| Size | Price | Stock | Qty |
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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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Purity: ≥98%
| Targets |
Ferroptosis ; p38α (IC50 = 50 nM); p38β (IC50 = 100 nM)
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|---|---|
| ln Vitro |
SB 202190 significantly inhibits both basal and anti-Fas antibody-induced MAPKAPK 2 activity in a dose-dependent manner. When expressed, bcl-2 can stop the activation of CPP32-like caspases, which are required to cause cell death in Jurkat and HeLa cells when SB202190 is used alone. p38α is a positive regulator of p38β but a negative regulator of SB202190-induced apoptosis. [2] The UVB-induced COX-2 mRNA and protein expression in HaCaT cells are both markedly and strongly inhibited by SB 202190. [3] In renal tubular cells (normal rat kidney-52E), SB 202190 treatment inhibits the expression of genes that are profibrotic (procollagen-Ialpha1) and proinflammatory (monocyte chemoattractant protein-1) when induced by transforming growth factor (TGF)-beta1.[4] In A549 cells, treatment with SB 202190 results in the phosphorylation of JNK in a dose- and time-dependent manner, as well as the phosphorylation of the transcription factor ATF-2 and an increase in AP-1 DNA binding. [6] THP-1 and MV4-11 cell growth is accelerated by SB 202190 treatment. The fact that SB 202190 increases c-Raf and ERK phosphorylation suggests that the Ras-Raf-MEK-Mitogen-Activated Protein Kinase (MAPK) pathway activation is responsible for the leukemia cell growth that is brought on by SB 202190. [7]
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| ln Vivo |
In the passive transfer mouse model, administration of SB 202190, which inhibits p38, prevents PV IgG-induced blister formation.[5] Treatment with SB 202190 results in a statistically significant survival advantage over control in the endotoxin model of sepsis.[8]
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| Enzyme Assay |
The p38α and p38β are measured in 25 mM Tris-HCl, pH 7.5, with 0.1 mM EGTA and 0.33 mg/mL of myelin basic protein as the substrate. When using [γ-33P]ATP, assays can be run manually for 10 minutes at 30 °C in 50 L incubations or automatically with a Biomek 2000 Laboratory Automation Workstation in a 96-well format for 40 minutes at room temperature in 25 L incubations. Magnesium acetate and ATP have concentrations of 10 and 0.1 mM, respectively. MgATP is used to start every assay. To end a manual assay, aliquots of the incubation are spotted on phosphocellulose paper and then submerged in 50 mM phosphoric acid. Robotic assays are ended by adding 5 μL of 0.5 M phosphoric acid, followed by the spotting of aliquots onto P30 filter mats. All papers are then cleaned four times in 50 mM phosphoric acid to remove ATP, once in acetone (for manual incubations) or methanol (for robotic incubations), dried, and radioactivity is counted.
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| Cell Assay |
Serum-starved cells are treated for 24 hours with various concentrations of SB 202190. Flow cytometry analysis is done after either a trypan blue exclusion or a propidium iodide exclusion is used to determine the viability of the cells. H33258 staining is used to see the apoptotic nuclei.
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| Animal Protocol |
C57BL/6J mice injected i.d. with a sterile solution of either control IgG or PV IgG
12.5 μg Administered via i.d. |
| References |
[1]. Biochem J . 2000 Oct 1;351(Pt 1):95-105. [2]. J Biol Chem . 1998 Jun 26;273(26):16415-20. [3]. Oncogene . 2001 Jun 28;20(29):3921-6. [4]. J Pharmacol Exp Ther . 2006 Oct;319(1):8-19. [5]. Proc Natl Acad Sci U S A . 2006 Aug 22;103(34):12855-60. [6]. Cell Signal . 2008 Apr;20(4):675-83. [7]. Leuk Res . 2009 May;33(5):693-9. [8]. J Surg Res . 2009 Mar;152(1):46-53. [9]. Cancer Res . 2011 Feb 1;71(3):1041-9. |
| Molecular Formula |
C20H14N3OF
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|---|---|
| Molecular Weight |
331.34
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| Exact Mass |
331.11
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| Elemental Analysis |
C, 72.50; H, 4.26; F, 5.73; N, 12.68; O, 4.83
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| CAS # |
152121-30-7
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| Related CAS # |
SB 202190 hydrochloride;350228-36-3
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| Appearance |
white solid powder
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| SMILES |
C1=CC(=CC=C1C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F)O
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| InChi Key |
QHKYPYXTTXKZST-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H14FN3O/c21-16-5-1-13(2-6-16)18-19(14-9-11-22-12-10-14)24-20(23-18)15-3-7-17(25)8-4-15/h1-12,25H,(H,23,24)
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| Chemical Name |
4-[4-(4-fluorophenyl)-5-pyridin-4-yl-1H-imidazol-2-yl]phenol
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| Synonyms |
FHPI; SB-202190; SB202190; SB202190
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0180 mL | 15.0902 mL | 30.1805 mL | |
| 5 mM | 0.6036 mL | 3.0180 mL | 6.0361 mL | |
| 10 mM | 0.3018 mL | 1.5090 mL | 3.0180 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Inhibiting p38MAPK prevents clinical blistering in PV passive transfer mice. Neonatal C57BL/6J mice were injected i.d. with either PV IgG (1.5 mg of IgG/g body weight) (Left) or PV IgG (1.5 mg of IgG/g body weight) plus SB202190 (Right). After 18 h, the skin of neonatal mice from the test and control groups was examined clinically. PV IgG-treated mice have a positive Nikolsky’s sign (white arrows), demonstrating loss of epithelial cell–cell adhesion. In contrast, mice treated with the SB202190 and PV IgG have a negative Nikoslky’s sign, indicating that epithelial adhesion remains intact. Proc Natl Acad Sci U S A. 2006 Aug 22; 103(34): 12855–12860. |
Inhibition of PV IgG-mediated p38MAPK and HSP27 phosphorylation in skin of PV IgG plus SB202190-treated mice. Neonatal C57BL/6 WT mice were injected i.d. with control IgG (CON; 1 mg of IgG/g body weight), PV IgG (1 mg of IgG/g body weight), or SB202190 and then PV IgG (PV IgG plus SB202190). Skin biopsies were obtained after 18 h of treatment and extracted in IEF lysis buffer. Proc Natl Acad Sci U S A. 2006 Aug 22; 103(34): 12855–12860. |
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