SML1731

A64 trifluoroacetate

≥98% (HPLC)

• 別名: 5-((6-Oxo-5-(6-(piperazin-1-yl)pyridin-3-yl)-1,6-dihydropyridin-3-yl)methylene)thiazolidine-2,4-dione trifluoroacetate
• 実験式（ヒル表記法）: C₁₈H₁₇N₅O₃S · xC₂HF₃O₂
• CAS番号: 2123107-10-6
• 分子量: 383.42 (free base basis)
• UNSPSCコード: 12352200
• PubChem Substance ID: 329826044
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• 形状: powder
• 色: white to beige
• 溶解性: H₂O: 10 mg/mL, clear
• 保管温度: 2-8°C
• SMILES記法: O=C1NC=C(/C=C2SC(NC\2=O)=O)C=C1C3=CC=C(N4CCNCC4)N=C3.FC(F)(C(O)=O)F

詳細

生物化学的／生理学的作用

A64 is a cell-permeable, ATP site-targeting pyridone thiazolidinedione compound that acts as a potent HIPK2-selective homeodomain-interacting protein kinase inhibitor (IC₅₀ = 74 nM and 136 nM against HIPK2 and HIPK1, respectively; [ATP] = 100 μM), affecting MPF only at higher concentrations (by 35% at 5 μM; [ATP] = 10 μM) and exhibiting little potency toward CDK1 (IC₅₀ >10 μM). A64 (1 μM) effectively prevents ER stresser tunicamycin (1 μg/mL) -induced HIPK2/JNK phosphorylation and cell death in HEK293 and primary rat motor neuron cultures. HIPK2 inhibition by A64 treatment is also efficacious in protecting rat motor neurons from death upon exogenous SOD1 G93A or TDP-43 expression. ff-target kinases revealed by kinome profiling include DYRK1A, CSNK2A2, DAPK2, DAPK1, PIM3, CSNK2A1, PIM1 (Kd = 8.8, 6.1, 6.1, 9.5, 3.7, 31, 37 nM, respectively) and DYRK1B (IC₅₀ = 62 nM).

安全性情報

• ピクトグラム: GHS07
• シグナルワード: Warning
• 危険有害性情報: H315,H319,H335
• 注意書き: P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338
• 危険有害性の分類: Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• ターゲットの組織: Respiratory system
• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable