YM-08

Blood-brain barrier permeable HSP70 Inhibitor

StressMarq catalog# SIH-122

CAS Number: 812647-88-4

Molecular Formula: C₁₉H₁₇N₃OS₂

Molecular Weight: 367.49 g/mol

 

Research Areas: Cancer Research, Heat Shock, Apoptosis, Cell Signalling, Neuroscience, Neurodegeneration, Alzheimer’s

Alternative Names: (2Z,5E)-3-ethyl-5-(3-methyl-1,3-benzothiazol-2-ylidene)-2-(pyridin-2-ylmethylidene)-1,3-thiazolidin-4-one, 3-Ethyl-5-(3-methyl-2(3H)–benzothiazolylidene)–2-(2-pyridinylmethylene)–4-thiazolidinone

 

Biological Description

YM-08 is a Heat Shock Protein 70 (Hsp70) inhibitor that is blood-brain barrier permeable. YM-08 is a neutral derivative of the Hsp70 inhibitor MKT-077. MKT-077 reduces tau levels in cellular models, but it cannot penetrate the blood brain barrier.

Although YM-08 is somewhat less effective than MKT-077 in anti-tau and anti-cancer assays, it selectively reduces pathogenic tau in brain slices, which MKT-077 cannot. Furthermore, YM-08 was not retained in the kidney, leading one to speculate that it would not have the nephrotoxicity that was a problem for MKT-077 in clinical trials.

 

References:

1. Miyata Y, et al. Synthesis and Initial Evaluation of YM-08, a Blood-Brain Barrier Permeable Derivative of the Heat Shock Protein 70 (Hsp70) Inhibitor MKT-077, Which Reduces Tau Levels. ACS Chem Neurosci. 2013;4(6):930-9.