SML2825

I-BET469

≥98% (HPLC)

• 別名: 5-(1-(1,3-Dimethoxypropan-2-yl)-5-morpholino-1H-benzo[d]imidazol-2-yl)-1,3-dimethylpyridin-2(1H)-one, 5-[1-[2-Methoxy-1-(methoxymethyl)ethyl]-5-(4-morpholinyl)-1H-benzimidazol-2-yl]-1,3-dimethyl-2(1H)-pyridinone
• 実験式（ヒル表記法）: C₂₃H₃₀N₄O₄
• CAS番号: 2003197-53-1
• 分子量: 426.51
• UNSPSCコード: 12352200

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• 形状: powder
• 色: white to beige
• 溶解性: DMSO: 2 mg/mL, clear
• 保管温度: 2-8°C

詳細

生物化学的／生理学的作用

I-BET469 is an orally active bromodomain (BrD) inhibitor with selectivity toward a subset of bromodomain-containng proteins (BCPs) and BrDs (K_d in nM: BRD4 BrD1/2 = 1.5/2.9, BRD3 BrD1/2 = 2/2.3, BRD2 BrD1/2 = 2.3/2.8, BRDT BrD1/2 = 12/100, CREBBP = 37, EP300 = 49; K_d ≥4.8 μM toward 22 other BCPs). I-BET469 targets cellular BRD4 with high affinity (pK_d = 8.3 or K_d = 5.0 nM by NanoBRET) and shows in vivo efficacy in a murine acute endotoxic shock model (1, 3, 10 mg/kg po. 30 min prior to LPS) and a chronic T cell-dependent immunization model (IgG suppression on day 14 = 24% and 65%, respectively, with 0.3 mg/kg or 3 mg/kg daily po.).

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