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 is a specific inhibitor of p38-MAPK pathway and is a new reversal agent of P-glycoprotein-mediated multidrug resistance. SB203580 suppresses the development of endometriosis by down-regulating proinflammatory cytokines and proteolytic factors in a mouse model. SB203580 also inhibits protein kinase B (PKB, also known as Akt) and TLR signaling pathway.
Food Chem Toxicol. 2018 Feb 12;114:78-87.
Nat Commun. 2015 Jan 19;6:6018.
Increased atrial arrhythmia susceptibility induced by intense endurance exercise in mice requires TNFα.
SB203580 purchased from AbMole
|Source||Food Chem Toxicol (2018). Figure 6. SB203580 (Abmole Bioscience, Houston, TX, USA)|
|Cell Lines||SPF (specific pathogen free) male BALB/c mice|
|Incubation Time||0 to 20 days|
|Results||To clarify the underlying mechanism of DIDP exposure on Th17 type asthmatic lesions, SB203580 was used to block the p38 MAPK signaling pathway.|
|Source||Nat Commun (2015). Figure 7. SB203580 (AbMole Bioscience)|
|Method||atrial arrhythmia induction and picrosirius red-stained atrial sections|
|Incubation Time||6 weeks|
|Results||Treatment of mice with the p38 inhibitor SB203580 during the 6-week exercise period completely prevented AF as well as atrial fibrosis.|
|Cell lines||CT6 cells,BA/F3 cells and PBMC/T cells|
|Preparation method||2–5 × 106 rested CT6 cells were resuspended in 2 ml of RPMI, 5% fetal calf serum and preincubated with inhibitors or vehicle control as indicated in figure legends. Cells were then stimulated with 20 ng/ml recombinant human IL-2 for 5 min at 37 °C and pelleted in a minifuge for 30 s, medium was aspirated, and the pellet was lysed in the appropriate buffer. BA/F3 cells stably expressing deletion mutants of IL-2 receptor β chain (a generous gift from Professor T. Taniguchi, Tokyo, Japan) were maintained in glutamine containing RPMI further supplemented with 5% fetal calf serum and 0.2 μg/ml G418 (Calbiochem-Novabiochem) as described previously. Human peripheral blood mononuclear cells were prepared from buffy coat leukophoresis residues (North London Blood Transfusion Service, Colindale, London UK) and activated with 50 ng/ml OKT3 for 48 h. The cells were then washed extensively, rested overnight, and washed again before activating with IL-2; such cell preparations were >90% T cells . Cellular proliferation assays were performed by measurement of [3H]thymidine incorporation as described previously.|
|Incubation time||24 h|
|Animal models||Systemic lupus erythematosus (SLE) model (female MRL/lpr mice and female C57BL/6 mice)|
|Formulation||Dissolved in drinking water (250 μM)|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Induction of autophagy in hepatocellular carcinoma cells by SB203580 requires activation of AMPK and DAPK but not p38 MAPK.
Zhang H, et al. Apoptosis. 2012 Apr;17(4):325-34. PMID: 22170404.
SB203580, a specific inhibitor of p38-MAPK pathway, is a new reversal agent of P-glycoprotein-mediated multidrug resistance.
Barancík M, et al. Eur J Pharm Sci. 2001 Aug;14(1):29-36. PMID: 11457647.
The MAP kinase inhibitors, PD098059, UO126 and SB203580, inhibit IL-1beta-dependent PGE(2) release via mechanistically distinct processes.
Newton R, et al. Br J Pharmacol. 2000 Jul;130(6):1353-61. PMID: 10903976.
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SB 239063 is a potent and selective p38 MAPK inhibitor (IC50 = 44 nM for p38α). SB 239063 displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580.
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