GSK 626616

Name: GSK 626616
Brand: Tocris Bioscience
SKU: 6638

Tocris Bioscience, part of Bio-Techne | Catalog # 6638

Citations (4)

COA / SDS

Potent and selective DYRK inhibitor; orally bioavailable.

Key Product Details

Description:	Potent and selective DYRK inhibitor; orally bioavailable.
Chemical Name:	(5Z)-2-[(2,6-Dichlorophenyl)amino]-5-(6-quinoxalinylmethylene)-4(5H)-thiazolone
Purity:	≥95% (HPLC)
Molecular Weight:	401.27

View Full Technical Details for GSK 626616

Technical Data
Citations

Biological Activity for GSK 626616

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.

Technical Data for GSK 626616

M. Wt	401.27
Formula	C₁₈H₁₀Cl₂N₄OS
Storage	Store at +4°C
Purity	≥95% (HPLC)
CAS Number	1025821-33-3
PubChem ID	135416229
InChi Key	RJPNRXFBYZVRIB-DHDCSXOGSA-N
Smiles	O=C(N=C(NC1=C(Cl)C=CC=C1Cl)S/2)C2=C\C3=CC=C(N=CC=N4)C4=C3

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.

Solubility for GSK 626616

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	40.13	100

Preparing Stock Solutions for GSK 626616

The following data is based on the product molecular weight 401.27.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.49 mL	12.46 mL	24.92 mL
5 mM	0.50 mL	2.49 mL	4.98 mL
10 mM	0.25 mL	1.25 mL	2.49 mL
50 mM	0.05 mL	0.25 mL	0.50 mL

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References for GSK 626616

References are publications that support the biological activity of the product.

Wippich Dual specificity kinase DYRK3 couples stress granule condensation/dissolution to mTORC1 signaling. Cell 2013 PMID: 23415227
Rai Kinase-controlled phase transition of membraneless organelles in mitosis. Nature 2018 PMID: 29973724
Erickson-Miller GSK626616: A DYRK3 inhibitor as a potential new therapy for the treatment of anemia. Blood