IRAK-1-4 Inhibitor I is an inhibitor of interleukin-1 receptor-associated kinase 1/4 (IRAK1/4) withIC₅₀s of 0.2 μM and 0.3 μM, respectively.

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

IRAK-1-4 Inhibitor I has IC₅₀greater 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 pp60^SRC. 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].

395.41

Solid

C₂₀H₂₁N₅O₄

509093-47-4

Room temperature in continental US; may vary elsewhere.

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

DMSO : 5 mg/mL(12.65 mM;ultrasonic and adjust pH to 3 with HCl)

H₂O :< 0.1 mg/mL(insoluble)

Ethanol :< 1 mg/mL(insoluble)

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