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IRAK inhibitor 6

Catalog No.
A3504
IRAK-4 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$266.00
In stock
5mg
$226.00
In stock
10mg
$308.00
In stock
50mg
$801.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

IC50: 0.16 μM for IRAK-4

IRAK inhibitor 6 is an interleukin-1 receptor associated kinase 4 (IRAK-4) inhibitor.

The interleukin-1 receptor associated kinases (IRAKs) are a family of serine/threonine kinases related with regulating cellular signalling downstream of the IL-18, IL-1 and various Toll-like receptors. IRAK-4 is reported to be essential for the activation of the intracellular signalling cascades including NFКB and MAPK pathways, which are critical for the production of inflammatory cytokines.

In vitro: A quantitative structure–activity relationship (QSAR) study of IRAK inhibitor 6 and its analogs were conducted by using the genetic algorithm and multiple linear regression (GA-MLR) method [1]. In vitro study showed that compared with its unsubstituted phenyl amide analog, the ortho-substitution with chloro, methoxy and difluoromethoxy analogs of IRAK inhibitor 6 improved potency against IRAK-4 significantly. These potency effects were additive, with the most active example in the set being IRAK inhibitor 6, in which the presence of nitrogen-linked substituents at the para position had a beneficial effect on the rate of turnover by human microsomes (20 μL/min/mg protein) [2].

Clinical trial: N/A

References:
[1] Pourbasheer E, Riahi S, Ganjali MR, Norouzi P.  Quantitative structure-activity relationship (QSAR) study of interleukin-1 receptor associated kinase 4 (IRAK-4) inhibitor activity by the genetic algorithm and multiple linear regression (GA-MLR) method. J Enzyme Inhib Med Chem. 2010 Dec;25(6):844-53.
[2] Buckley GM, Gowers L, Higueruelo AP, Jenkins K, Mack SR, Morgan T, Parry DM, Pitt WR, Rausch O, Richard MD, Sabin V, Fraser JL.  IRAK-4 inhibitors. Part 1: a series of amides. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3211-4.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt396.46
Cas No.1042672-97-8
FormulaC20H20N4O3S
Solubility≥9.9 mg/mL in DMSO,insoluble in EtOH,insoluble in H2O
Chemical NameN-(2-methoxy-4-morpholin-4-ylphenyl)-2-pyridin-3-yl-1,3-thiazole-4-carboxamide
SDFDownload SDF
Canonical SMILESCOC1=C(C=CC(=C1)N2CCOCC2)NC(=O)C3=CSC(=N3)C4=CN=CC=C4
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.

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