IRAK-1-4 Inhibitor I
Based on 11 publication(s) in Google Scholar
IRAK-1-4 Inhibitor I is an inhibitor of interleukin-1 receptor-associated kinase 1/4 (IRAK 1/4) with IC50s of 0.2 μM and 0.3 μM, respectively.
For research use only. We do not sell to patients.
- Purity: 99.90%
- CAS No.: 509093-47-4
- Formula: C20H21N5O4
- Molecular Weight:395.41
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) IRAK-1-4 Inhibitor I
More- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- J Clin Invest. 2026 Jun 9;136(14):e201124. [Abstract]
- Arch Toxicol. 2023 Jun;97(6):1783-1794. [Abstract]
- Oncogene. 2020 Sep;39(36):5888-5901. [Abstract]
- Clin Transl Med. 2022 Jun;12(6):e850. [Abstract]
- Environ Health. 2020 Aug 1;19(1):87. [Abstract]
- Antibiotics (Basel). 2020 Jan 17;9(1):33. [Abstract]
- Sci Rep. 2016 Jun 8:6:27460. [Abstract]
- J Virol. 2026 Jun 12:e0042826. [Abstract]
- J Immunol. 2021 Jul 1;207(1):115-124. [Abstract]
- Mol Biol Rep. 2026 Feb 4;53(1):361. [Abstract]
Customer Validation & Images
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WB
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WB
Biological Activity
IC50: 0.2 μM (IRAK-4), 0.3 μM (IRAK-1)[1]
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Cell Line
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Type | Value | Description | References |
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| HeLa | ED50 |
>30 μM
Compound: 46
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Antiproliferative activity against human HeLa cell line after 72 hrs
Antiproliferative activity against human HeLa cell line after 72 hrs
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[PMID: 16563752] |
IRAK-1-4 Inhibitor I has IC50 greater than the highest concentration tested (10 μM) against a panel of 27 other kinases, including the most closely homologous (outside of the IRAK family) Lck and pp60SRC. Additionally, IRAK-1-4 Inhibitor I does not show any signs of cytotoxicity in a 72 h proliferation assay in HeLa cells (ED50>30 μM). Significant inhibition of IRAK-1 is observed with IRAK-1-4 Inhibitor I (IRAK-1 IC50=0.3 μM)[1]. IRAK-1/4 inhibitor eliminates the LPS-induced increases in Bcl10, NF-κB, and IL-8. IRAK-1/4 mediates LPS-induced IL-8 activation and functions upstream of Bcl10. The LPS-induced increase in Bcl10 declines by 73% (from 5.18±0.22 to 2.36±0.08 ng/mL), and the IL-8 response decline by 60% (from 2.64±0.31 to 1.14±0.08 ng/mL)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 509093-47-4
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Appearance Solid
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Molecular Weight 395.41
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Formula C20H21N5O4
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Color White to yellow
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SMILES
O=C(C1=CC=CC([N+]([O-])=O)=C1)NC2=NC3=CC=CC=C3N2CCN4CCOCC4
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Synonyms
IRAK-1/4 Inhibitor I
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (11)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
J Clin Invest
Single-cell analysis of fetal testis reveals dysfunction of human Leydig cells in Klinefelter syndrome. [Abstract]2026 Jun 9;136(14):e201124. PMID: 42262893 -
Arch Toxicol
The tick saliva peptide HIDfsin2 promotes the tick-borne virus SFTSV replication in vitro by enhancing p38 signal pathway. [Abstract]2023 Jun;97(6):1783-1794. PMID: 37148319 -
Oncogene
Restoring MLL reactivates latent tumor suppression-mediated vulnerability to proteasome inhibitors. [Abstract]2020 Sep;39(36):5888-5901. PMID: 32733069
IRAK-1-4 Inhibitor I purchased from MedChemExpress. Usage Cited in: Oncogene. 2020 Sep;39(36):5888-5901. [Abstract]
The indicated cells are treated with IRAK1/4 inhibitor for 48 h. Nucleoplasm and chromatin-bound fractions are purified and immunoblots of the indicated antibodies are analyzed. Upon IRAK1/4 inhibitor treatment, while both chromatin-bound and free nucleoplasmic MLL are proportionally increased in the parental cells, only nucleoplasmic MLL is increased in the resistant cells.
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Clin Transl Med
Uterus globulin associated protein 1 (UGRP1) binds podoplanin (PDPN) to promote a novel inflammation pathway during Streptococcus pneumoniae infection. [Abstract]2022 Jun;12(6):e850. PMID: 35652821 -
Environ Health
Dibutyl phthalate promotes juvenile Sertoli cell proliferation by decreasing the levels of the E3 ubiquitin ligase Pellino 2. [Abstract]2020 Aug 1;19(1):87. PMID: 32738922 -
Antibiotics (Basel)
2020 Jan 17;9(1):33. PMID: 31963532
IRAK-1-4 Inhibitor I purchased from MedChemExpress. Usage Cited in: Antibiotics (Basel). 2020 Jan 17;9(1):33. [Abstract]
Huh7.5.1 cells are infected with J399EM at an MOI of 0.1, and then treated with different concentrations of IRAK-1/4 inhibitor I for 72 h. The expression level of the HCV core protein is determined by western blotting. The IRAK-1/4 inhibitor I is dissolved in dimethyl sulfoxide (DMSO) and the DMSO without IRAK-1/4 inhibitor I is used as a negative control.
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Sci Rep
Cinnamaldehyde and allopurinol reduce fructose-induced cardiac inflammation and fibrosis by attenuating CD36-mediated TLR4/6-IRAK4/1 signaling to suppress NLRP3 inflammasome activation. [Abstract]2016 Jun 8:6:27460. PMID: 27270216 -
J Virol
Highly pathogenic porcine reproductive and respiratory syndrome virus nonstructural protein 1 interacts with TRAF6 to activate the TAK1/p38/JNK/AP-1 signaling and induce IL-1β. [Abstract]2026 Jun 12:e0042826. PMID: 42283627 -
J Immunol
2021 Jul 1;207(1):115-124. PMID: 34145059 -
Mol Biol Rep
Pharmacological inhibition of IRAK1/4 ameliorates high-fat diet-induced vascular dysfunction and cognitive impairment. [Abstract]2026 Feb 4;53(1):361. PMID: 41636883
Solvent & Solubility
DMF : 25 mg/mL (63.23 mM; ultrasonic and warming and heat to 60°C)
DMSO : 5 mg/mL (12.65 mM; ultrasonic and adjust pH to 3 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
DMSO : 3.33 mg/mL (8.42 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : < 1 mg/mL (insoluble)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
NCM460 cells, grown in 24-well plates, are incubated with 50 μM IRAK-1/4 inhibitor for 2 h. After 2 h, the media are changed, and new media with or without LPS (10 ng/mL) added. Treatment is terminated at 6 h, and spent media and cells are collected for IL-8 and other assays[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
References
[1]. Powers JP, et al. Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-4. Bioorg Med Chem Lett. 2006 Jun 1;16(11):2842-2845. [Content Brief]
[2]. Bhattacharyya S, et al. Bcl10 mediates LPS-induced activation of NF-kappaB and IL-8 in human intestinal epithelial cells. Am J Physiol Gastrointest Liver Physiol. 2007 Aug;293(2):G429-37. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO / DMSO / DMF | 1 mM | 2.5290 mL | 12.6451 mL | 25.2902 mL | 63.2255 mL |
| 5 mM | 0.5058 mL | 2.5290 mL | 5.0580 mL | 12.6451 mL | |
| DMSO / DMF | 10 mM | 0.2529 mL | 1.2645 mL | 2.5290 mL | 6.3226 mL |
| DMF | 15 mM | 0.1686 mL | 0.8430 mL | 1.6860 mL | 4.2150 mL |
| 20 mM | 0.1265 mL | 0.6323 mL | 1.2645 mL | 3.1613 mL | |
| 25 mM | 0.1012 mL | 0.5058 mL | 1.0116 mL | 2.5290 mL | |
| 30 mM | 0.0843 mL | 0.4215 mL | 0.8430 mL | 2.1075 mL | |
| 40 mM | 0.0632 mL | 0.3161 mL | 0.6323 mL | 1.5806 mL | |
| 50 mM | 0.0506 mL | 0.2529 mL | 0.5058 mL | 1.2645 mL | |
| 60 mM | 0.0422 mL | 0.2108 mL | 0.4215 mL | 1.0538 mL |
IRAK-1-4 Inhibitor I Related Classifications
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