5.31067
HSP70 Inhibitor, PES-Cl
Synonym(s):
HSP70 Inhibitor, PES-Cl, Heat Shock Protein 70 Inhibitor
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About This Item
Empirical Formula (Hill Notation):
C8H6ClNO2S
CAS Number:
Molecular Weight:
215.66
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
Assay
≥98% (HPLC)
Quality Level
form
powder
potency
2-5 μM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
white
solubility
DMSO: 100 mg/mL
storage temp.
2-8°C
General description
A cell-permeable chlorophenylethynylsulfonamide compound that binds directly to the substrate-binding domain of heat shock protein 70 (HSP70) and disrupts its interaction with client proteins. Impairs the activity of the anaphase promoting complex/cyclosome (APC/C) in cell-free extracts. Arrests cell cycle at G2/M phase and preferentially induces genomic instability in cancer cells (IC50 = 2 to 5 µM in melanoma cell lines). Exhibits much reduced toxicity in non-transformed cells (IC50 >100 µM in primary melanocytes). Induces apoptosis and inhibits autophagy as evidenced by increased p62SQSTM1 and LC3 accumulation. Also, shown to extend life in murine models of pre-B cell lymphoma.
A cell-permeable chlorophenylethynylsulfonamide compound that binds directly to the substrate-binding domain of heat shock protein 70 (HSP70) and disrupts its interaction with client proteins. Impairs the activity of the anaphase promoting complex/cyclosome (APC/C) in cell-free extracts. Arrests cell cycle at G2/M phase and preferentially induces genomic instability in cancer cells (IC50 = 2 to 5 µM in melanoma cell lines). Exhibits much reduced toxicity in non-transformed cells (IC50 >100 µM in primary melanocytes). Induces apoptosis and inhibits autophagy as evidenced by increased p62SQSTM1 and LC3 accumulation. Also, shown to extend life in murine models of pre-B cell lymphoma.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
HSP70
HSP70
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Balaburski, G., et al. 2013. Mol. Cancer Res.11, 1.
Budina-Kolomets, A. et al. 2013. Cancer Biol. Ther.15, 194.
Budina-Kolomets, A. et al. 2013. Cancer Biol. Ther.15, 194.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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Anna Budina-Kolomets et al.
Cancer biology & therapy, 15(2), 194-199 (2013-10-09)
The chaperone HSP70 promotes the survival of cells exposed to many different types of stresses, and is also potently anti-apoptotic. The major stress-induced form of this protein, HSP70-1, is overexpressed in a number of human cancers, yet is negligibly expressed
Gregor M Balaburski et al.
Molecular cancer research : MCR, 11(3), 219-229 (2013-01-11)
The stress-induced HSP70 is an ATP-dependent molecular chaperone that plays a key role in refolding misfolded proteins and promoting cell survival following stress. HSP70 is marginally expressed in nontransformed cells, but is greatly overexpressed in tumor cells. Silencing HSP70 is
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