IRAK inhibitor 1
IC50: 35 nM for IRAK-4
The interleukin-1 receptor associated kinase (IRAK) family is comprised of four family members IRAK-1, IRAK-2, IRAK-3/M, and IRAK-4. Upon activation of their upstream cognate receptors, IRAK-4 is thought to phosphorylate IRAK-1 resulting in the activation and autophosphorylation of IRAK-1 an subsequent phosphorylation of downstream substrates. IRAK inhibitor 1 is an inhibitor of interleukin-1 receptor associated kinase 4 (IRAK-4).
In vitro: The regioisomeric pyridines IRAK inhibitor 1 (6) and it analogue (7) showed contrasting SAR, with the 2,6-pyridine isomer IRAK inhibitor 1 having low-nanomolar potency whilst the 2,4-pyridine isomer 7 showed little activity, despite having a more accessible bidentate-binding motif. At 10 μM, IRAK inhibitor 1 was found to have 39% inhibition for JNK-1 and 15% inhibition for JNK-2, respectivley [1].
In vivo: No animal in-vivo data available currently IRAK inhibitor 1 and its analogues.
Clinical trial: IRAK inhibitor 1 is currently in the preclinical development stage and no clinical data are available.
Reference:
[1] Buckley GM, Ceska TA, Fraser JL, Gowers L, Groom CR, Higueruelo AP, Jenkins K, Mack SR, Morgan T, Parry DM, Pitt WR, Rausch O, Richard MD, Sabin V. IRAK-4 inhibitors. Part II: a structure-based assessment of imidazo[1,2-a]pyridine binding. Bioorg Med Chem Lett. 2008;18(11):3291-5.
- 1. Upadhyay K, Park JE, et al. "Group B Streptococci Induce Proinflammatory Responses via a Protein Kinase D1-Dependent Pathway." J Immunol. 2017 Jun 1;198(11):4448-4457. PMID:28461572
- 2. Marinho FV, Fahel JS, et al. "Lack of IL-1 Receptor-Associated Kinase-4 Leads to Defective Th1 Cell Responses and Renders Mice Susceptible to Mycobacterial Infection." J Immunol. 2016 Sep 1;197(5):1852-63. PMID:27439514
Storage | Store at -20°C |
M.Wt | 293.37 |
Cas No. | 1042224-63-4 |
Formula | C17H19N5 |
Solubility | insoluble in EtOH; insoluble in H2O; ≥14.4 mg/mL in DMSO |
Chemical Name | 6-imidazo[1,2-a]pyridin-3-yl-N-piperidin-4-ylpyridin-2-amine |
SDF | Download SDF |
Canonical SMILES | C1CNCCC1NC2=CC=CC(=N2)C3=CN=C4N3C=CC=C4 |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Description | IRAK inhibitor 1 is an inhibitor of interleukin-1 receptor associated kinase 4 (IRAK-4). | |||||
Targets | IRAK-4 | |||||
IC50 |
Quality Control & MSDS
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Chemical structure

Related Biological Data

Related Biological Data
