HSP70 INHIBITOR PES-CL (C15-1305-041)

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Molecular Weight: 215.66. Empirical Formula: C₈H₆ClNO₂S. Assay: ≥. 98% (HPLC). Quality Level: 100. form: powder. potency: 2-5 . μ. M IC₅₀. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: white. solubility: DMSO: 100 . mg/mL. storage temp.: 2-8°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.