GLPG0259

GLPG0259 is a ATP-competitive inhibitor of MAPK-activated protein kinase 5 (MK5) with oral activity. GLPG0259 reduces inflammation and bone destruction in a mouse model of collagen-induced arthritis. GLPG0259 also inhibited the metastasis of prostate cancer (PCa) cells[1][2].

Product Specifications

CAS Number

[959754-85-9]

UNSPSC

12352005

Target

Others

Type

Reference compound

Related Pathways

Others

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/glpg0259.html

Purity

99.84

Solubility

DMSO : 3.33 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(C1=CC(C2=CN=C(NC3=CC=C(N4CCN(C(C)(C)C)CC4)C=C3)C5=NC=NN52)=CO1)N

Molecular Formula

C24H28N8O2

Molecular Weight

460.53

References & Citations

[1]Westhovens R, et al. Oral administration of GLPG0259, an inhibitor of MAPKAPK5, a new target for the treatment of rheumatoid arthritis: a phase II, randomised, double-blind, placebo-controlled, multicentre trial. Ann Rheum Dis. 2013 May;72 (5) :741-4. |[2]Khalil MI, et al. The TLK1-MK5 Axis Regulates Motility, Invasion, and Metastasis of Prostate Cancer Cells. Cancers (Basel) . 2022 Nov 22;14 (23) :5728.