SML1960

GSK583

≥98% (HPLC)

• 別名: GSK583, 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine, GSK′583, GSK-2616583A
• 実験式（ヒル表記法）: C₂₀H₁₉FN₄O₂S
• CAS番号: 1346547-00-9
• 分子量: 398.45
• UNSPSCコード: 51111800
• NACRES: NA.77

特性

• 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

詳細

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.

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable