| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
IRAK inhibitor 4 targets IRAK4, a serine/threonine kinase that plays a critical role in signaling downstream of the interleukin-1 receptor (IL-1R) and Toll-like receptors (TLRs). By inhibiting IRAK4, it can block the production of pro-inflammatory mediators by macrophages and dendritic cells.
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| ln Vitro |
The inability of DCs and macrophages to produce proinflammatory mediators in response to Mycobacterium bovis and Mycobacterium tuberculosis is caused by IRAK-4 deficiency. E stimulated IRAK-4-/- cells. Coli LPS demonstrated a considerable decrease in p65 phosphorylation as well as delayed activation kinetics of all examined signaling proteins [1]. IRAK1/4 (20 μM) inhibits the production of IL-6 mediated by LPS. IRAK1/4 inhibitors do not cause AM to have less p38 phosphorylation. The combination of IRAK1/4 and Rip2 inhibitors inhibits TLR2-mediated cytokine production in sarcoidosis PBMCs and AMs [2]. IRAK4 is overexpressed and activated in T-ALL. When patient T-ALL cells are compared to thymic or peripheral blood T cells, IRAK4 mRNA levels are higher [3].
In vitro, IRAK inhibitor 4 is a potent inhibitor of IRAK4. It is used to study the role of IRAK4 in inflammatory signaling. Lack of IRAK-4 activity impairs the production of pro-inflammatory mediators by macrophages and DCs in response to M. bovis and M.. |
| ln Vivo |
In comparison to IRAK-4+/+ or IRAK-4+/-mice, IRAK-4-/- mice exhibited a markedly decreased survival rate following aerosol infection. In all organs at 15, 30, and 60 days after infection, the bacterial burden is higher in IRAK-4-/-mice [1]. Combination therapy using IRAK1/4 inhibitors and ABT-737 has been shown to be more effective in treating MCL1 but not BCL-xL in vivo [3].
In vivo, IRAK inhibitor 4 is used in research to study the inflammatory response. By inhibiting IRAK4, it can modulate the production of pro-inflammatory mediators, making it a valuable tool for studying immune signaling and inflammation. |
| Enzyme Assay |
In vitro enzyme assays for IRAK inhibitor 4 involve measuring its inhibition of IRAK4 kinase activity. These assays use purified recombinant enzyme and a peptide substrate. The compound is incubated with the enzyme and substrates, and phosphorylation is quantified. Its potency is expressed as an IC50 value.
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| Cell Assay |
Cellular assays for IRAK inhibitor 4 are conducted using immune cells such as macrophages or dendritic cells. Cells are stimulated with IL-1 or TLR ligands in the presence of the compound, and the production of pro-inflammatory cytokines is measured to assess its inhibitory activity.
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| Animal Protocol |
In vivo animal studies for IRAK inhibitor 4 are conducted in models of inflammation. Animals are treated with the compound, and the production of inflammatory mediators and the severity of the inflammatory response are assessed.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of IRAK inhibitor 4 are characteristic of a small molecule. It has a molecular weight of 620.66 and a molecular formula of C33H35F3N6O3. Its exact PK parameters are not detailed in the provided literature.
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| Toxicity/Toxicokinetics |
The toxicological profile of IRAK inhibitor 4 is not fully detailed. As a research compound, its safety is evaluated in preclinical studies. It is for research use only and is not for human therapeutic use. Standard safety precautions should be followed.
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| References |
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| Additional Infomation |
IRAK inhibitor 4 is an inhibitor of IRAK4. It is used in research to study inflammatory signaling pathways. Its mechanism involves blocking the production of pro-inflammatory mediators. It is available for research use only.
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| Molecular Formula |
C33H35N6O3F3
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|---|---|
| Molecular Weight |
620.6646
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| Exact Mass |
620.272
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| CAS # |
1012104-68-5
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| Related CAS # |
IRAK inhibitor 4 (trans);2070014-89-8
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| PubChem CID |
24797387
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| Appearance |
Off-white to light brown solid powder
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| LogP |
7.47
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
45
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| Complexity |
982
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)CCNC(=O)C1=CC2=C(C=C1)N(C(=N2)NC3=NNC4=C3C=C(C=C4)C5=CC=CC=C5OC(F)(F)F)C6CCC(CC6)O
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| InChi Key |
QZMAOGLWCNTFCG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C33H35F3N6O3/c1-19(2)15-16-37-31(44)21-8-14-28-27(18-21)38-32(42(28)22-9-11-23(43)12-10-22)39-30-25-17-20(7-13-26(25)40-41-30)24-5-3-4-6-29(24)45-33(34,35)36/h3-8,13-14,17-19,22-23,43H,9-12,15-16H2,1-2H3,(H,37,44)(H2,38,39,40,41)
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| Chemical Name |
1-(4-hydroxycyclohexyl)-N-(3-methylbutyl)-2-[[5-[2-(trifluoromethoxy)phenyl]-1H-indazol-3-yl]amino]benzimidazole-5-carboxamide
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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 : ~12.5 mg/mL (~20.14 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.01 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 12.5 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: ≥ 1.25 mg/mL (2.01 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6112 mL | 8.0559 mL | 16.1119 mL | |
| 5 mM | 0.3222 mL | 1.6112 mL | 3.2224 mL | |
| 10 mM | 0.1611 mL | 0.8056 mL | 1.6112 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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