| Size | Price | Stock | Qty |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
p38 MAP Kinase Inhibitor IV specifically targets the ATP-binding site of p38α and p38β MAP kinases. It acts as an ATP-competitive inhibitor. The IC50 values for p38α and p38β are 0.13 μM and 0.55 μM, respectively. It also inhibits p38χ and p38δ with IC50 values of 5.47 μM and 8.63 μM, respectively.
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| ln Vitro |
For p38α, β, χ, and δ, the IC50 values of p38 MAP Kinase Inhibitor IV (MT4) are 0.13, 0.55, 5.47, and 8.63μM, in that order. With IC50 values of 22 and 44 nM, respectively, p38 MAP Kinase Inhibitor IV inhibits the release of TNF-α and IL-1β in PBMC [1].
In vitro, p38 MAP Kinase Inhibitor IV demonstrates potent inhibition of p38α and p38β MAPK with IC50 values of 0.13 μM and 0.55 μM, respectively. It inhibits the release of TNF-α and IL-1β in peripheral blood mononuclear cells (PBMCs) with IC50 values of 22 nM and 44 nM, respectively. The compound is cell-permeable. |
| ln Vivo |
In vivo, p38 MAP Kinase Inhibitor IV is expected to inhibit p38 MAPK-mediated signaling pathways. By inhibiting the release of pro-inflammatory cytokines such as TNF-α and IL-1β, it may have anti-inflammatory effects. However, specific in vivo data is not detailed in the available literature.
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| Enzyme Assay |
Cell-free assays for p38 MAP Kinase Inhibitor IV are performed to measure its inhibition of p38 kinase activity. In these assays, the recombinant p38 enzyme is incubated with a substrate peptide and ATP in the presence of varying concentrations of the inhibitor. The amount of phosphorylated substrate is then measured to calculate the IC50.
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| Cell Assay |
In vitro cell-based assays for p38 MAP Kinase Inhibitor IV are performed to evaluate its effects on cells. For example, its ability to inhibit the release of TNF-α and IL-1β can be assessed in PBMCs. Cells are treated with the compound and stimulated to produce cytokines, and the levels of cytokines in the culture medium are measured using ELISA.
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| Animal Protocol |
In vivo animal experiments for p38 MAP Kinase Inhibitor IV would involve models of inflammation or other diseases where p38 MAPK plays a role. However, specific protocols for this compound are not detailed in the available literature. Its use is limited to research.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) data for p38 MAP Kinase Inhibitor IV is not provided in the available literature. It is a cell-permeable compound with a molecular weight of 456.9. For storage, it is typically kept as a powder at -20°C.
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| Toxicity/Toxicokinetics |
Toxicological data for p38 MAP Kinase Inhibitor IV is not available in the public literature. As a research compound, its safety profile has not been extensively characterized. Its use is strictly for research purposes.
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| References | |
| Additional Infomation |
p38 MAP Kinase Inhibitor IV is a research-grade compound used to study the role of p38 MAPK in various biological processes. It is a specific ATP-competitive inhibitor of p38α and p38β. It has not been approved for clinical use. All information is for research reference only.
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| Molecular Formula |
C12H4O4SCL6
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|---|---|
| Molecular Weight |
456.94076
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| Exact Mass |
453.796
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| CAS # |
1638-41-1
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| PubChem CID |
3816490
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| Appearance |
White to off-white solid powder
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| Density |
1.854 g/cm3
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| Boiling Point |
590ºC at 760 mmHg
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| Flash Point |
310.6ºC
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| LogP |
6.931
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
23
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| Complexity |
488
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1C(Cl)=C(Cl)C=C(Cl)C=1O)(C1C(Cl)=C(Cl)C=C(Cl)C=1O)(=O)=O
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| InChi Key |
AKUKHICVNCCQHN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H4Cl6O4S/c13-3-1-5(15)9(19)11(7(3)17)23(21,22)12-8(18)4(14)2-6(16)10(12)20/h1-2,19-20H
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| Chemical Name |
3,4,6-trichloro-2-(2,3,5-trichloro-6-hydroxyphenyl)sulfonylphenol
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1885 mL | 10.9424 mL | 21.8847 mL | |
| 5 mM | 0.4377 mL | 2.1885 mL | 4.3769 mL | |
| 10 mM | 0.2188 mL | 1.0942 mL | 2.1885 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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