| Identification | Back Directory | [Name]
GSK-626616 | [CAS]
1025821-33-3 | [Synonyms]
GSK-626616
(5Z)-2-[(2,6-Dichlorophenyl)amino]-5-(6-quinoxalinylmethylene)-4(5H)-thiazolone
4(5H)-Thiazolone, 2-[(2,6-dichlorophenyl)amino]-5-(6-quinoxalinylmethylene)-, (5Z)- | [Molecular Formula]
C18H10Cl2N4OS | [MDL Number]
MFCD31689261 | [MOL File]
1025821-33-3.mol | [Molecular Weight]
401.27 |
| Chemical Properties | Back Directory | [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) | [form ]
Solid | [pka]
-0.94±0.20(Predicted) | [color ]
Pale Yellow to Light Yellow |
| Hazard Information | Back Directory | [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 availableATP-competitivepotent 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 culturesand exhibits therapeutic efficacy in a murine anemia model in vivo (0.03 mg/kg/d i.p.) | [IC 50]
DYRK1; DYRK2; DYRK3 | [storage]
Store at +4°C |
|
|