DC Chemicals Limited
China
Product Name: IRAK inhibitor 1
Price: $600.0/100mg $1100.0/250mg $2200.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

1042224-63-4

1042224-63-4 structure

Name: IRAK inhibitor 1
Chemical Name: 6-imidazo[1,2-a]pyridin-3-yl-N-piperidin-4-ylpyridin-2-amine
CAS Number: 1042224-63-4
Molecular Formula: C₁₇H₁₉N₅
Molecular Weight: 293.36600
Catalog: Signaling Pathways Immunology/Inflammation IRAK
Create Date: 2017-01-04 14:49:52
Modify Date: 2024-01-02 12:08:12
IRAK inhibitor 1 is a potent IRAK-4 inhibitor with IC50 of 216 nM, is poorly active against JNK-1 and JNK-2 with IC50 of 3.801 μM, and >10 μM, respectively.

Name	6-imidazo[1,2-a]pyridin-3-yl-N-piperidin-4-ylpyridin-2-amine
Synonyms	CS-0603 IRAK inhibitor 1

Description	IRAK inhibitor 1 is a potent IRAK-4 inhibitor with IC50 of 216 nM, is poorly active against JNK-1 and JNK-2 with IC50 of 3.801 μM, and >10 μM, respectively.
Related Catalog	Signaling Pathways >> Immunology/Inflammation >> IRAK Signaling Pathways >> Protein Tyrosine Kinase/RTK >> IRAK Research Areas >> Inflammation/Immunology
Target	IC50: 216 nM (IRAK-4), 3.801 μM (JNK-1), >10 μM (JNK-2)[1]
In Vitro	IRAK inhibitor 1 possesses significant potency in an IRAK-4 enzyme assay but is poorly active against JNK-1 and JNK-2[1]. IRAK-4 is a novel member of the IRAK family with unique functional properties. IRAK-4 is the closest human homolog to Pelle. Endogenous IRAK-4 interacts with IRAK-1 and TRAF6 in an IL-1-dependent manner, and overexpression of IRAK-4 can activate NF-κB as well as mitogen-activated protein (MAP) kinase pathways. Most strikingly, and in contrast to the other IRAKs, IRAK-4 depends on its kinase activity to activate NF-κB. In addition, IRAK-4 is able to phosphorylate IRAK-1, and overexpression of dominant-negative IRAK-4 is blocking the IL-1-induced activation and modification of IRAK-1, suggesting a role of IRAK-4 as a central element in the early signal transduction of Toll/IL-1 receptors, upstream of IRAK-1. IRAK-4 shares the domain structure of the other IRAKs and it is able to activate similar signal transduction pathways, namely NF-κB and MAPK pathways. It rapidly and transiently associates with IRAK-1 and TRAF6 in an IL-1-dependent manner but it is not functionally redundant with IRAK-1. IRAK-4 is an active protein kinase and requires its kinase activity to activate NF-κB. IRAK-4 might act upstream of IRAK-1 as an IRAK-1 activator[2].
References	[1]. Buckley GM, et al. IRAK-4 inhibitors. Part II: A structure-based assessment of imidazo[1,2-a]pyridine binding. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3291-5. [2]. Li S, et al. IRAK-4: a novel member of the IRAK family with the properties of an IRAK-kinase. Proc Natl Acad Sci U S A. 2002 Apr 16;99(8):5567-72.

Molecular Formula	C₁₇H₁₉N₅
Molecular Weight	293.36600
Exact Mass	293.16400
PSA	54.25000
LogP	2.96200
Storage condition	2-8℃

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