Catalog No.S1076 Synonyms: RWJ 64809, PB 203580
Molecular Weight(MW): 377.43
SB203580 is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM.
Cited by 53 Publications
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C57BL/6 male mice (8 weeks, Harlan) were pretreated with by intravenous injections with PERY or SCR peptides (15 mg/kg) or DMSO. The following day, mice were treated with 1.5% dextran sodium sulfate (DSS) in drinking water for 7 days followed by 3 days of normal drinking water. During DSS administration, mice were treated every other day (total of five intravenous injections). Control groups included nontreated mice (no DSS, no treatment) and mice receiving PERY peptide with normal drinking water (PERY only, no DSS). Mice were then euthanized and analyzed. Colitis was evaluated using (C) hematoxylin and eosin (H&E) histological sections of the colons (top) and their magnifications (bottom). Scale bar, 2 mm.
Science, 2018, 11(525), doi: 10.1126/scisignal.aao3428. SB203580 purchased from Selleck.
A, effects of p38 inhibitor SB203580 (1, 5, and 10 μM) on SRP72 protein expression was evaluated by WB using antibodies against human SRP72,SRP54, and GAPDH. A decreased intensity of SRP72 bands was noted when using the inhibitor at 5 μM concentration at 240 min (lane 6) and 10 μM at 120 and 240 min (lanes 8 and 9). B, results were analyzed and RUA illustrated, finding significant results at 5 μM, 240 versus 0 min, and 10 μM, 240 versus 0 and 120 versus 0 min, respectively, (p<0.05).
J Biol Chem 2010 285, 32824-32833. SB203580 purchased from Selleck.
A, effect of p38 MAPK inhibitor SB203580 (1, 5, and 10 μM) on SRP72 phosphorylation was evaluated. Jurkat cells were stimulated with rhIL-1, harvested at 0, 120, and 240 min, lysed, and immunoprecipitated using anti-human SRP19 andWBusing anti-phosphoserine antibodies. A decreased intensity of SRP72 band was found when using the inhibitor at concentration of 1μM at 240 min and 5 and 10 μM at 120 and 240 min. B, results were analyzed and RUA illustrated, finding significant results at 1 μM 240 versus 120, 5, and 10 μM at 120 versus 0 and 240 versus 0 min *, p<0.05.
J Biol Chem 2010 285, 32824–32833. SB203580 purchased from Selleck.
We used real time RT-PCR to investigate the effects of SB203580 on SRP72 mRNA expression. All the samples were treated under the same experimental conditions used in protein tests done by WB, and phosphorylation was measured indirectly by IP-WB. The results did not show significant changes on the mRNA expression of SRP72 after the treatment with these inhibitors.
J Biol Chem 2010 285, 32824–32833. SB203580 purchased from Selleck.
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Choose Selective p38 MAPK Inhibitors
|Description||SB203580 is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM.|
|Features||First reported p38 inhibitor.|
SB203580 inhibits the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC50 of 3–5 μm. SB203580 also inhibits IL-2-induced p70S6 kinase activation, although the concentration required is slightly higher with an IC50 above 10 μm. SB203580 also inhibits the activity of PDK1 in a dose-dependent manner with an IC50 in the 3–10 μm range.  SB203580 inhibits p38-MAPK stimulation of MAPKAPK2 with an IC50 of approximately 0.07 μM, whereas inhibits total SAPK/JNK activity with an IC50 of 3–10 μM. SB203580 at higher concentrations activates the ERK pathway, which subsequently enhances NF-κB transcriptional activity.  SB203580 induces autophagy in human hepatocellular carcinoma (HCC) cells. 
|In vivo||SB203580 protects pig myocardium against ischemic injury in an in vivo model. SB203580 is effective to prevent and treat the disease in MRL/lpr mice model of Systemic lupus erythematosus (SLE). |
Cellular receptor kinase phosphorylation assay :4 μg of sheep anti-PKBα is immobilized on 25 μL of protein G-Sepharose overnight (or 1.5 hours) and washed in Buffer A (50 mm Tris, pH 7.5, 1 mm EDTA, 1 mm EGTA, 0.5 mm Na3VO4, 0.1% β-mercaptoethanol, 1% Triton X-100, 50 mm sodium fluoride, 5 mm sodium pyrophosphate, 0.1 mm phenylmethylsulfonyl fluoride, 1 μg/mL aprotinin, pepstatin, leupeptin, and 1 μm microcystin). The immobilized anti-PKB is then incubated with 0.5 ml of lysate (from 5 × 106 cells) for 1.5 hours and washed three times in 0.5 mL of Buffer A supplemented with 0.5 m NaCl, two times in 0.5 mL of Buffer B (50 mm Tris-HCl, pH 7.5, 0.03% (w/v) Brij-35, 0.1 mm EGTA, and 0.1% β-mercaptoethanol), and twice with 100 μl of assay dilution buffer; 5× assay dilution buffer is 100 mm MOPS, pH 7.2, 125 mm β-glycerophosphate, 25 mm EGTA, 5 mm sodium orthovanadate, 5 mm DTT. To the PKB enzyme immune complex is added 10 μL of assay dilution buffer, 40 μm protein kinase A inhibitor peptide, 100 μm PKB-specific substrate peptide, and 10 μCi of [γ-32P]ATP, all made up in assay dilution buffer. The reaction is incubated for 20 minutes at room temperature with shaking, then samples are pulse spun, and 40 μL of reaction volume are removed into another tube to which is added 20 μL of 40% trichloroacetic acid to stop the reaction. This is mixed and incubated for 5 minutes at room temperature, and 40 μL is transferred onto P81 phosphocellulose paper and allowed to bind for 30 seconds. The P81 piece is washed three times in 0.75% phosphoric acid then in acetone at room temperature. γ-32P incorporation is then measured by scintillation counting.
-  Ferdinand V. Lali, et al. J Biol Chem, 2000, 275(10), 7395-402.
-  Birkenkamp KU, et al. Br J Pharmacol, 2000, 131(1): 99-107.
-  Zhang H, et al. Apoptosis, 2011
|In vitro||DMSO||43 mg/mL (113.92 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||RWJ 64809, PB 203580|
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