ccc(cc1)c1nc(c([nH]1)c1ccncc1)c1ccc(cc1)F)O
Chemical Structure

Biological activities

SB202190 is an effective and selective inhibitor of p38 with an IC50 of 30 nM. SB202190 suppresses genes encoding interferon-induced gene 15, neuroleukin, radiation-inducible immediate-early gene-1, A20, IL-1β, and superoxide dismutase by more than 50%. SB202190 inhibits ISG15, neuroleukin, A20, and IEX-1 mRNA with half-maximal between 41 and 123 nM. Furthermore, the inhibition of SB202190 for gene activation is stimulus-dependent. Although SB202190 inhibits the LPS response half maximally at 100 nM, concentrations as high as 3.3 µM has no effect on neuroleukin mRNA levels induced by IFN-a. SB202190 exhibits a broad impact on LPS-induced monocyte activation, suppressing the production of both cytokine and non-cytokine mediators. ^[1] SB202190 is sufficient to induce cell death, with typical apoptotic features such as nucleus condensation and intranucleosomal DNA fragmentation. SB202190 stimulates the activity of CPP32-like caspases, and the apoptotic effect of SB202190 is completely blocked by the protease inhibitor benzyloxycarbonyl-Val-Ala-Asp-fluoromethyl ketone and expression of bcl-2. In addition, SB202190 is able to potentiate apoptosis induced by Fas (APO-1) ligation or UV irradiation. SB202190 is sufficient to induce apoptosis through activation of DEVD-sensitive caspases, and p38b inhibits apoptosis. ^[2] In vivo, the inhibition of SB202190 for p38 half maximally is at roughly 41 nM. ^[1]

Protocols

Stock solutions of 10 or 20 mM SB 202190 respectively are prepared in DMSO. ^[3]

References

[1] Manthey CL, et al. SB202190, a selective inhibitor of p38 mitogen-activated protein kinase, is a powerful regulator of LPS-induced mRNAs in monocytes. J Leukoc Biol. 1998, 64(3): 409-417. [2] Nemoto S, et al. Induction of Apoptosis by SB202190 through Inhibition of p38β Mitogen-activated Protein Kinase. J Biol Chem. 1998, 273(26): 16415-16420. [3] Meyer-ter-Vehn T, et al. Helicobacter pylori Activates Mitogen-activated Protein Kinase Cascades and Induces Expression of the Proto-oncogenes c-fos and c-jun. J Biol Chem. 2000, 275(21): 16064-16072.

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