GLPG4970 

GLPG4970 is a potent, selective and orally active salt-inducible kinase 2/3 (SIK2/SIK3) dual inhibitor with IC₅₀ values of 0.3 nM and 0.7 nM. GLPG4970 has weak inhibition of hERG channel with an IC₅₀ of 29 μM. GLPG4970 can decrease TNFα release and increase IL-10 release GLPG4970 can be used for the researches of inflammation and immunology, such as colitis^[1].

GLPG4970 (Compound 8) shows inhibition effect to many off-target Kinases with IC₅₀ range from 4 nM to 292 nM^[1].
GLPG4970 induces nuclear translocation of CRTC3 in U2OS cells with an EC₅₀ of 16 nM in U2OS cells^[1].
GLPG4970 dose-dependently inhibits TNFα release in monocytes and macrophages stimulated with LPS (HY-D1056), with an IC₅₀ of 3.6 nM and 8.1 nM, respectively^[1].
GLPG4970 increases IL-10 release in monocytes and macrophages stimulated with LPS (HY-D1056) ^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GLPG4970 (Compound 8) (0.5-30 mg/kg, p.o., 15 mins before LPS) decreases TNFα release and increases IL-10 release in LPS (HY-D1056)-treated mice^[1].
GLPG4970 (3-30 mg/kg, p.o., twice a day) decreases disease progression in dextran sulfatesodium (DSS)-induced colitis mice models^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

524.58

C₂₉H₃₁F₃N₄O₂

O=C1N(CC(F)(F)F)CCC2=C1C(OC)=CC(C3=CC(C4=CC5=C(C=C4)CC(C)(C)N(C)C5)=CN=C3N)=C2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Kelgtermans H, et al. Structure-Activity Relationship Guided Scaffold Hopping Resulted in the Identification of GLPG4970, a Highly Potent Dual SIK2/SIK3 Inhibitor. J Med Chem. 2025 Aug 14;68(15):16551-16577.  [Content Brief]