GLPG2534

GLPG2534 is an orally active and selective IRAK4 inhibitor, with IC50 values of 6.4 nM and 3.5 nM for human and mouse IRAK4. GLPG2534 can be used for the research of inflammatory skin diseases.

GLPG2534 (2 h) inhibits IRAK4 with IC₅₀ values of 6.4 nM and 3.5 nM for human and mouse IRAK4^[1].
GLPG2534 inhibits IL-1β–driven IL-6 release, with an IC₅₀ of 55 nM^[1].
GLPG2534 inhibits TNF-α–driven IL-6 release with an IC₅₀ of 6.6 μM^[1].
GLPG2534 (0.1-10 μM, 16 h) inhibits expression of S100A7, DEFB4A, CXCL8, TNF in Flagellin-stimulated keratinocytes^[1].

GLPG2534 (0.3-10 mg/kg, p.o.) Inhibits CL097-driven release of TNF-α in blood of mice^[1].
GLPG2534 (10 and 30 mg/kg, p.o., b.i.d. 5 days) attenuates inflammation in psoriasis-like mouse models^[1].
GLPG2534 (3-30 mg/kg, p.o., b.i.d. 5 days) attenuates the development of IL-33- and MC903-induced AD-like skin inflammation in mice^[1].

References:
[1]. Lavazais S, et al. IRAK4 inhibition dampens pathogenic processes driving inflammatory skin diseases. Sci Transl Med. 2023 Feb 15;15(683):eabj3289.