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A propos de cet article
Formule empirique (notation de Hill) :
C20H20ClN3OS2
Numéro CAS:
Poids moléculaire :
417.98
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
powder
Service technique
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≥98% (HPLC)
Quality Segment
form
powder
color
orange to dark red
solubility
H2O: 2 mg/mL, clear (warmed)
storage temp.
2-8°C
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).
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).
Classe de stockage
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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