GSK 626616

Pricing Availability   Qty
Cat.No. 6638 - GSK 626616 | C18H10Cl2N4OS | CAS No. 1025821-33-3
Description: Potent and selective DYRK inhibitor; orally bioavailable.
Chemical Name: (5Z)-2-[(2,6-Dichlorophenyl)amino]-5-(6-quinoxalinylmethylene)-4(5H)-thiazolone
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

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

M. Wt 401.27
Formula C18H10Cl2N4OS
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1025821-33-3
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 401.27. Batch specific molecular weights may vary from batch to batch due to solvent 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 0.5 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 0.5 mL

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References

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

Erickson-Miller et al (2007) GSK626616: A DYRK3 inhibitor as a potential new therapy for the treatment of anemia. Blood 110 510

Wippich et al (2013) Dual specificity kinase DYRK3 couples stress granule condensation/dissolution to mTORC1 signaling. Cell 152 791 PMID: 23415227

Rai et al (2018) Kinase-controlled phase transition of membraneless organelles in mitosis. Nature 559 211 PMID: 29973724


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Citations for GSK 626616

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