959754-85-9
959754-85-9
Chemical Structure
GLPG0259
- CAS No.: 959754-85-9
- Formula:C24H28N8O2
- Molecular Weight:460.53
IUPAC Name: 4-(8-((4-(4-(tert-butyl)piperazin-1-yl)phenyl)amino)-[1,2,4]triazolo[1,5-a]pyrazin-5-yl)furan-2-carboxamide
InChIKey: DLGZLIXYVSQGOX-UHFFFAOYSA-N
SMILES: O=C(C1=CC(C2=CN=C(NC3=CC=C(N4CCN(C(C)(C)C)CC4)C=C3)C5=NC=NN52)=CO1)N
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
GLPG0259 | 99.63% | 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. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
Structural Analogs
-
Similarity Score 0.76
HY-W782935MAPKAPK5-IN-1 -
Similarity Score 0.51
HY-109091Lanraplenib -
Similarity Score 0.49
HY-120590Ruserontinib -
Similarity Score 0.49
HY-161917HPK1-IN-49 -
Similarity Score 0.49
HY-10424RMilciclib (Standard) -
Similarity Score 0.48
HY-151961RSH-7 -
Similarity Score 0.48
HY-109091ALanraplenib monosuccinate -
Similarity Score 0.48
HY-109091BLanraplenib succinate -
Similarity Score 0.48
HY-151279ALK5-IN-30 -
Explore the MedChemAI to find more analogs
References
- [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. [Content Brief]
- [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. [Content Brief]
