| Description | GLPG2534 is an orally active, selective and potent IRAK4 inhibitor with anti-inflammatory activity. GLPG2534 inhibits human and mouse IRAK4 and could be used to study psoriasis and atopic dermatitis. |
| In vitro | GLPG2534 inhibits IL-6 release driven by IL-1β with an IC50 of 55 nM[1]. It also inhibits TNF-α-driven IL-6 release, with an IC50 of 6.6 μM[1]. When applied at concentrations ranging from 0.1 to 10 μM for 16 hours, GLPG2534 inhibits the expression of S100A7, DEFB4A, CXCL8, and TNF in ciliated epithelial cells stimulated with ciliogenesis-promoting factors[1]. |
| In vivo | GLPG2534, administered orally at doses ranging from 0.3 to 10 mg/kg, inhibits CL097-driven TNF-α release in mouse blood[1]. Furthermore, oral administration of GLPG2534 at doses of 10 and 30 mg/kg, twice daily, alleviates inflammation in a psoriasis-like mouse model[1]. Additionally, GLPG2534, at doses of 3-30 mg/kg, orally administered twice daily for 5 days, mitigates the development of IL-33 and MC903-induced atopic dermatitis-like skin inflammation in mice[1]. |
| Target activity | IL-1β:55 nM, IRAK1:179 nM, mIRAK4:3.5 nM, hIRAK4:6.4 nM |
| Synonyms | GLPG-2534 |
| molecular weight | 424.45 |
| Molecular formula | C21H24N6O4 |
| CAS | 2095615-97-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 80 mg/mL (188.48 mM), Sonication is recommended. |
| References | 1. Lavazais S, et al. IRAK4 inhibition dampens pathogenic processes driving inflammatory skin diseases. Sci Transl Med. 2023 Feb 15;15(683):eabj3289. |