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MedChemExpress - Model GLPG0259 - ...

MedChemExpress - Model GLPG0259 - 959754-85-9

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

MCE China：GLPG0259

Brand：MedChemExpress (MCE)

Cat. No.HY-136990

CAS：959754-85-9

Purity：99.84%

Storage：Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

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.

In Vitro：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].

In Vivo：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].

IC50 & Target：MAPK-activated protein kinase 5 (MK5)[1] In Vitro 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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> GLPG0259 Related Antibodies

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]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
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•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
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•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。