| Bioactivity | GSK-626616 is a potent, orally bioavailable inhibitor of DYRK3 (IC50=0.7 nM). GSK-626616 inhibits other members of the DYRK family (e.g., DYRK1A and DYRK2) with similar potency, which is a potential therapy for the treatment of anemia[1]. | ||||||||||||
| Target | IC50: 0.7 nM (DYRK3) | ||||||||||||
| Invitro | GSK-626616 abolishes the phosphorylation of S6K1 at Thr389 in nonstimulated HeLa cells. GSK-626616 reduces the phosphorylation of S6K1 at Thr389 in EGF- and insulin-stimulated HeLa cells, showing that mTORC1 activity is impaired[2].GSK-626616 (serum-deprived HeLa cells) reduces EGF-induced phosphorylation of PRAS40 at Thr246. Binding of PRAS40 to mTORC1 is enhanced by GSK-626616[2]. | ||||||||||||
| Name | GSK-626616 | ||||||||||||
| CAS | 1025821-33-3 | ||||||||||||
| Formula | C18H10Cl2N4OS | ||||||||||||
| Molar Mass | 401.27 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Connie L. Erickson-Miller, et al. GSK626616: A DYRK3 Inhibitor as a Potential New Therapy for the Treatment of Anemia. Blood 2007 110:510; [2]. Wippich F, et al. Dual specificity kinase DYRK3 couples stress granule condensation/dissolution to mTORC1 signaling. Cell. 2013;152(4):791-805. |
GSK-626616
CAS: 1025821-33-3 F: C18H10Cl2N4OS W: 401.27
GSK-626616 is a potent, orally bioavailable inhibitor of DYRK3 (IC50=0.7 nM). GSK-626616 inhibits other members of the D
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