GSK583
6-[(1,1-Dimethylethyl)sulfonyl]-N-(5-fluoro-1H-indazol-3-yl)-4-quinolinamine
CAS: 1346547-00-9
Molecular Formula: C20H19FN4O2S
GSK583 - Names and Identifiers
GSK583 - Physico-chemical Properties
| Molecular Formula | C20H19FN4O2S |
| Molar Mass | 398.4539 |
| Density | 1.402±0.06 g/cm3(Predicted) |
| Boling Point | 652.9±55.0 °C(Predicted) |
| Solubility | DMSO: ≥ 37 mg/mL |
| Appearance | Form solid, color Pale yellow |
| pKa | 12.59±0.40(Predicted) |
| Storage Condition | under inert gas (nitrogen or Argon) at 2–8 °C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. |
| Physical and Chemical Properties | Bioactive GSK583 is a highly effective and selective RIP2 kinase inhibitor with an IC50 of 5 nM. GSK583 also inhibited TNF-α and IL-6 production, with an IC50 value of about 200 nM in explant culture. |
GSK583 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.51 ml | 12.549 ml | 25.097 ml |
| 5 mM | 0.502 ml | 2.51 ml | 5.019 ml |
| 10 mM | 0.251 ml | 1.255 ml | 2.51 ml |
| 5 mM | 0.05 ml | 0.251 ml | 0.502 ml |
Last Update：2024-01-02 23:10:35
GSK583 - Nature
| Solubility | Soluble in DMSO (up to at least 25 mg/ml). |
Last Update：2024-04-10 22:29:15
GSK583 - Uses and synthesis methods
Target
Target Value
RIP2
(Cell-free assay) 5 nM
RIP3
(Cell-free assay) 16 nM
in vitro studies
GSK583 has a similar binding affinity for RIP3 kinase to RIP2 (RIP2 FP IC50 = 5 nM; RIP3 FP IC50 = 16 nM). Nevertheless, GSK583 at concentrations up to 10 μM had no inhibitory effect on RIP3-dependent necrotic cell death in cell experiments. GSK583 effectively and concentration-dependently inhibited MDP-stimulated tumor necrotizing TNFα production in primary human monocytes with IC50 = 8 nM. After treatment with 1 μM GSK583, when Toll-like receptor (TLR2, TLR4, TLR7) or cytokine receptor (IL-1R, TNFR) is activated, the pro-inflammatory factor signal is not inhibited, but once NOD1 and NOD2 receptors are activated, the pro-inflammatory factor signal is completely inhibited. Although GSK583 has good kinase selectivity, it can also inhibit hERG channels and Cyp3A4, which will affect its development as a candidate drug.
In vivo studies
GSK583 has low clearance rate, medium distribution volume and oral biological activity in rats and mice. Although GSK583 does not produce a human pharmacodynamic response within an acceptable concentration range, affecting its subsequent development as a drug candidate, its pharmacokinetics in mice and rats make it an effective preclinical in vivo research tool that plays a role in acute inflammatory models.
Last Update：2024-04-09 01:59:50
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View History
GSK583
AF 710B
N-Boc-L-arginine hydrochloride monohydrate
4'-(4-羟基苯基)-2,2':6',2''-三联吡啶
2-Bromo-7-hydroxynaphthalene
2-[2-bromo-4-(tert-butyl)phenoxy]-1-(3,5-dimethyl-1H-pyrazol-1-yl)-1-ethanone
1,4-双(三甲基硅氧基)苯
BOC-L-DAB(Z)-OH DCHA
LORAZEPAM IMPURITY A
3-AMino-5-nitro-benzo[b]thiophene-2-carboxylic acid Methyl ester
AF 710B
N-Boc-L-arginine hydrochloride monohydrate
4'-(4-羟基苯基)-2,2':6',2''-三联吡啶
2-Bromo-7-hydroxynaphthalene
2-[2-bromo-4-(tert-butyl)phenoxy]-1-(3,5-dimethyl-1H-pyrazol-1-yl)-1-ethanone
1,4-双(三甲基硅氧基)苯
BOC-L-DAB(Z)-OH DCHA
LORAZEPAM IMPURITY A
3-AMino-5-nitro-benzo[b]thiophene-2-carboxylic acid Methyl ester