| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
p38 35 nM (IC50)
p38 MAPK |
|---|---|
| ln Vitro |
p38 MAPK-IN-4 (compound 6) is a p38 MAPK inhibitor with an IC₅0 of 35 nM. It selectively inhibits p38 MAPK activity and effectively suppresses downstream signaling. It can be used to study the role of p38 MAPK in inflammation and immune regulation.
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| ln Vivo |
No detailed in vivo activity data for p38 MAPK-IN-4 has been reported. As a selective p38 MAPK inhibitor, it is expected to exhibit anti‑inflammatory activity in animal models of inflammatory diseases, such as collagen‑induced arthritis (CIA) or LPS‑induced endotoxemia.
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| Enzyme Assay |
For p38 MAPK enzymatic assays, recombinant p38 MAPK protein is incubated with p38 MAPK-IN-4 (0.1‑1000 nM) and a MAPK substrate (e.g., MBP or ATF2) in the presence of ATP (including [gamma‑32P]ATP for radiometric detection). After incubation (30‑60 min at 30degC), the reaction is terminated, and substrate phosphorylation is quantified via scintillation counting, Western blotting, or ELISA.
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| Cell Assay |
p38 MAPK-IN-4 is dissolved in DMSO to a stock solution and diluted in cell culture media (final DMSO ≤0.1%). Cells (e.g., RAW264.7 macrophages or THP‑1 monocytes) are treated with p38 MAPK-IN-4 (1 nM - 10 uM) for 1‑4 h, then stimulated with LPS (1 ug/mL) for an additional 30‑60 min. p38 MAPK activity is assessed by measuring phospho‑p38 or phospho‑ATF2 via Western blotting, or by quantifying pro‑inflammatory cytokines (e.g., IL‑6, TNF‑alpha) using ELISA.
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| Animal Protocol |
No detailed in vivo protocol for p38 MAPK-IN-4 has been reported. For p38 MAPK inhibitors in general, they are formulated in suitable vehicles (e.g., 0.5% methylcellulose, 10% DMSO, 40% PEG400, 5% Tween 80) and administered orally or intraperitoneally to mice (doses typically 5‑50 mg/kg). Efficacy is assessed by measuring cytokine levels or inflammation scores.
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| ADME/Pharmacokinetics |
No detailed PK data for p38 MAPK-IN-4 has been reported. As a small‑molecule p38 MAPK inhibitor, it is expected to have moderate oral bioavailability and a short plasma half‑life, consistent with many kinase inhibitors. Detailed parameters such as half‑life, Cmax, and clearance are not publicly available.
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| Toxicity/Toxicokinetics |
No detailed toxicity data for p38 MAPK-IN-4 has been reported. As a p38 MAPK inhibitor, potential toxicities may include immunosuppression, hepatotoxicity, or effects on cytokine homeostasis. High doses may cause off‑target kinase inhibition, but no toxicology studies have been published to date.
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| References | |
| Additional Infomation |
p38 MAPK-IN-4 (compound 6; CAS: 219138-24-6; formula: C20H13ClFN3O; MW: 365.79) is a selective p38 MAPK inhibitor for research use only. It has not been approved for clinical use, and no clinical trial data has been reported. As with all p38 MAPK inhibitors, careful dose titration is required in cellular assays to avoid non‑specific effects.
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| Molecular Formula |
C20H13CLFN3O
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|---|---|
| Molecular Weight |
365.79
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| Exact Mass |
365.073
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| CAS # |
219138-24-6
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| PubChem CID |
4665
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.687
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
547
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1C2=C(NN(C2=O)C3=CC=C(C=C3)Cl)C4=CC=NC=C4)F
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| InChi Key |
DZFBYHUKZSRPHU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H13ClFN3O/c21-15-3-7-17(8-4-15)25-20(26)18(13-1-5-16(22)6-2-13)19(24-25)14-9-11-23-12-10-14/h1-12,24H
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| Chemical Name |
2-(4-chlorophenyl)-4-(4-fluorophenyl)-5-pyridin-4-yl-1H-pyrazol-3-one
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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 |
| 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) |
DMSO: 20 mg/mL (54.68 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (5.47 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 20.0 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 mg/mL (5.47 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 20.0 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: ≥ 2 mg/mL (5.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7338 mL | 13.6690 mL | 27.3381 mL | |
| 5 mM | 0.5468 mL | 2.7338 mL | 5.4676 mL | |
| 10 mM | 0.2734 mL | 1.3669 mL | 2.7338 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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