An IRAK4 inhibitor
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GLPG2534

Item No. 42048

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[6-[2-(2-hydroxyethoxy)ethoxy]-5-[(tetrahydro-2H-pyran-4-yl)amino]-3H-imidazo[4,5-b]pyridin-3-yl]-3-pyridinecarbonitrile
CAS Number
2095615-97-5
Molecular Formula
C21H24N6O4
Formula Weight
424.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly Soluble: 1-10 mg/mlEthanol: Slightly Soluble: 0.1-1 mg/ml
SMILES
N#CC1=CN=C(N2C=NC3=C2N=C(NC4CCOCC4)C(OCCOCCO)=C3)C=C1
InChi Code
InChI=1S/C21H24N6O4/c22-12-15-1-2-19(23-13-15)27-14-24-17-11-18(31-10-9-30-8-5-28)20(26-21(17)27)25-16-3-6-29-7-4-16/h1-2,11,13-14,16,28H,3-10H2,(H,25,26)
InChi Key
VNAPWQDUDZCVCA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $72

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    5 mg

    $323

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    10 mg

    $572

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    25 mg

    $1,073

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    Product Description

    GLPG2534 is an inhibitor of IL-1 receptor-associated kinase 4 (IRAK4; IC50s = 6.4 and 3.5 nM for the human and mouse enzymes, respectively).1 It is selective for IRAK4 over IRAK1 (IC50 = 179 nM) and a panel of 151 additional kinases at 1 µM but does inhibit FMS-related tyrosine kinase 3 (FLT3), tropomyosin-related kinase B (TrkB), and VEGFR3 (IC50s = 2.2, 5.8, and 57 nM, respectively). GLPG2534 inhibits TNF-α release induced by CL097 (Item No. 39513) in isolated human peripheral blood mononuclear cells (PBMCs) and human whole blood (IC50s = 122.8 and 568 nM, respectively). In vivo, GLPG2534 (30 mg/kg, p.o.) reduces ear thickness in mouse models of psoriasis induced by recombinant mouse IL-23 or imiquimod (Item No. 14956) and mouse models of atopic dermatitis induced by recombinant mouse IL-33 or MC903.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lavazais, S., Jargosch, M., Dupont, S., et al. IRAK4 inhibition dampens pathogenic processes driving inflammatory skin diseases. Sci. Transl. Med. 15(683), 683 (2023).