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.
Toxicol Lett. 2023 Aug 1;384:73-85.
Co-exposure to polystyrene microplastics and di-(2-ethylhexyl) phthalate aggravates allergic asthma through the TRPA1-p38 MAPK pathway
Adezmapimod (SB203580) purchased from AbMole
journal of environmental sciences. 2022 Nov 29.
Ethylene thiourea exposure induces neurobehavioral toxicity in zebrafish by disrupting axon growth and neuromuscular junctions
Adezmapimod (SB203580) purchased from AbMole
Environ Pollut. 2021 Feb 1;270:116051.
Bisphenol AF induces apoptosis via estrogen receptor beta (ERβ) and ROS-ASK1-JNK MAPK pathway in human granulosa cell line KGN
Adezmapimod (SB203580) purchased from AbMole
Ecotoxicol Environ Saf. 2021 Sep 1;220:112341.
Cadmium induces apoptosis of human granulosa cell line KGN via mitochondrial dysfunction-mediated pathways
Adezmapimod (SB203580) purchased from AbMole
Ecotoxicol Environ Saf. 2021 Jan 15;208:111429.
Bisphenol A induces apoptosis through GPER-dependent activation of the ROS/Ca 2+-ASK1-JNK pathway in human granulosa cell line KGN
Adezmapimod (SB203580) purchased from AbMole
Cancer Immunol Res. 2020 Oct;8(10):1273-1286.
An IL6-Adenosine Positive Feedback Loop between CD73 + γδTregs and CAFs Promotes Tumor Progression in Human Breast Cancer
Adezmapimod (SB203580) purchased from AbMole
Mar Drυgs. 2020 Aug 17;18(8):429.
Comparison of Physicochemical Characteristics and Macrophage Immunostimulatory Activities of Polysaccharides from Chlamys farreri
Adezmapimod (SB203580) purchased from AbMole
Toxicol Appl Pharmacol. 2020 May 15;395:114981.
Exposure to Diisononyl Phthalate Promotes Atopic March by Activating of NF-κB and p38 MAPK
Adezmapimod (SB203580) purchased from AbMole
Int J Oncol. 2020 Jul;57(1):197-212.
G6PD Facilitates Clear Cell Renal Cell Carcinoma Invasion by Enhancing MMP2 Expression Through ROS‑MAPK Axis Pathway
Adezmapimod (SB203580) purchased from AbMole
Front Immunol. 2019 Apr 26;10:913.
IL-12 Expands and Differentiates Human Vγ2Vδ2 T Effector Cells Producing Antimicrobial Cytokines and Inhibiting Intracellular Mycobacterial Growth.
Adezmapimod (SB203580) purchased from AbMole
Food Chem Toxicol. 2018 Feb 12;114:78-87.
Exposure to diisodecyl phthalate exacerbated Th2 and Th17-mediated asthma through aggravating oxidative stress and the activation of p38 MAPK
Adezmapimod (SB203580) purchased from AbMole
Nat Commun. 2015 Jan 19;6:6018.
Increased atrial arrhythmia susceptibility induced by intense endurance exercise in mice requires TNFα.
Adezmapimod (SB203580) purchased from AbMole
Cell Experiment | |
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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 | |
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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 |
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 |
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.
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