All Photos(1)
Synonym(s):
HSP70 Inhibitor, PES-Cl, Heat Shock Protein 70 Inhibitor
Empirical Formula (Hill Notation):
C8H6ClNO2S
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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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
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
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