Chemical Name: (5Z)-2-[(2,6-Dichlorophenyl)amino]-5-(6-quinoxalinylmethylene)-4(5H)-thiazolone
Biological ActivityGSK 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.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
GSK626616: A DYRK3 inhibitor as a potential new therapy for the treatment of anemia.
Erickson-Miller et al.
Dual specificity kinase DYRK3 couples stress granule condensation/dissolution to mTORC1 signaling.
Wippich et al.
Kinase-controlled phase transition of membraneless organelles in mitosis.
Rai et al.
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