For research use only. Not for therapeutic Use.
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].
GLPG0259 reduces inflammation and release of bone degrading mediators, but did not affect phosphorylation of c-jun NH(2) -terminal protein kinase (JNK), ERK, and p38 MAP kinase[1].
GLPG0259 (1-5 μM; 48 h) leads to the reduction and remodeling of actin filamentation in prostate cancer (PCa) cell lines, LNCaP and PC3[2].
GLPG0259 (2 mg/kg, 10 mg/kg; i.p.; twice weekly for 7 weeks) impairs tumor cells lung metastasis in SCID beige mice bearing prostate cancer (PCa) cell lines P3 cells (i.v.)[1].
| Catalog Number | I028088 |
| CAS Number | 959754-85-9 |
| Synonyms | 4-[8-[4-(4-tert-butylpiperazin-1-yl)anilino]-[1,2,4]triazolo[1,5-a]pyrazin-5-yl]furan-2-carboxamide |
| Molecular Formula | C24H28N8O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H28N8O2/c1-24(2,3)31-10-8-30(9-11-31)18-6-4-17(5-7-18)29-22-23-27-15-28-32(23)19(13-26-22)16-12-20(21(25)33)34-14-16/h4-7,12-15H,8-11H2,1-3H3,(H2,25,33)(H,26,29) |
| InChIKey | DLGZLIXYVSQGOX-UHFFFAOYSA-N |
| SMILES | CC(C)(C)N1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C(N4C3=NC=N4)C5=COC(=C5)C(=O)N |
| Reference | [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. |
