1. Immunology/Inflammation
    Protein Tyrosine Kinase/RTK
  2. IRAK

IRAK inhibitor 1 

Cat. No.: HY-13275 Purity: 99.47%
Handling Instructions

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.

For research use only. We do not sell to patients.
IRAK inhibitor 1 Chemical Structure

IRAK inhibitor 1 Chemical Structure

CAS No. : 1042224-63-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 319 In-stock
5 mg USD 290 In-stock
10 mg USD 396 In-stock
50 mg USD 1030 In-stock
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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.

IC50 & 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
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 3.4087 mL 17.0433 mL 34.0866 mL
5 mM 0.6817 mL 3.4087 mL 6.8173 mL
10 mM 0.3409 mL 1.7043 mL 3.4087 mL
Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

293.37

Formula

C₁₇H₁₉N₅

CAS No.

1042224-63-4

SMILES

C1(C2=CN=C3N2C=CC=C3)=CC=CC(NC4CCNCC4)=N1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 12.2 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.47%

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Product Name:
IRAK inhibitor 1
Cat. No.:
HY-13275
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