| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 1g |
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Purity: ≥98%
Adezmapimod hydrochloride (formerly SB-203580 HCl; SB203580; RWJ-64809; RWJ 64809) is a p38 mitogen-activated protein kinase inhibitor (p38MAPK inhibitor) with IC50 of 0.3-0.5 μM in THP-1 cells, it is 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM. In a mouse model, SB203580 inhibits the production of proinflammatory cytokines and proteolytic factors, thereby preventing the development of endometriosis. A competitive ATPsite inhibitor of p38MAPK, SB203580 has a Ki of 21 nM and selectivity that is likely governed by nonconserved regions within or close to the ATP binding pocket.
| Targets |
p38 (IC50 = 50 nM); p38β2 (IC50 = 500 nM)
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| ln Vitro |
SB203580 has an IC50 of 3-5 μm and blocks the proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells when IL-2 is present. Although the concentration needed is a little bit higher and the IC50 is above 10 μM, SB203580 also inhibits IL-2-induced p70S6 kinase activation. With an IC50 in the 3-10 μM range, SB203580 also inhibits the activity of PDK1 in a dose-dependent manner. MAPKAPK2 stimulation by p38-MAPK is inhibited by SB203580 with an IC50 of roughly 0.07 μM, whereas total SAPK/JNK activity is inhibited with an IC50 of 3–10 μM. Higher concentrations of SB203580 cause the ERK pathway to be activated, which then improves the transcriptional activity of NF-κB. Human hepatocellular carcinoma (HCC) cells are induced to undergo autophagy by SB203580.
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| ln Vivo |
SB203580 protects the pig myocardium in an in vivo model from ischemic damage. In the MRL/lpr mouse model of systemic lupus erythematosus (SLE), SB203580 is effective in preventing and treating the illness.
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| Enzyme Assay |
4 μg of sheep anti-PKBα is immobilized on 25 μL of protein G-Sepharose overnight (or 1.5 hours) and washed in Buffer A (50 mm Tris, pH 7.5, 1 mm EDTA, 1 mm EGTA, 0.5 mm Na3VO4, 0.1% β-mercaptoethanol, 1% Triton X-100, 50 mm sodium fluoride, 5 mm sodium pyrophosphate, 0.1 mm phenylmethylsulfonyl fluoride, 1 μg/mL aprotinin, pepstatin, leupeptin, and 1 μm microcystin). The immobilized anti-PKB is then incubated with 0.5 ml of lysate (from 5 × 106 cells) for 1.5 hours and washed three times in 0.5 mL of Buffer A supplemented with 0.5 m NaCl, two times in 0.5 mL of Buffer B (50 mm Tris-HCl, pH 7.5, 0.03% (w/v) Brij-35, 0.1 mm EGTA, and 0.1% β-mercaptoethanol), and twice with 100 μl of assay dilution buffer; 5× assay dilution buffer is 100 mm MOPS, pH 7.2, 125 mm β-glycerophosphate, 25 mm EGTA, 5 mm sodium orthovanadate, 5 mm DTT. To the PKB enzyme immune complex is added 10 μL of assay dilution buffer, 40 μm protein kinase A inhibitor peptide, 100 μm PKB-specific substrate peptide, and 10 μCi of [γ-32P]ATP, all made up in assay dilution buffer. The reaction is incubated for 20 minutes at room temperature with shaking, then samples are pulse spun, and 40 μL of reaction volume are removed into another tube to which is added 20 μL of 40% trichloroacetic acid to stop the reaction. This is mixed and incubated for 5 minutes at room temperature, and 40 μL is transferred onto P81 phosphocellulose paper and allowed to bind for 30 seconds. The P81 piece is washed three times in 0.75% phosphoric acid then in acetone at room temperature. γ-32P incorporation is then measured by scintillation counting.
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| Cell Assay |
In the absence of growth factors, antibiotics, or β-mercaptoethanol supplements, CT6 cells and BA/F3 F7 cells are rested by washing three times in RPMI and culturing overnight in RPMI with 5% fetal calf serum. Preincubation with SB203580 or a vehicle control, as indicated in the figure legends, is performed on 2-5 106 rested CT6 cells in 2 mL of RPMI, 5% fetal calf serum. Following a 5-minute incubation period at 37 °C with 20 ng/ml recombinant human IL-2 stimulation, cells are pelleted in a minifuge for 30 seconds, the medium is aspirated, and the pellet is lysed in the proper buffer. BA/F3 cells are maintained in glutamine-containing RPMI that is additionally supplemented with 5% fetal calf serum and 0.2 μg/mL G418 and stably express deletion mutants of the IL-2 β receptor chain. The cells are then thoroughly washed, allowed to rest for the night, and then washed once more before being activated with IL-2. Such cell preparations contain >90% T cells. The incorporation of [3H]thymidine is measured in cellular proliferation assays.
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| Animal Protocol |
Six-week-old female atymic Nu/Nu mice CAL27 p38WT and p38TM tumors[1]
5 mg/kg/day Intra peritoneal injected daily for 16 consecutive days |
| References |
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| Molecular Formula |
C₂₁H₁₇CLFN₃OS
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| Molecular Weight |
413.90
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| Exact Mass |
413.0764892
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| Elemental Analysis |
C, 60.94; H, 4.14; Cl, 8.56; F, 4.59; N, 10.15; O, 3.87; S, 7.75
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| CAS # |
869185-85-3
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| Related CAS # |
Adezmapimod;152121-47-6
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| Appearance |
Solid powder
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| SMILES |
CS(=O)C1=CC=C(C=C1)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F.Cl
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| InChi Key |
WOSGGXINSLMASH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H16FN3OS.ClH/c1-27(26)18-8-4-16(5-9-18)21-24-19(14-2-6-17(22)7-3-14)20(25-21)15-10-12-23-13-11-15;/h2-13H,1H3,(H,24,25);1H
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| Chemical Name |
4-[4-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-1H-imidazol-5-yl]pyridine;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.04 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.04 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 4% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4160 mL | 12.0802 mL | 24.1604 mL | |
| 5 mM | 0.4832 mL | 2.4160 mL | 4.8321 mL | |
| 10 mM | 0.2416 mL | 1.2080 mL | 2.4160 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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