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Potent RIP2 kinase 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.
|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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
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 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
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