GLPG3312

GLPG3312 (Compound 28) is an orally active SIK inhibitor with IC50 values of 2.0 nM, 0.7 nM and 0.6 nM for SIK1, SIK2 and SIK3, respectively. GLPG3312 exhibits anti-inflammatory and immunomodulatory activity in vitro on human primary myeloid cells and in vivo in mouse models. GLPG3312 has good oral bioavailability and can be used for research on inflammatory and immune diseases[1].

Product Specifications

CAS Number

[2340388-72-7]

UNSPSC

12352005

Target

Bcr-Abl; Discoidin Domain Receptor; LIM Kinase (LIMK) ; MAP3K; RIP kinase; Salt-inducible Kinase (SIK) ; Src; TGF-β Receptor

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Immunology/Inflammation; MAPK/ERK Pathway; Protein Tyrosine Kinase/RTK; TGF-beta/Smad

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/glpg3312.html

Purity

98.63

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(NC1CC1)C2=C(OC)C=C(N3C=NC4=CC(C5=CN(C)N=C5)=CC=C34)C=C2OC(F)F

Molecular Formula

C23H21F2N5O3

Molecular Weight

453.44

References & Citations

[1]Temal-Laib T, et al. Optimization of Selectivity and Pharmacokinetic Properties of Salt-Inducible Kinase Inhibitors that Led to the Discovery of Pan-SIK Inhibitor GLPG3312. J Med Chem. 2024 Jan 11;67 (1) :380-401.