IRAK-1-4 Inhibitor I
IRAK-1-4 Inhibitor I is an inhibitor of both IRAK-1 and IRAK-4 with IC50 values of 0.3μM and 0.2μM , respectively [1].
IL-1 receptor-associated kinases play important roles in signal transduction. There are totally four members of the IRAKs, they are IRAK-1, IRAK-2, IRAK-M and IRAK-4. IRAK-4 can activate NF-κB and MAPK pathways and it is shown that the inhibition of IRAK-4 can be an anti-inflammatory therapy. IRAK-1-4 Inhibitor I is an analog of an Initial IRAK-4 inhibitor hit, which is screened out from a small molecule li brary against IRAK-4. With the less basic N-ethylenemorpholine moiety, IRAK-1-4 Inhibitor I has a higher potency than other analogs. Additionally, it does not show any cytotoxicity in a 72 h proliferation assay in HeLa cells(ED50 >30μM) [1].
References:
[1] Jay P. Powers, Shyun Li, Juan C. Jaen, Jinqian Liu, Nigel P. C. Walker, Zhulun Wang and Holger Wesche. Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-4. Bioorganic & Medicinal Chemistry Letters. 2006, 16: 2842–2845.
- 1. Pan B, Gao J, et al. "Selective inhibition of interleukin-1 receptor-associated kinase 1 ameliorates lipopolysaccharide-induced sepsis in mice." Int Immunopharmacol. 2020;85:106597. PMID:32422509
- 2. Zha C, Zhang W, et al. "Anti-β(2)GPI/β(2)GPI induces neutrophil extracellular traps formation to promote thrombogenesis via the TLR4/MyD88/MAPKs axis activation." Neuropharmacology. 2018 Jun 5;138:140-150. PMID:29883691
- 3. Ghorpade DS, Ozcan L, et al. "Hepatocyte-secreted DPP4 in obesity promotes adipose inflammation and insulin resistance." Nature. 2018 Mar 29;555(7698):673-677. PMID:29562231
- 4. Chang MC, Chan CP, et al. "Areca nut components stimulate ADAM17, IL-1α, PGE2 and 8-isoprostane production in oral keratinocyte: role of reactive oxygen species,EGF and JAK signaling." Oncotarget. 2016 Mar 29;7(13):16879-94. PMID:26919242
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 395.41 |
| Cas No. | 509093-47-4 |
| Formula | C20H21N5O4 |
| Synonyms | IRAK-1/4 Inhibitor I |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥19.75 mg/mL in DMSO |
| Chemical Name | N-[1-(2-morpholin-4-ylethyl)benzimidazol-2-yl]-3-nitrobenzamide |
| SDF | Download SDF |
| Canonical SMILES | C1COCCN1CCN2C3=CC=CC=C3N=C2NC(=O)C4=CC(=CC=C4)[N+](=O)[O-] |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
HeLa cells |
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Preparation method |
Soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reaction Conditions |
72 hrs |
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Applications |
In a 72-hr proliferation assay, IRAK-1-4 Inhibitor I did not show any cytotoxicity in HeLa cells (ED50 > 30 μM). In addition, IRAK-1-4 Inhibitor I significantly inhibited IRAK-1 and IRAK-4 (IC50 = 0.3 μM and 0.2 μM, respectively). |
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References: [1]. Jay P. Powers, Shyun Li, Juan C. Jaen, Jinqian Liu, Nigel P. C. Walker, Zhulun Wang and Holger Wesche. Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-4. Bioorganic & Medicinal Chemistry Letters. 2006, 16: 2842–2845. |
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| Description | IRAK-1-4 Inhibitor I is an inhibitor of interleukin-1 receptor associated kinase (IRAK) with IC50 values of 0.3 μM and 0.2 μM for IRAK-1 and IRAK-4, respectively . | |||||
| Targets | IRAK-1 | IRAK-4 | ||||
| IC50 | 0.3 μM | 0.2 μM | ||||
Quality Control & MSDS
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