JavaScript seems to be disabled in your browser. For the best experience on our site, be sure to turn on Javascript in your browser.
Tel: +1-832-696-8203
Email: [email protected]
Worldwide Distributors
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
Cell lines
HeLa cells
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.
Reaction Conditions
72 hrs
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).
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.