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GLPG-0259

Names

[ CAS No. ]:
959754-85-9

[ Name ]:
GLPG-0259

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Others >> Others

[Target]

MAPK-activated protein kinase 5 (MK5)[1]


[In Vitro]

GLPG0259 能够减少炎症和骨降解介质的释放，但不影响 c-jun NH(2)-末端蛋白激酶 (JNK)、ERK 和 p38 MAP 激酶的磷酸化[1]。 GLPG0259 (1-5 μM; 48 h) 导致前列腺癌 (PCa) 细胞株 LNCaP 和 PC3 中，肌动蛋白丝状减少和重塑[2]。

[In Vivo]

GLPG0259 (2 mg/kg, 10 mg/kg;腹腔注射; 每周 2 次, 共 7 周) 在携带有前列腺癌细胞系 P3 细胞 (i.v.) 的 SCID 米色小鼠中，抑制肿瘤细胞在肺转移[2].

[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.  

[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.  

Chemical & Physical Properties

[ Molecular Formula ]:
C24H28N8O2

[ Molecular Weight ]:
460.53200

[ Exact Mass ]:
460.23400

[ PSA ]:
117.82000

[ LogP ]:
3.92350

Related Compounds