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Merck
CN

SML0943

YM-1

Synonym(s):

2-[[3-Ethyl-5-(3-methyl-2(3H)-benzothiazolylidene)-4-oxo-2-thiazolidinylidene]methyl]-1-methyl-pyridinium chloride

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About This Item

Empirical Formula (Hill Notation):
C20H20ClN3OS2
CAS Number:
Molecular Weight:
417.98
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

assay

≥98% (HPLC)

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).


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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