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.
|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.
|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.|
Nat Commun. 2015 Jan 19;6:6018.
Increased atrial arrhythmia susceptibility induced by intense endurance exercise in mice requires TNFα.
SB203580 purchased from AbMole
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.
|Related p38 MAPK Products|
TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM. IC50 value: 20 nM. TA-02 is a novel compound with similar cardiogenic properties as SB203580 and SB202190. TA-02 especially inhibits TGFBR-2.
Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.
Losmapimod (GW856553) is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively.
VX-745 is a potent and selective inhibitor of p38α with IC50 of 10 nM, 22-fold greater selectivity versus p38β and no inhibition to p38γ.
TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1.
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