| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
IRAK inhibitor 2 targets interleukin-1 receptor-associated kinase 4 (IRAK4), a serine/threonine kinase that plays a critical role in the initiation of innate immune responses. By inhibiting IRAK4, it blocks the downstream activation of NF-κB and MAPK signaling pathways, thereby reducing the production of pro-inflammatory cytokines. Its IC50 against IRAK4 is less than 20 μM.
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| ln Vitro |
In vitro, IRAK inhibitor 2 (Compound 23) exhibits an IC50 of less than 20 μM against IRAK4 in a cell-free kinase assay. It demonstrates potent inhibition of IRAK4 enzymatic activity, confirming its role as a targeted inhibitor of this key inflammatory kinase. The compound is used to study the effects of IRAK4 inhibition on downstream signaling and cytokine production in various cell types.
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| ln Vivo |
In vivo, IRAK inhibitor 2 has been used in preclinical research models to study innate immunity, inflammatory signaling, and autoimmune disease mechanisms. While specific standalone in vivo efficacy data for this compound are not extensively published, its mechanism of action suggests potential for reducing inflammation in animal models of immune-mediated diseases.
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| Enzyme Assay |
The in vitro IRAK4 kinase assay involves incubating the enzyme with a peptide substrate and ATP in the presence of varying concentrations of IRAK inhibitor 2. The amount of phosphorylated substrate is measured using a luminescent or fluorescent detection system, and the IC50 is calculated from the dose-response curve.
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| Cell Assay |
In vitro cell-based assays for IRAK inhibitor 2 utilize immune cells stimulated with TLR agonists or IL-1β to induce an inflammatory response. Cells are treated with the compound, and the production of pro-inflammatory cytokines such as TNF-α and IL-6 is measured by ELISA.
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| Animal Protocol |
In vivo animal experiments for IRAK inhibitor 2 would typically involve models of inflammatory or autoimmune diseases, such as collagen-induced arthritis or LPS-induced endotoxemia. The compound would be administered orally or intraperitoneally, and endpoints such as cytokine levels, tissue histopathology, and disease scores would be assessed.
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| ADME/Pharmacokinetics |
IRAK inhibitor 2 has a molecular weight of 306.32 g/mol and is soluble in DMSO at ≥50 mg/mL. For in vivo studies, it can be formulated as a clear solution in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline. Powder formulations are stable for up to 3 years at -20°C and 2 years at 4°C.
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| Toxicity/Toxicokinetics |
In vitro, IRAK inhibitor 2 shows no significant change in cell viability at concentrations up to 10 μM, but decreases viability at high millimolar concentrations. As a research compound, it is not intended for human use, and comprehensive in vivo toxicity studies have not been reported. Standard safety precautions for handling chemical reagents should be followed.
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| References | |
| Additional Infomation |
IRAK inhibitor 2 is a research compound with no clinical approval. It is a valuable tool for studying IRAK4 biology and the role of this kinase in inflammatory and immune diseases. It is used in drug discovery programs to explore the therapeutic potential of IRAK4 inhibitors for the treatment of autoimmune and inflammatory disorders.
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| Molecular Formula |
C17H14N4O2
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|---|---|
| Molecular Weight |
306.31866
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| Exact Mass |
306.112
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| CAS # |
928333-30-6
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| PubChem CID |
135900142
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.067
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
23
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| Complexity |
389
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OPKXXSDVMPBIOF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H14N4O2/c22-13-5-3-12(4-6-13)15-11-19-17-8-7-16(20-21(15)17)18-10-14-2-1-9-23-14/h1-9,11,22H,10H2,(H,18,20)
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| Chemical Name |
4-[6-(furan-2-ylmethylamino)imidazo[1,2-b]pyridazin-3-yl]phenol
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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 : ≥ 50 mg/mL (~163.23 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (8.98 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 27.5 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2646 mL | 16.3228 mL | 32.6456 mL | |
| 5 mM | 0.6529 mL | 3.2646 mL | 6.5291 mL | |
| 10 mM | 0.3265 mL | 1.6323 mL | 3.2646 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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