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Biological Activity for GSK 583
GSK 583 is a potent RIPK2 inhibitor (IC50 values are 2 and 5 nM at rat and human kinases, respectively). Displays selectivity for RIP2K over p38α, VEGFR2 and a panel of 300 kinases. Exhibits some inhibition at BRK and Aurora A. Also displays similar binding affinity, but no detectable functional activity at RIP3. Active in vivo. Moderately orally bioavailable and cell permeable.
Technical Data for GSK 583
|Storage||Store at +4°C|
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 583
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for GSK 583
The following data is based on the product molecular weight 398.45. 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||2.51 mL||12.55 mL||25.1 mL|
|5 mM||0.5 mL||2.51 mL||5.02 mL|
|10 mM||0.25 mL||1.25 mL||2.51 mL|
|50 mM||0.05 mL||0.25 mL||0.5 mL|
References for GSK 583
References are publications that support the biological activity of the product.
Haile et al (2016) The identification and pharmacological characterization of 6-(tert-butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a highly potent and selective inhibitor of RIP2 kinase. J.Med.Chem. 59 4867 PMID: 27109867
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Keywords: GSK 583, GSK 583 supplier, GSK583, Potent, RIP2, kinase, inhibitors, inhibits, oral, bioavailability, cell, permeable, receptor-interacting, protein, 1, RIP, Kinases, 6480, Tocris Bioscience
1 Citation for GSK 583
Citations are publications that use Tocris products. Selected citations for GSK 583 include:
Rui et al (2021) Integrated transcriptomic analysis of human tuberculosis granulomas and a biomimetic model identifies therapeutic targets. J Clin Invest 131 PMID: 34128839
Do you know of a great paper that uses GSK 583 from Tocris? Please let us know.
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