GSK-626616 Chemical Properties

Melting point:

281 - 282oC

Boiling point:

574.8±60.0 °C(Predicted)

Density 

1.55±0.1 g/cm3(Predicted)

storage temp. 

Refrigerator, under inert atmosphere

solubility 

Chloroform (Slightly, Heated), Methanol (Slightly)

pka

-0.94±0.20(Predicted)

form 

Solid

color 

Pale Yellow to Light Yellow

GSK-626616 Usage And Synthesis

Uses

GSK-626616 is a potent and selective DYRK inhibitor (IC50 = 0.7 nM for DYRK3, similar potency for DYRK1 and 2). Exhibits ~20-fold selectivity over casein kinase 2 and negligible activity against a panel of 451 kinases screened. Enhances number of CFU-E stimulated by Epo from human marrow. Increases hemoglobin levels in anemic mice. Orally bioavailable.

Biological Activity

GSK626616 is an orally available, ATP-competitive, potent and selective dual-specificity tyrosine phosphorylation-regulated kinase DYRK inhibitor (DYRK3 IC50 = 0.7 nM; similar potency against DYRK1A and DYRK2) with 20-fold selectivity over the closed related casein kinase 2. GSK626616 enhances Epo-stimulated increase of human marrow erythroid colony formation units (CFU-E), without affecting megakaryocyte colony growth or CFU-GM formation. GSK626616 enhances the percentage and number of Ter119+/CD71+ erythroid progenitors derived from kit+ mouse marrow in the presence of SCF and Epo in cultures, and exhibits therapeutic efficacy in a murine anemia model in vivo (0.03 mg/kg/d i.p.)

storage

Store at +4°C

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