Merck
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SML1960

Sigma-Aldrich

GSK583

≥98% (HPLC)

All Photos(1)
Synonym(s):
GSK583, 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine, GSK′583, GSK-2616583A
Empirical Formula (Hill Notation):
C20H19FN4O2S
CAS Number:
1346547-00-9
Molecular Weight:
398.45

品質水準

100

アッセイ

≥98% (HPLC)

形状

powder

保管条件

desiccated
protect from light

色

white to beige

溶解性

DMSO: 20 mg/mL, clear

保管温度

2-8°C

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SML1960

GSK583

GSK2334470 ≥98% (HPLC)

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SML0217

GSK2334470

GSK343 ≥98% (HPLC)

Sigma-Aldrich

SML0766

GSK343

GSK626616 ≥98% (HPLC)

Sigma-Aldrich

SML3355

GSK626616

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

form

powder

form

powder

form

powder

form

powder

storage condition

desiccated, protect from light

storage condition

-

storage condition

-

storage condition

-

color

white to beige

color

white to light brown

color

, white to beige to brown

color

white to beige

solubility

DMSO: 20 mg/mL, clear

solubility

DMSO: ≥10 mg/mL

solubility

DMSO: 15 mg/mL, clear

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°C

生物化学的／生理学的作用

GSK583 is a cell-permeable indazolylquinolinamine that acts as an ATP-competitive (IC50 = 2 & 5 nM using rat & human RIPK2, respectively) inhibitor against RIPK2 kinase activity (66.6% inhibition at 1 μM; [ATP] = 10 μM), exhibiting much reduced or no inhibitory potency against a panel of 209 other kinases <34% inhibition at 1 μM; [ATP] = 10 ?M). GSK583 selectively inhibits against NOD1- and NOD2-, but not TLR2-, TLR4-, TLR7-. IL-1R-, or TNFR-dependent pro-inflammatory cytokines release (>95% inhibition vs. <40% inhibition at 1 ?M using primary human monocytes stimulated with respective ligands). GSK583 effectively inhibits TNF? and IL-6 production from Crohn′s disease (CD) and ulcerative colitis (UC) patients intestinal explant cultures ex vivo (IC50 = 200 nM) and is efficacious against NOD1 ligand FK156- and NOD2 ligand MDP-induced inflammatory responses in mice and rats (10 mg/kg p.o.) in vivo.

保管分類コード

11 - Combustible Solids

WGK

WGK 3

引火点(°F)

Not applicable

引火点(℃)

Not applicable

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