Search Site
Home >> Signaling Pathways >> JAK/STAT Signaling >> JAK >> GLPG0634 analogue
Related Products
GLPG0634 analogueJAK1 inhibitor, potent and selective

GLPG0634 analogue

Catalog No. B6116
Size Price Stock Qty
5mg $228.00 In stock

Tel: +1-832-696-8203

Email: sales@apexbt.com

Worldwide Distributors

Sample solution is provided at 25 µL, 10mM.

Biological Activity

Description GLPG0634 is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.
Targets JAK1 JAK2 TYK2 JAK3    
IC50 10 nM 28 nM 116 nM 810 nM    

GLPG0634 analogue Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

GLPG0634 analogue Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 1206101-20-3 SDF Download SDF
Chemical Name (E)-N-(5-(4-((6-cyanopyridin-3-yl)methoxy)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2(3H)-ylidene)cyclopropanecarboxamide
Canonical SMILES N#CC1=NC=C(COC2=CC=C(C3=CC=CC4=N/C(NN34)=N\C(C5CC5)=O)C=C2)C=C1
Formula C23H18N6O2 M.Wt 410.43
Solubility Limited solubility Storage Desiccate at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

GLPG0634 is a potent and selective inhibitor of JAK1 with IC50 values of 10, 28, 810 and 116 nM for JAK1, JAK2, JAK3 and TYK2, respectively [1].

Janus kinase 1 (JAK1) is a member of the JAK family and is a non-receptor tyrosine kinase. JAKs play an important role in the immune system. JAK1 is a potential target for the treatment of immune-inflammatory diseases [1].

GLPG0634 is a potent and selective JAK1 inhibitor. GLPG0634 inhibited JAK1, JAK2, JAK3 and TYK2 with IC50 values of 10, 28, 810 and 116 nM, respectively. In CD4+ T cells, GLPG0634 significantly reduced IL-6-induced STAT1 phosphorylation with IC50 value of 629 nM, which suggested the inhibition of JAK1. In CD33+ T cells, GLPG0634 reduced GM-CSF-induced STAT5 phosphorylation with IC50 value of 17.5 µM, suggesting the inhibition of JAK2. GLPG0634 inhibited the differentiation of Th1 and Th2 cells mediated by IL-4 and IL-12, respectively. Also, GLPG0634 inhibited Th17 differentiation induced by TGF-β, IL-23, IL-6 and IL-1β [1].

In rats, GLPG0634 significantly reduced the mRNA levels of Mx2, which were modulated by IFN-α-JAK1/TYK2 signaling. In collagen-induced arthritis (CIA) rat model, GLPG0634 significantly reduced the infiltration of inflammatory cells and reduced the levels of IL-6, IP-10, XCL1 and MCP-1 [1].

Reference:
[1].  Van Rompaey L, Galien R, van der Aar EM, et al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. J Immunol, 2013, 191(7): 3568-3577.