SML0943

YM-1

• Synonym(e): 2-[[3-Ethyl-5-(3-methyl-2(3H)-benzothiazolylidene)-4-oxo-2-thiazolidinylidene]methyl]-1-methyl-pyridinium chloride
• Empirische Formel (Hill-System): C₂₀H₂₀ClN₃OS₂
• CAS-Nummer: 409086-68-6
• Molekulargewicht: 417.98
• NACRES: NA.77
• UNSPSC Code: 12352200
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• assay: ≥98% (HPLC)
• Quality Segment: 100
• form: powder
• color: orange to dark red
• solubility: H₂O: 2 mg/mL, clear (warmed)
• storage temp.: 2-8°C

Beschreibung

Application

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

Biochem/physiol Actions

YM-1 is a Hsp70 modulator; anticancer agent.

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).

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• Was ist los?: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable