Toggle Nav

IRAK-1-4 Inhibitor I

In stock
Catalog No.
A3505
IRAK-1/4 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$100.00
In stock
10mg
$123.00
In stock
20mg
$236.00
In stock
50mg
$544.00
In stock
100mg
$914.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt395.41
Cas No.509093-47-4
FormulaC20H21N5O4
SynonymsIRAK-1/4 Inhibitor I
Solubility≥19.75 mg/mL in DMSO, <2.57 mg/mL in EtOH, <2.19 mg/mL in H2O
Chemical NameN-[1-(2-morpholin-4-ylethyl)benzimidazol-2-yl]-3-nitrobenzamide
SDFDownload SDF
Canonical SMILESC1COCCN1CCN2C3=CC=CC=C3N=C2NC(=O)C4=CC(=CC=C4)[N+](=O)[O-]
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment [1]:

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.

Biological Activity

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

Chemical structure

IRAK-1-4 Inhibitor I

Related Biological Data

IRAK-1-4 Inhibitor I

Related Biological Data

IRAK-1-4 Inhibitor I

Related Biological Data

IRAK-1-4 Inhibitor I