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| 25mg |
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IRAK inhibitor 1 is a potent IRAK-4 inhibitor with IC50 of 216 nM, is poorly active against JNK-1 and JNK-2 with IC50 of 3.801 μM, and >10 μM, respectively.
| ln Vitro |
Although less effective against JNK-1 and JNK-2, IRAK inhibitor 1 exhibits considerable activity in the IRAK-4 enzyme assay [1]. A recent addition to the IRAK family, IRAK-4 has special functional characteristics. The closest human homologue to Pelle is IRAK-4. Overexpression of IRAK-4 can activate the NF-κB and mitogen-activated protein (MAP) kinase pathways. Endogenous IRAK-4 interacts with IRAK-1 and TRAF6 in an IL-1-dependent manner. Most remarkably, IRAK-4 depends on its kinase activity to activate NF-κB, unlike other IRAKs. Moreover, IRAK-4 has the ability to phosphorylate IRAK-1, and dominant-negative IRAK-4 overexpression prevents IL-1-induced IRAK-1 activation and modification, suggesting that IRAK-4 is a key component of Toll/IL Early signaling by the -1 receptor (upstream of IRAK-1). Like other IRAKs, IRAK-4 can activate the NF-κB and MAPK signal transduction pathways. It also shares the same domain structure. It is not functionally redundant with IRAK-1, but it associates quickly and momentarily in an IL-1-dependent way with TRAF6 and IRAK-1. To activate NF-κB, IRAK-4, an active protein kinase, must have kinase activity. Upstream of IRAK-1, IRAK-4 may act as an IRAK-1 activator [2].
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| References |
[1]. Buckley GM, et al. IRAK-4 inhibitors. Part II: A structure-based assessment of imidazo[1,2-a]pyridine binding. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3291-5.
[2]. Li S, et al. IRAK-4: a novel member of the IRAK family with the properties of an IRAK-kinase. Proc Natl Acad Sci U S A. 2002 Apr 16;99(8):5567-72. |
| Molecular Formula |
C17H19N5
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|---|---|
| Molecular Weight |
293.36626
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| CAS # |
1042224-63-4
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| SMILES |
C1(C2=CN=C3N2C=CC=C3)=CC=CC(NC4CCNCC4)=N1
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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 : ~16.67 mg/mL (~56.82 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (5.69 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 16.7 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: ≥ 1.67 mg/mL (5.69 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 16.7 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: ≥ 1.67 mg/mL (5.69 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 | 3.4087 mL | 17.0433 mL | 34.0866 mL | |
| 5 mM | 0.6817 mL | 3.4087 mL | 6.8173 mL | |
| 10 mM | 0.3409 mL | 1.7043 mL | 3.4087 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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