GSK-626616 is a dual-specificity tyroxie-regulated kinase (DYRK3) inhibitor with an IC50 of 0.7 nM, which is a potential drug for the treatment of anemia.

 

Brand: BCM

 

Target: DYRK

 

Signaling Pathways: Cell Cycle/Checkpoint; Tyrosine Kinase/Adaptors

 

In Vitro: GSK-626616 (serum-deprived HeLa cells) reduces EGF-induced phosphorylation of PRAS40 at Thr246. GSK-626616 enhances the binding of PRAS40 to mTORC1. 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.

 

Melting Point: 281 ~ 282°C

 

Boiling Point: 574.8±60.0 °C(Predicted)

 

pKa: -0.94±0.20(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; Insoluble in Ethanol.

 

GHS: GHS07

 

Isomeric SMILES: C1=CC(=C(C(=C1)Cl)N=C2NC(=O)/C(=C/C3=CC4=NC=CN=C4C=C3)/S2)Cl  

 

InChIKey: RJPNRXFBYZVRIB-DHDCSXOGSA-N  

 

InChI: InChI=1S/C18H10Cl2N4OS/c19-11-2-1-3-12(20)16(11)23-18-24-17(25)15(26-18)9-10-4-5-13-14(8-10)22-7-6-21-13/h1-9H,(H,23,24,25)/b15-9-

 

Attribute
[Chem Name]	(5Z)-2-(2,6-dichlorophenyl)imino-5-(quinoxalin-6-ylmethylidene)-1,3-thiazolidin-4-one
[Synonym]	GSK626616
[CAS No.]	1025821-33-3
[MDL No.]	MFCD31689261
[Formula]	C18H10Cl2N4OS
[Molecular]	401.27
[Form]	Light yellow solid
[Storage]	Stored at -20°C

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