GSK-626616 是一种口服具有活力的DYRK3抑制剂 (IC50:0.7 nM)。它以相似的效力抑制 DYRK 家族的其他成员，可用于研究贫血。

GSK-626616 is a potent and orally bioavailable DYRK3 inhibitor (IC50: 0.7 nM). It inhibits other members of the DYRK family with similar potency. GSK-626616 is a potential therapy for the treatment of anemia.

GSK-626616 (serum-deprived HeLa cells) reduces EGF-induced phosphorylation of PRAS40 at Thr246. GSK-626616 enhances the binding of PRAS40 to mTORC1[2]. 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].

1025821-33-3

C18H10Cl2N4OS

401.27

DMSO:49 mg/mL (122.11 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years