SML0943

YM-1

• 別名: 2-[[3-Ethyl-5-(3-methyl-2(3H)-benzothiazolylidene)-4-oxo-2-thiazolidinylidene]methyl]-1-methyl-pyridinium chloride
• 実験式（ヒル表記法）: C₂₀H₂₀ClN₃OS₂
• CAS番号: 409086-68-6
• 分子量: 417.98
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• アッセイ: ≥98% (HPLC)
• 品質水準: 100
• 形状: powder
• 色: orange to dark red
• 溶解性: H₂O: 2 mg/mL, clear (warmed)
• 保管温度: 2-8°C

詳細

アプリケーション

YM-1 has been used as a Hsp70 (heat shock protein) inhibitor in cell viability assay.

生物化学的／生理学的作用

YM-1 modulates Hsp70 activity by binding to the nucleotide-binding domain of ADP- but not ATP-bound Hsp70, stabilizing Hsp70 in its ADP-bound conformation. The ADP-bound state has tight affinity for its substrates, promoting their ubiquitination and degradation, and a greatly reduced off rate compared to the ATP-bound state. YM-1 appears to behave in a similar manner to Hip, a Hsp70 co-chaperone that stabilizes Hsp70 in its ADP-bound conformation which favors degradation of misfolded substrates such as those involved in various neurodegenerative diseases.

YM-1 also has anticancer activity, which could be due to enhanced ubiquitination and clearance of Akt, a major survival kinase. In studies with multiple cancer lines, YM-1 was found to selectively target cancer cells over normal cells and to overcome tamoxifen resistance in a tamoxifen-resistant MCF7 cell model. YM-1 had greater efficacy and cytosolic localization than the closely related MKT-077 (M5449).

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