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Adezmapimod (SB203580)

Cat. No. M1781
Adezmapimod (SB203580) Structure
Synonym:

RWJ 64809; PB 203580; Adezmapimod

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 60  USD60 In stock
5mg USD 40  USD40 In stock
10mg USD 55  USD55 In stock
50mg USD 130  USD130 In stock
100mg USD 220  USD220 In stock
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Quality Control & Documentation
Biological Activity

Adezmapimod (SB203580) is a P38 MAPK inhibitor with an IC50 of 0.3-0.5 μM, which is 10 times less selective than SAPK3(106T) and SAPK4(106T), and inhibits PKB phosphorylation with an IC50 of 3-5 μM. Adezmapimod is an autophagy and mitophagy activator and does not disrupt JNK activity.

Product Citations
Customer Product Validations & Biological Datas
Source Food Chem Toxicol (2018). Figure 6. SB203580 (Abmole Bioscience, Houston, TX, USA)
Method i.p.
Cell Lines SPF (specific pathogen free) male BALB/c mice
Concentrations 5 mg/kg
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
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.
Protocol (for reference only)
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
Chemical Information
Molecular Weight 377.43
Formula C21H16FN3OS
CAS Number 152121-47-6
Solubility (25°C) DMSO 20 mg/mL (ultrasonic and warming)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Zhang H, et al. Apoptosis. Induction of autophagy in hepatocellular carcinoma cells by SB203580 requires activation of AMPK and DAPK but not p38 MAPK.

[2] Barancík M, et al. Eur J Pharm Sci. SB203580, a specific inhibitor of p38-MAPK pathway, is a new reversal agent of P-glycoprotein-mediated multidrug resistance.

[3] Newton R, et al. Br J Pharmacol. The MAP kinase inhibitors, PD098059, UO126 and SB203580, inhibit IL-1beta-dependent PGE(2) release via mechanistically distinct processes.

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  Catalog
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Keywords: Adezmapimod (SB203580), RWJ 64809; PB 203580; Adezmapimod supplier, p38 MAPK, inhibitors, activators


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