| Identification | Back Directory | [Name]
GSK583 | [CAS]
1346547-00-9 | [Synonyms]
SK583
GSK583
CS-2216
GSK583, >98%
GSK-583;GSK 583
GSK583 >=98% (HPLC)
RIP2 kinase inhibitor 583
6-[(1,1-Dimethylethyl)sulfonyl]-N-(5-fluoro-1H-indazol-3-yl)-4-quinolinamine
4-Quinolinamine, 6-[(1,1-dimethylethyl)sulfonyl]-N-(5-fluoro-1H-indazol-3-yl)- | [Molecular Formula]
C20H19FN4O2S | [MDL Number]
MFCD30343846 | [MOL File]
1346547-00-9.mol | [Molecular Weight]
398.45 |
| Chemical Properties | Back Directory | [Boiling point ]
652.9±55.0 °C(Predicted) | [density ]
1.402±0.06 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Inert atmosphere,2-8°C | [solubility ]
Soluble in DMSO (up to at least 25 mg/ml). | [form ]
solid | [pka]
12.59±0.40(Predicted) | [color ]
Pale yellow | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. |
| Hazard Information | Back Directory | [Description]
GSK583 (1346547-00-9) is a highly selective and potent inhibitor of RIP2 kinase, IC50?= 5 nM human and IC50?= 2 nM rat.1?It also potently inhibits isolated RIP3 kinase (IC50?= 5 nM) but is inactive against RIP3 in cellular assays due to a very low KM,ATP. GSK583 blocks NOD2 signaling by interfering with XIAP-RIP2 binding resulting in decreased cytokine and chemokine production.1,2 | [Uses]
GSK 583, is a selective inhibitor of RIP-like interacting CLARP kinase RIP2 Kinase is a central component of the innate immune system and enables downstream signaling following activation of the pattern recognition receptors NOD1 and NOD2, leading to the production of inflammatory cytokines. | [in vivo]
GSK583 (0.1, 1, and 10 mg/kg, p.o.) inhibits serum KC (the rodent orthologue of IL-8) levels in rats in a dose-dependent manner, with an IC50 derived from rat blood concentrations of 50 nM (or 20 ng/mL). Similarly, GSK583 inhibits serum KC levels and recruitment of neutrophils into the peritoneal cavity in mice in a dose-dependent manner, with an IC50 of 37 nM (15 ng/mL) derived from mouse blood concentration[1]. | [storage]
Store at +4°C | [References]
1) Haile?et al.?(2016),?The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinoline-4-amine; J. Med. Chem.,?59?4867
2) Goncharov?et al.?(2018),?Disruption of XIAP-RIP2 Association Blocks NOD2-Mediated Inflammatory Signaling; Mol. Cell,?69?551 |
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