GLPG3970 | SIK2/3 inhibitor

CAS:
 2403733-82-2
Catalog Number:
 10-4446
GLPG3970 chemical structure

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GLPG3970 (2403733-82-2) is a potent and selective (against a panel of 372 kinases) SIK2/3 inhibitor (IC50s: SIK2 = 7.8 nM, SIK3 = 3.8 nM).1 It reduced THFα and increased IL-10 levels in an LPS challenge model in mice and displayed efficacy in a mouse model of colitis. GLPG3970 promoted reprogramming of human myeloid cells toward an anti-inflammatory phenotype, reprogrammed monocyte-dendritic differentiation toward stable tolerogenic phenotypes, and suppressed T-cell activation.2 It also displayed efficacy in mouse models of psoriasis and arthritis.

References/Citations:

  1. Peixoto et al. (2024), Discovery of Clinical Candidate GLPG3970: A Potent and Selective Dual SIK2/SIK3 Inhibitor for the Treatment of Autoimmune and Inflammatory Diseases; J. Med. Chem. 67 5233
  2. De Vos et al. (2026), Selective SIK2/SIK3 inhibition reprograms pro- and anti-inflammatory pathways in myeloid cells, improving autoimmune disease outcomes; JCI Insight 11 e171776
2403733-82-2, GLPG3970, GLPG3970 supplier, SIK2 inhibitor, SIK2/3 inhibitor, SIK2/SIK3 inhibitor, SIK3 inhibitor
CAS:
2403733-82-2
Catalog Number:
10-4446
Activity:
SIK2/3 inhibitor
Chemical Names:
8-Methoxy-6-[7-(2-morpholin-4-ylethoxy)imidazo[1,2-a]pyridin-3-yl]-2-(2,2,2-trifluoroethyl)-3,4-dihydroisoquinolin-1-one
Molecular Weight:
504.51
Molecular Formula:

C25H27F3N4O4

Solubility:
Soluble in DMSO (>50 mg/ml)
Physical Properties:
Off-white solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

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GLPG3970 (2403733-82-2) is a potent and selective (against a panel of 372 kinases) SIK2/3 inhibitor (IC50s: SIK2 = 7.8 nM, SIK3 = 3.8 nM).1 It reduced THFα and increased IL-10 levels in an LPS challenge model in mice and displayed efficacy in a mouse model of colitis. GLPG3970 promoted reprogramming of human myeloid cells toward an anti-inflammatory phenotype, reprogrammed monocyte-dendritic differentiation toward stable tolerogenic phenotypes, and suppressed T-cell activation.2 It also displayed efficacy in mouse models of psoriasis and arthritis.

References/Citations:

  1. Peixoto et al. (2024), Discovery of Clinical Candidate GLPG3970: A Potent and Selective Dual SIK2/SIK3 Inhibitor for the Treatment of Autoimmune and Inflammatory Diseases; J. Med. Chem. 67 5233
  2. De Vos et al. (2026), Selective SIK2/SIK3 inhibition reprograms pro- and anti-inflammatory pathways in myeloid cells, improving autoimmune disease outcomes; JCI Insight 11 e171776

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