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Submit ReviewGSK 626616
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)
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 Data for GSK 626616
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 | 0.5 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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Product Datasheets for GSK 626616
References for GSK 626616
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
If you know of a relevant reference for GSK 626616, please let us know.
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Keywords: GSK 626616, GSK 626616 supplier, GSK626616, potent, dyrk1, dyrk2, dyrk3, dual, specificity, tyrosine, phosphorylation, regulated, kinases, inhibitors, inhibits, selective, DYRK, 6638, Tocris Bioscience
1 Citation for GSK 626616
Citations are publications that use Tocris products. Selected citations for GSK 626616 include:
Scott R et al (2019) Mammalian cell growth dynamics in mitosis. Elife 8 PMID: 31063131
Do you know of a great paper that uses GSK 626616 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Alzheimer's Disease Poster
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