1. IRAK
  2. IRAK-1-4 Inhibitor I

IRAK-1-4 Inhibitor I (Synonyms: IRAK-1/4 Inhibitor I)

Cat. No.: HY-13329 Purity: 99.88%
Handling Instructions

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.

IRAK-1-4 Inhibitor I Chemical Structure

IRAK-1-4 Inhibitor I Chemical Structure

CAS No. : 509093-47-4

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Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    IRAK-1-4 Inhibitor I purchased from MCE. Usage Cited in: Antibiotics (Basel). 2020 Jan 17;9(1). pii: E33.

    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.

    IRAK-1-4 Inhibitor I purchased from MCE. Usage Cited in: Oncogene. 2020 Jul 30.

    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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    Description

    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.

    IC50 & Target

    IC50: 0.2 μM (IRAK-4), 0.3 μM (IRAK-1)[1]

    In Vitro

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    395.41

    Formula

    C₂₀H₂₁N₅O₄

    CAS No.

    509093-47-4

    SMILES

    O=C(C1=CC=CC([N+]([O-])=O)=C1)NC2=NC3=CC=CC=C3N2CCN4CCOCC4

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMF : 25 mg/mL (63.23 mM; ultrasonic and warming and heat to 60°C)

    DMSO : 5 mg/mL (12.65 mM; Need ultrasonic)

    Ethanol : < 1 mg/mL (insoluble)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5290 mL 12.6451 mL 25.2902 mL
    5 mM 0.5058 mL 2.5290 mL 5.0580 mL
    10 mM 0.2529 mL 1.2645 mL 2.5290 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Cell Assay
    [2]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.88%

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    Keywords:

    IRAK-1-4 Inhibitor IIRAK-1/4 Inhibitor IIRAKInterleukin-1 receptor associated kinaseIL-1R associated kinaseInhibitorinhibitorinhibit

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    Product Name:
    IRAK-1-4 Inhibitor I
    Cat. No.:
    HY-13329
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