GSK 583

Pricing Availability   Qty
Description: Potent RIPK2 inhibitor; orally bioavailable and cell permeable
Chemical Name: 6-[(1,1-Dimethylethyl)sulfonyl]-N-(5-fluoro-1H-indazol-3-yl)-4-quinolinamine
Purity: ≥98% (HPLC)
Citations (1)

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

M. Wt 398.45
Formula C20H19FN4O2S
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1346547-00-9
PubChem ID 67469084
Smiles CC(C)(S(=O)(C1=CC2=C(N=CC=C2NC3=NNC4=CC=C(C=C34)F)C=C1)=O)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
DMSO 39.84 100
ethanol 7.97 20

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.

Select a batch to recalculate based on the batch molecular weight:
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

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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

If you know of a relevant reference for GSK 583, please let us know.

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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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