SML2721

GSK8612

≥98% (HPLC)

• 別名: 4-(((5-Bromo-2-((3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)amino)methyl)benzenesulfonamide, 4-((5-Bromo-2-(3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-ylamino)pyrimidin-4-ylamino)methyl)benzenesulfonamide, GSK 8612, GSK-8612
• 実験式（ヒル表記法）: C₁₇H₁₇BrF₃N₇O₂S
• CAS番号: 2361659-62-1
• 分子量: 520.33
• MDL番号: MFCD32062739
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• フォーム: powder
• 色: white to beige
• 溶解性: DMSO: 2 mg/mL, clear
• 保管温度: 2-8°C
• SMILES記法: FC(F)(F)C[n]1nc(c(c1)Nc2nc(c(cn2)Br)NCc3ccc(cc3)[S](=O)(=O)N)C
• InChI Key: FFPHMUIGESPOTK-UHFFFAOYSA-N

詳細

生物化学的／生理学的作用

GSK8612 is a potent and highly selective tank-binding kinase-1 (TBK1) inhibitor (pIC₅₀ = 6.8; pK_d = 8.0 vs pK_a = 6.2/STK17B, 6.0/IKKε, 6.1/LRRK2, 6.0/FLT4, 5.8/ULK3, 5.7/BMP2K, 5.7/CSNK2A1, 5.6/CSNK2A2, 5.6/FLT4, 5.5/PIK3CD, <5.5/more than 270 kinases). GSK8612 inhibits IFNβ secretion induced by dsDNA containing virus or STING ligand cGAMP (IC₅₀ = 1.25 & 0.5 μM, respectively; THP-1), as well as suppresses TLR3 ligand poly(I:C)-induced IRF3 Ser396 phosphorylation (IC₅₀ = 1 μM; Ramos) and IFNα release (IC₅₀ = 0.79 μM; human PBMCs), a IFN positive feedback response steming from IFNβ.

Potent and highly selective tank-binding kinase-1 (TBK1) inhibitor.

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