HSP Modulators: Methylene Blue
Methylene Blue
Heat Shock Protein 70/HSP70 Inhibitor
CAS Number: 61-73-4
Molecular Formula: C16H18ClN3S
Molecular Weight: 319.85 g/mol
Research Areas: Cancer Research, Heat Shock, Apoptosis
Alternative Names: N-(7-(dimethylamino)-3H-phenothiazin-3-ylidene)-N-methylmethanaminium chloride
Biological Description
Methylene blue irreversibly inhibits heat-shock inducible Hsp72 by oxidizing Cys306. It has no inhibitory effect against cytosolic constitutive heat shock cognate Hsc70. Methylene blue inhibits Hsp70 ATPase turnover rate, with EC50 of 80 uM. It reduces tau levels in engineered tau-overexpressed HeLa cells. Methylene blue is a pleiotropic molecule that is not selective for Hsp70.
References:
- Jinwal UK, et al. Chemical Manipulation of Hsp70 ATPase Activity Regulates Tau Stability. J Neurosci. 2009;29(39):12079-88.
- Miyata et al., Cysteine reactivity distinguishes redox sensing by the heat-inducible and constitutive forms of heat shock protein 70. Chem Biol. 2012;19(11):1391-9.
- Thompson AD, et al. Analysis of the Tau-Associated Proteome Reveals That Exchange of Hsp70 for Hsp90 Is Involved in Tau Degradation. ACS Chem Biol. 2012;7(10):1677-86.