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SB203580

Cat. No. M1781
SB203580 Structure
Synonym:

RWJ 64809, PB 203580

Size Price Availability Quantity
10mg USD 50 In stock
50mg USD 120 In stock
100mg USD 200 In stock
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Quality Control
Biological Activity

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.

Protocol
Cell Experiment
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.
Concentrations 0~30 µm
Incubation time 24 h
Animal Experiment
Animal models Systemic lupus erythematosus (SLE) model (female MRL/lpr mice and female C57BL/6 mice)
Formulation Dissolved in drinking water (250 μM)
Dosages 0.1 M/day
Administration orally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 377.43
Formula C21H16FN3OS
CAS Number 152121-47-6
Purity >99%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source Nat Commun (2015). Figure 7. SB203580 (AbMole Bioscience)
Method atrial arrhythmia induction and picrosirius red-stained atrial sections
Cell Lines
Concentrations i.p.4 mg/kg
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.
Rating
Product Citations
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SB203580, RWJ 64809, PB 203580 supplier, p38 MAPK, inhibitors

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